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| Yoshiaki Kiso, Ph.D. 1 Haruaki Yajima, Yoshiaki Kiso, Studies on peptides XXV. A convenient procedure for the preparation of p-methoxybenzyl azidoformate. Chem. Pharm. Bull., 17 (9), 1962-1964 (1969). 2 H. Yajima, H. Kawatani, Y. Kiso: Peptides. Warning for the explosive carbazide formation during the direct preparation of tert-butyl azidoformate or p-methoxybenzyl azidoformate. Chem. Pharm. Bull., 18 (4), 850-851 (1970). 3 Haruaki Yajima, Koichi Kawasaki, Hideo Minami, Hiroki Kawatani, Nariakira Mizokami, Yoshiaki Kiso, Fusako Tamura: Studies on peptides. XXVIII. Synthesis of the docosapeptide which embodies the entire amino acid sequence of beta-melanocyte-stimulating hormone from human pituitary gland. Chem. Pharm. Bull., 18 (7), 1394-1401 (1970). 4 Haruaki Yajima, Fusako Tamura, Yoshiaki Kiso, Studies on peptides. XXIX. p-Methoxybenzyl mixed carbonates. Chem. Pharm. Bull., 18 (12), 2574-2576 (1970). 5 Haruaki Yajima, Yoshiaki Kiso, Studies on peptides. XXX. Trichloroethyloxycarbonylhydrazine. Chem. Pharm. Bull., 19 (2), 420-423 (1971). 6 Haruaki Yajima, Norio Shirai, Yoshiaki Kiso, Studies on peptides. XXXI. Synthesis of two model pentapeptides related to clostridial ferredoxin. Chem. Pharm. Bull., 19 (9), 1900-1904 (1971). 7 H. Yajima, K. Kawasaki, Y. Okada, H. Kawatani, Y. Kiso, Synthetic aspects of human ß-melanocyte-stimulating hormone. Progress in Peptide Research, 2, 317-325 (1972). 8 Y. Kiso, H. Yajima, 2-Isobutoxy-1-isobutoxycarbonyl-1,2-dihydroquinoline as a coupling reagent in peptide synthesis. J. Chem. Soc., Chem. Commun., (16), 942-943 (1972). 9 H. Yajima, F. Tamura, Y. Kiso, M. Kurobe, Studies on peptides. XXXV. Some p-methoxybenzyloxycarbonyl-amino acid derivatives. Chem. Pharm. Bull., 21 (6), 1380-1382 (1973). 10 Y. Kiso, Y. Kai, H. Yajima, Studies on peptides. XXXIX. N-Isobutoxycarbonyl-2-alkoxy-1, 2-dihydroquinoline derivatives, as coupling reagents in peptide synthesis. Chem. Pharm. Bull., 21(11), 2507-2510 (1973). 11 H. Yajima, Y. Kiso, Y. Okada, H. Watanabe, Synthesis of the basic trypsin inhibitor from bovine pancreas (Kunitz and Northrop) by fragment condensation on a polymer support. J. Chem. Soc., Chem. Commun., 106-107 (1974). 12 H. Yajima, Y. Kiso, Studies on peptides. XL. Synthesis of the protected dodecapeptide corresponding to positions 1 to 12 of the basic trypsin inhibitor from bovine pancreas (Kunitz and Northrop). Chem. Pharm. Bull., 22(5), 1061-1066 (1974). 13 H. Yajima, Y. Okada, H. Watanabe, Y. Kiso, Studies on peptides. XLI. Synthesis of the protected hexadecapeptide corresponding to positions 13 to 28 of the basic trypsin inhibitor from bovine pancreas (Kunitz and Northrop). Chem. Pharm. Bull., 22(5), 1067-1074 (1974). 14 H. Yajima, N. Mizokami, M. Kiso, T. Jinnouchi, Y. Kai, Y. Kiso, Studies on peptides. XLII. Synthesis of the protected nonapeptide corresponding to positions 29 to 37 of the basic trypsin inhibitor from bovine pancreas (Kunitz and Northrop). Chem. Pharm. Bull., 22(5), 1075-1078 (1974). 15 H. Yajima, Y. Kiso, K. Kitagawa, Studies on peptides. XLIII. Synthesis of two protected peptides related to the C-terminal portion of the basic trypsin inhibitor from bovine pancreas (Kunitz and Northrop). Chem. Pharm. Bull., 22(5), 1079-1086 (1974). 16 H. Yajima, Y. Kiso, Studies on peptides. XLIV. Synthesis of basic trypsin inhibitor from bovine pancreas (Kunitz and Northrop) by the fragment condensation procedure on polymer support. Chem. Pharm. Bull., 22 (5), 1087-1094 (1974). 17 H. Yajima, Y. Kiso, H. Ogawa, N. Fujii, H. Irie, Studies on peptides. L. Acidolysis of protecting groups in peptide chemistry by fluorosulphonic acid and methanesulphonic acid. Chem. Pharm. Bull., 23 (5), 1164-1166 (1975). 18 K. Koyama, Y. Mori, Y. Kiso, S. Hirabayashi, H. Yajima, Studies on peptides. LIII. Synthesis of the docosapeptide corresponding to the entire amino acid sequence of porcine ACTH-like intermediate lobe peptide (CLIP). Chem. Pharm. Bull., 23 (10), 2301-2305 (1975). 19 F. Tamura, Y. Kiso, H. Yajima, A. Tanaka, M. Nakamura, Studies on peptides. LVII. Synthesis of the octadecapeptide corresponding to the entire amino acid sequence of equine ß-melanocyte-stimulating hormone. Chem. Pharm. Bull., 23 (10), 2405-2409 (1975). 20 H. Yajima, Y. Kiso, Structure-function relationships of the melanotropins. Pharmacol. Therap. B, 1, 529-543 (1975). 21 H. Yajima, K. Koyama, Y. Kiso, A. Tanaka, M. Nakamura, Studies on peptides. LIX. Synthesis of the nonatriacontapeptide corresponding to the entire amino acid sequence of porcine adrenocorticotropic hormone. Chem. Pharm. Bull., 24, 492 (1976). 22 H. Yajima, Y. Mori, Y. Kiso, K. Koyama, T. Tobe, M. Setoyama, H. Adachi, T. Kanno, A. Saito, Synthesis of [27-Tyr]-cholecystokinin-pancreozymin (CCK-PZ). Chem. Pharm. Bull., 24 (5), 1110-1113 (1976). 23 Y. Mori, K. Koyama, Y. Kiso, H. Yajima, Studies on peptides. LXVII. Synthesis of the hexadecapeptide corresponding to position 1 through 16 of porcine cholecystokinin-pancreozymin (CCK-PZ). Chem. Pharm. Bull., 24 (11), 2788-2793 (1976). 24 K. Hofmann, Y. Kiso, An approach to the targeted attachment of peptides and proteins to solid supports. Proc. Nat. Acad. Sci., U.S.A., 73 (10), 3516-3518 (1976). 25 K. Hofmann, F. M. Finn, Y. Kiso, Avidin-biotin affinity columns. General methods for attaching biotin to peptides and proteins. J. Amer. Chem. Soc., 100 (11), 3585-3590 (1978). 26 Yoshiaki Kiso, Hiroko Isawa, Kouki Kitagawa, Tadashi Akita, Suppressing effect of thioanisole on a side reaction during the acidolytic cleavage of protecting groups of tyrosine. Chem. Pharm. Bull., 26 (8), 2562-2564 (1978). 27 Yoshiaki Kiso, Kaoru Ito, Shizuo Nakamura, Kouki Kitagawa, Tadashi Akita, Hideki Moritoki, A deblocking method using thioanisole-sulfonic acid system. Application to the synthesis of Met-enkephalin. Peptide Chemistry 1978, 25-28, (1979). 28 K. Kitagawa, K. Ujita, Y. Kiso, T. Akita, Y. Nakata, N. Nakamoto, T. Segawa, H. Yajima, Synthesis and activity of C-terminal heptapeptides of tachykinins and bombesin-like peptides. Chem. Pharm. Bull., 27, 48 (1979). 29 Y. Kiso, K. Ito, S. Nakamura, K. Kitagawa, T. Akita, H. Moritoki, A deblocking method using thioether-sulfonic acid systems. Application to the synthesis of Met-enkephalin. Chem. Pharm. Bull., 27 (6), 1472-1475 (1979). 30 K. Kitagawa, K. Kitade, Y. Kiso, T. Akita, S. Funakoshi, N. Fujii, H. Yajima, Nin-p-Methoxyphenylsulphonylhistidine, a new derivative for peptide synthesis. J. Chem. Soc., Chem. Commun., 955, (1979). 31 Yoshiaki Kiso, Shizuo Nakamura, Kaoru Ito, Kazuko Ukawa, Kouki Kitagawa, Tadashi Akita, Hideki Moritoki, Deprotection of O-methyltyrosine by a ‘push-pull’ mechanism using the thioanisole-trifluoromethanesulphonic acid system. Application to the convenient synthesis of a potent N-methylenkephalin derivative. J. Chem. Soc., Chem. Commun., 971-972 (1979). 32 Yoshiaki Kiso, Kazuko Ukawa, Masahiko Satomi, Shizuo Nakamura, Kouki Kitagawa, Tadashi Akita, Efficient removal of protecting groups and peptide synthesis by a ‘push-pull’ mechanism. Peptide Chemistry 1979, 193-198 (1980). 33 Yoshiaki Kiso, Shizuo Nakamura, Kazuko Ukawa, Kouki Kitagawa, Tadashi Akita, Hideki Moritoki, Synthesis and activity of enkephalin analogs. Peptide Chemistry 1979, 199-204 (1980) 34 Yoshiaki Kiso, Kazuko Ukawa, Shizuo Nakamura, Kaoru Ito, Tadashi Akita, Efficient removal of protecting groups by a ‘push-pull’ mechanism. II. Deprotection of O-benzyltyrosine with a thioanisole-trifluoroacetic acid system without O-to-C rearrangements. Chem. Pharm. Bull., 28 (2), 673-676 (1980). 35 Yoshiaki Kiso, Kazuko Ukawa, Tadashi Akita, Efficient removal of N-benzyloxycarbonyl group by a ‘push-pull’ mechanism using thioanisole-trifluoroacetic acid, exemplified by a synthesis of Met-enkephalin. J. Chem. Soc., Chem. Commun., 101-102 (1980). 36 K. Kitagawa, K. Kitade, Y. Kiso, T. Akita, S. Funakoshi, N. Fujii, H. Yajima, Studies on peptides. LXXXV. A new deprotecting procedure for p-toluenesulfonyl and p-methoxybenzenesulfonyl groups from the Nim-function of histidine. Chem. Pharm. Bull., 28, 926 (1980). 37 Yoshiaki Kiso, Toshitsugu Miyazaki, Masahiko Satomi, Hidemi Hiraiwa, Tadashi Akita, An ‘active ester’-type mixed anhydride method for peptide synthesis. Use of the new reagent, norborn-5-ene-2,3-dicarboximido diphenyl phosphate (NDPP). J. Chem. Soc., Chem. Commun., 1029-1030 (1980). 38 Yoshiaki Kiso, Masahiko Satomi, Kazuko Ukawa, Tadashi Akita, Efficient deprotection of NG-tosylarginine with a thioanisole-trifluoromethanesulphonic acid system. J. Chem. Soc., Chem. Commun., 1063-1064 (1980). 39 H. Moritoki, Y. Kiso, T. Kageyama, K. Matsumoto, Morphine-like activities of synthetic enkephalin analogues. J. Pharm. Pharmacol., 33, 54-55 (1981). 40 Yoshiaki Kiso, Toshitsugu Miyazaki, Masahiko Satomi, Hidemi Hiraiwa, Tadashi Akita, An ‘active-ester’-type mixed anhydride method for peptide synthesis. Peptide Chemistry 1980, 1-4 (1981). 41 Yoshiaki Kiso, Masahiko Satomi, Toshitsugu Miyazaki, Hidemi Hiraiwa, Tadashi Akita, A new method for racemization test in peptide synthesis: use of reversed-phase high performance liquid chromatography. Peptide Chemistry 1980, 71-74 (1981). 42 Yoshiaki Kiso, Masanaga Yamaguchi, Shizuo Nakamura, Masahiko Satomi, Tadashi Akita, Hideki Moritoki, Masao Takei, Shinji Fujita, Takefumi Kageyama, Keizo Matsumoto, Opioid activities of enkephalin analogs. Peptide Chemistry 1980, 187-192 (1981). 43 Yoshiaki Kiso, Masanaga Yamaguchi, Tadashi Akita, Hideki Moritoki, Masao Takei, Hideo Nakamura, Super-active enkephalin analogues. Simple tripeptide hydroxyalkylamide exhibit surprisingly high and long-lasting opioid activities. Naturwissenschaften, 68, 210-212 (1981). 44 Yoshiaki Kiso, Toshitsugu Miyazaki, Tadashi Akita, Hideo Nakamura, Syndyphalin, an enkephalin-like peptide with prolonged subcutaneous analgesic activity. Eur. J. Pharmacol., 71, 347-348 (1981). 45 Yoshiaki Kiso, Toshitsugu Miyazaki, Tadashi Akita, Hideki Moritoki, Masao Takei, Hideo Nakamura, Syndyphalin-33, a synthetic tripeptide alkylamide with prolonged analgesic activity. FEBS Letters, 136 (1), 101-104 (1981). 46 Yoshiaki Kiso, Toshitsugu Miyazaki, Masanaga Yamaguchi, Tadashi Akita, Hideki Moritoki, Masao Takei, Hideo Nakamura, “Minimal segment” of enkephalin for analgesia: syndyphalin (SD)-33, a simple tripeptide alkylamide with prolonged subcutaneous analgesic activity. Advances in Endogenous & Exogenous Opioids, 386-388 (1981). 47 Yoshiaki Kiso, Toshitsugu Miyazaki, Masahiko Satomi, Masatoshi Inai, Tadashi Akita, Hideki Moritoki, Masao Takei, Hideo Nakamura, Synthesis and activity of short-chain enkephalin-like peptides. Peptide Chemistry 1981, 65-70 (1982). 48 Remi Quirion, Yoshiaki Kiso, Candice B. Pert: Syndyphalin SD-25: a highly selective ligand for mu opiate receptors. FEBS Letters, 141 (2), 203-206 (1982). 49 Hiroshi Takagi, Hirohito Shiomi, Kiyoshi Fukui, Kyozo Hayashi, Yoshiaki Kiso, Kouki Kitagawa, Isolation of a novel analgesic pentapeptide, neo-kyotorphin, from bovine brain. Life Sci., 31 (16/17), 1733-1736 (1982). 50 Hideo Nakamura, Yoshiaki Kiso, Satoru Motoyoshi, Naoyuki Yoshida, Katsumi Ishii, Yuichi Yokoyama, Toshiaki Kadokawa, Masanao Shimizu, Analgesic and other pharmacological activities of an enkephalin analogue, syndyphalin (SD)-25. Eur. J. Pharmacol., 85 (2), 133-142 (1982). 51 Kiyoshi Fukui, Hirohito Shiomi, Hiroshi Takagi, Kyozo Hayashi, Yoshiaki Kiso, Kouki Kitagawa, Isolation from bovine brain of a novel analgesic pentapeptide, neo-kyotorphin, containing the Tyr-Arg (kyotorphin) unit. Neuropharmacol., 22 (2), 191-196 (1983). 52 Yoshiaki Kiso, Masatoshi Inai, Kunio Yoneto, Kouki Kitagawa, Tadashi Akita, Protection of the tryptophan indole ring in peptide synthesis. Peptide Chemistry 1982, 65-68 (1983). 53 Kouki Kitagawa, Nobuyuki Kawai, Yoshiaki Kiso, Tadashi Akita, Kiyoshi Fukui, Hiroo Amano, Hiroshi Takagi, Synthesis and activity of a newly isolated analgesic pentapeptide: neo-kyotorphin. Peptide Chemistry 1982, 241-244 (1983). 54 Yoshiaki Kiso, Toshitsugu Miyazaki, Masatoshi Inai, Kouki Kitagawa, Tadashi Akita, Hideki Moritoki, Hideo Nakamura, Synthesis and activity of opioid peptides. Peptide Chemistry 1982, 245-250 (1983). 55 Yoshiaki Kiso, Masatoshi Inai, Kouki Kitagawa, Tadashi Akita, Protection of the tryptophan indole ring in peptide synthesis. Use of a new derivative, Nin-2, 2, 2-trichloroethoxycarbonyltryptophan. Chem. Lett., (5), 739-742 (1983). 56 Yoshiaki Kiso, Kouki Kitagawa, Nobuyuki Kawai, Tadashi Akita, Hiroshi Takagi, Hiroo Amano, Kiyoshi Fukui, Neo-kyotorphin (Thr-Ser-Lys-Tyr-Arg), a new analgesic peptide. FEBS Letters, 155 (2), 281-284 (1983). 57 Yoshiaki Kiso, Masatoshi Inai, Kouki Kitagawa, Tadashi Akita, Hideki Moritoki, Synthesis of a newly isolated opioid tridecapeptide, rimorphin, from pituitary using a trifluoroacetic acid-thioanisole deprotection system. Chem. Pharm. Bull., 31 (5), 1818-1820 (1983). 58 Kouki Kitagawa, Nobuyuki Kawai, Yoshiaki Kiso, Tadashi Akita, Kiyoshi Fukui, Hiroo Amano, Hiroshi Takagi, Synthesis and activity of a newly isolated analgesic pentapeptide, neo-kyotorphin. Chem. Pharm. Bull., 31 (7), 2349-2352, (1983). 59 Hideki Moritoki, Hiroshi Fukuda, Yukio Ishida, Yoshiaki Kiso, Neuronal opiate receptors in rabbit ear artery. Jpn. J Pharmacol., 33, 297P (1983). 60 Kiyoshi Fukui, Hiroo Amano, Yoshiaki Kiso, Kouki Kitagawa, Hiroshi Takagi, The analgesic activity of neo-kyotorphin. a newly identified pentapeptide from bovine brain. Pharmaceut. Res., (1), 39 (1984). 61 Yoshiaki Kiso, Masatoshi Inai, Kouki Kitagawa, Tadashi Akita, Hideki Moritoki, Takahiro Nakazawa, Tetsuo Oka, Synthesis and activity of rimorphin (dynorphin B) and related peptides. Peptide Chemistry 1983, 93-98 (1984). 62 Hideki Moritoki, Masao Takei, Masahiro Kotani, Yoshiaki Kiso, Yukio Ishida, Kouichi Endoh, Tripeptides acting on opioid receptors in rat colon. Eur. J. Pharmacol., 100 (1), 29-39 (1984). 63 Yoshiaki Kiso, Toshitsugu Miyazaki, Masatoshi Inai, Kouki Kitagawa, Tadashi Akita, Hideki Moritoki, Hideo Nakamura, Syntheses and opioid activities of enkephalin- and dermorphin-related peptides. J. Pharmacobio-Dyn., 7 (5), s-91 (1984). 64 Kenji Okamoto, Koichi Yasumura, Kazuyoshi Fujitani, Yoshiaki Kiso, Hiroshi Kawauchi, Ichiro Kawazoe, Haruaki Yajima, Synthesis of the heptadecapeptide corresponding to the entire amino acid sequence of salmon melanin-concentrating hormone (MCH). Chem. Pharm. Bull., 32 (8), 2963-2970 (1984). 65 Hideki Moritoki, Masao Takei, Yoshiaki Kiso, Yukio Ishida, Kouichi Endoh, Tripeptides acting on opioid receptors in rat colon. Jpn. J. Pharmacol., 36, 179P (1984). 66 Kazuwa Nakao, Akira Sugawara, Narito Morii, Makoto Sakamoto, Mitsuaki Suda, Junichi Soneda, Toshiaki Ban, Masahiro Kihara, Yukio Yamori, Masanori Shimokura, Yoshiaki Kiso, Hiroo Imura, Radioimmunoassay for alpha-human and rat atrial natriuretic polypeptide. Biochem. Biophys. Res. Commun., 124 (3), 815-821 (1984). 67 菅原照, 中尾一和, 須田光明, 坂本誠, 森井成人, 吉政孝明, 木原正博, 家森幸男, 霜倉正徳, 木曽良明, 井村裕夫, α-human atrial natriuretic polypeptide (α-hANP) のラジオイムノアッセイ(RIA). 高血圧 ,7 (1), 73 (1984). Akira Sugawara, Kazuwa Nakao, Mitsuaki Suda, Makoto Sakamoto, Narito Morii, Takaaki Yoshimasa, Masahiro Kihara, Yukio Yamori, Masanori Shimokura, Yoshiaki Kiso, Hiroo Imura: Radioimmunoassay of alpha-human atrial natriuretic polypeptide (alpha-hANP). Kouketsuatsu, 7 (1), 73 (1984). 68 米原典史, 工藤照夫, 張恵珍, 中前順次, 猪木令三, 木曽良明, オピオイドペプチドならびに関連薬物の浮腫抑制効果, 炎症, 4 (4),445ｰ446 (1984). Norifumi Yonehara, Teruo Kudo, Huei-Ling Chang, Junji Nakamae, Reizo Inoki, Yoshiaki Kiso. Inhibition of edema by opioid peptides and related drugs. Ensho, 4 (4),445ｰ446 (1984). 69 Kouki Kitagawa, Nobuyuki Kawai, Shinya Kiyama, Tadashi Akita, Yoshiaki Kiso, Hiroshi Ueda, Ge Ming, Hiroshi Takagi, Synthesis and analgesic activity of neo-kyotorphin analogs. Chem. Pharm. Bull., 33 (1), 377-382 (1985). 70 Narito Morii, Kazuwa Nakao, Akira Sugawara, Makoto Sakamoto, Mitsuaki Suda, Masanori Shimokura, Yoshiaki Kiso, Masahiro Kihara, Yukio Yamori, Hiroo Imura, Occurrence of atrial natriuretic polypeptide in brain. Biochem. Biophys. Res. Commun., 127 (2), 413-419 (1985). 71 Yoshiaki Kiso, Kenji Okamoto, Masaki Makiyama, Masanori Shimokura, Yoshikatsu Hirai, Kazuyoshi Kawai, Hiroshi Kikuishi, Preparation of a monoclonal antibody to a synthetic peptide related to human interleukin-2 (IL-2, T-cell growth factor) and affinity-purification of IL-2 produced by recombinant gene. Peptide Chemistry 1984, 103-108 (1985). 72 Masanori Shimokura, Satoshi Hosoi, Kenji Okamoto, Yoichi Fujiwara, Makoto Yoshida, Yoshiaki Kiso, Synthesis of a-human and rat atrial natriuretic polypeptide (a-hANP, a-rANP) using a new deprotecting procedure. Peptide Chemistry 1984, 235-240 (1985). 73 Yoshiaki Kiso, Toshio Fujisaki, Masanori Shimokura, Kenji Okamoto, Mika Kaimoto, Sakae Uemura, Synthesis of a novel endogenous opioid peptide, adrenorphin-metorphamide using a new deprotecting procedure. Peptide Chemistry 1984, 289-294 (1985). 74 Yoshiaki Kiso, Masanori Shimokura, Satoshi Hosoi, Toshio Fujisaki, Yoichi Fujiwara, Makoto Yoshida, Kazuwa Nakao, Akira Sugawara, Narito Morii, Makoto Sakamoto, Mitsuaki Suda, Hiroo Imura, Masahiro Kihara, Kengo Nakayama, Yukio Yamori, Biological properties of synthetic peptides related to atrial natriuretic hormone. Peptide Chemistry 1984, 305-310 (1985). 75 Masahiro Kihara, Kengo Nakayama, Kazuwa Nakao, Akira Sugawara, Narito Morii, Makoto Sakamoto, Mitsuaki Suda, Masanori Shimokura, Yoshiaki Kiso, Hiroo Imura, Yukio Yamori, Accelerated natriuresis induced by synthetic atrial natriuretic polypeptide in spontaneously hypertensive rats. Clin. Exp. Hypertension, Theory Practice A, 7 (4), 539-551 (1985). 76 Makoto Sakamoto, Kazuwa Nakao, Masahiro Kihara, Narito Morii, Akira Sugawara, Mitsuaki Suda, Masanori Shimokura, Yoshiaki Kiso, Yukio Yamori, Hiroo Imura, Existence of atrial natriuretic polypeptide in kidney. Biochem. Biophys. Res. Commun., 128 (3), 1281-1287 (1985). 77 Akira Sugawara, Kazuwa Nakao, Narito Morii, Makoto Sakamoto, Mitsuaki Suda, Masanori Shimokura, Yoshiaki Kiso, Masahiro Kihara, Yukio Yamori, Kazunobu Nishimura, Junichi Soneda, Toshihiko Ban, Hiroo Imura, a-Human atrial natriuretic polypeptide is released from the heart and circulates in the body. Biochem. Biophys. Res. Commun., 129 (2), 439-446 (1985). 78 Narito Morii, Kazuwa Nakao, Masahiro Kihara, Akira Sugawara, Makoto Sakamoto, Mitsuaki Suda, Masanori Shimokura, Yoshiaki Kiso, Yukio Yamori, Hiroo Imura, Atrial natriuretic polypeptides in SHR and SHR stroke-prone. Jpn. Heart J., 26 (4), 693 (1985). 79 Akira Sugawara, Kazuwa Nakao, Narito Morii, Makoto Sakamoto, Mitsuaki Suda, Masahiro Kihara, Yukio Yamori, Masanori Shimokura, Yoshiaki Kiso, Hiroo Imura, Radioimmunoassay for atrial natriuretic polypeptide. Jpn. Heart J., 26 (4), 694 (1985). 80 Jacob P. Mtabaji, Yuta Kobayashi, Masahiro Kihara, Kazuwa Nakao, Akira Sugawara, Mitsuaki Suda, Narito Morii, Makoto Sakamoto, Masanori Shimokura, Yoshiaki Kiso, Hiroo Imura, Yukio Yamori, Keisuke Hattori, Effects of a-human atrial natriuretic polypeptide on vascular strips and perfused mesenteric vessels of SHR and WKY. Jpn. Heart J., 26 (4), 695 (1985). 81 Masahiro Kihara, Kengo Nakayama, Kazuwa Nakao, Akira Sugawara, Narito Morii, Makoto Sakamoto, Mitsuaki Suda, Masanori Shimokura, Yoshiaki Kiso, Hiroo Imura, Yukio Yamori, Effect of synthetic atrial natriuretic polypeptide on diuresis, natriuresis and blood pressure in spontaneously hypertensive rats (SHR) and Wistar Kyoto rats (WKY). Jpn. Heart J., 26 (4), 696 (1985). 82 Kazuwa Nakao, Makoto Sakamoto, Narito Morii, Akira Sugawara, Mitsuaki Suda, Masanori Shimokura, Yoshiaki Kiso, Masahiro Kihara, Yukio Yamori, Hiroo Imura, Atrial natriuretic polypeptides in rat heart and plasma. Jpn. Heart J., 26 (4), 697 (1985). 83 Makoto Sakamoto, Kazuwa Nakao, Akira Sugawara, Narito Morii, Mitsuaki Suda, Masanori Shimokura, Yoshiaki Kiso, Masahiro Kihara, Yukio Yamori, Hiroo Imura, Effects of DOCA and salt overloading on the content of a-rat atrial natriuretic polypeptide-like immunoreactivity in rat atrium. Jpn. Heart J., 26 (4), 698 (1985). 84 Yoshiro Sogawa, Masahiro Kihara, Masayuki Mano, Kazuwa Nakao, Akira Sugawara, Mitsuaki Suda, Makoto Sakamoto, Narito Morii, Masanori Shimokura, Yoshiaki Kiso, Hiroo Imura, Yukio Yamori, Effect of a-rat atrial natriuretic polypeptide on blood pressure in rats bilateral renal vessels ligated. Jpn. Heart J., 26 (4), 699 (1985). 85 Kazuko Mori, Masahiro Kihara, Kazuwa Nakao, Akira Sugawara, Mitsuaki Suda, Makoto Sakamoto, Narito Morii, Masanori Shimokura, Yoshiaki Kiso, Masayuki Mano, Hiroo Imura, Yukio Yamori, Effect of a-human atrial natriuretic polypeptide (a-hANP) on canine renal Na+-K+ ATPase activity. Jpn. Heart J., 26 (4), 700 (1985). 86 Mitsuhiro Kawata, Shuichi Ueda, Kazuwa Nakao, Narito Morii, Yoshiaki Kiso, Hiroo Imura, Yutaka Sano, Immunohistochemical demonstration of a-atrial natriuretic polypeptide-containing neurons in the rat brain. Histochemistry, 83 (11), 1-3 (1985). 87 Yuta Kobayashi, Masahiro Kihara, Kazuwa Nakao, Masanori Shimokura, Yoshiaki Kiso, Hiroo Imura, Yukio Yamori, Keisuke Hattori, Vasodilatory effects of atrial natriuretic polypeptide on rat. Jpn. J. Pharmacol., 39, 99P (1985). 88 Midori Kajiwara, Kaori Ishii, Yoshiaki Kiso, Kouki Kitagawa, Tetsuo Oka, The choice by dynorphin-related octapeptides of opioid-receptor subtype in isolated preparations. Jpn. J. Pharmacol., 39, 245P (1985). 89 Yoshiaki Kiso, Efficient deprotection by a “push-pull” mechanism and syntheses of biologically active peptides. Proc. Akabori Conf., German-Jpn. Symp. Peptide Chemistry, 24-27 (1985). 90 Ken-ichi Inui, Hideyuki Saito, Yasuhisa Matsukawa, Kazuwa Nakao, Narito Morii, Hiroo Imura, Masanori Shimokura, Yoshiaki Kiso, Ryohei Hori, Specific binding activities and cyclic GMP responses by atrial natriuretic polypeptide in kidney epithelial cell line (LLC-PK1). Biochem. Biophys. Res. Commun., 132 (1), 253-260 (1985). 91 Mitsuhiro Kawata, Kazuwa Nakao, Narito Morii, Yoshiaki Kiso, Hiroshi Yamashita, Hiroo Imura, Yutaka Sano, Atrial natriuretic polypeptide: Topographical distribution in the rat brain by radioimmunoassay and immunohistochemistry. Neuroscience, 16 (3), 521-546 (1985). 92 Yoshiaki Kiso, Masanori Shimokura, Satoshi Hosoi, Toshio Fujisaki, Yoichi Fujiwara, Makoto Yoshida, Syntheses and properties of peptides related to atrial natriuretic hormone. Peptides: Str. Funct., Proc. 9th Amer. Peptide Symp., 949-952 (1985). 93 菅原照, 中尾一和, 森井成人, 坂本誠, 山田敬行, 伊藤裕, 塩野尚三, 西村和修, 木原正博, 霜倉正徳, 木曽良明, 伴敏彦, 家森幸男, 井村裕夫. ヒト血中の心房性ナトリウム利尿ホルモン--容量調節系における生理的, 病態生理的意義について. 高血圧, 8 (1), 24 (1985). Akira Sugawara, Kazuwa Nakao, Narito Morii, Makoto Sakamoto, Takayuki Yamada, Yutaka, Ito, Shozo Shiono, Kazunobu Nishimura, Masahiro Kihara, Masanori Shimokura, Yoshiaki Kiso, Toshihiko Ban, Yukio Yamori, Hiroo Imura. Physiological and pathophysiological significance in volume regulatory system of atrial natriuretic hormone in human plasma. Koketsuatsu, 8 (1), 24 (1985). 94 木曽良明, peptide合成の本. ファルマシア, 21 (3), 218-219 (1985). Yoshiaki Kiso. Books of peptide synthesis. Farumashia, 21 (3), 218-219 (1985). 95 木曽良明, オピオイドペプチドの構造と作用. 病態生理, 4 (3), 180-186 (1985). Yoshiaki Kiso. Structure and activity of opioid peptides. Byotai Seiri, 4 (3), 180-186 (1985). 96 木曽良明, 心房性ナトリウム利尿ホルモン及び関連ペプチドの合成研究. ホルモンと臨床,33 (4), 326-330 (1985). Yoshiaki Kiso. Synthetic study of atrial natriuretic hormone and related peptides. Horumon to Rinsho, 33 (4), 326-330 (1985). 97 中尾一和, 菅原照, 森井成人, 坂本誠, 須田光明, 木原正博, 家森幸男, 霜倉正徳, 木曽良明, 西村和修, 曽根田純一, 伴敏彦, 河田光博, 佐野豊, 井村裕夫, 心房性ナトリウム利尿ポリペプチド(ANP)のラジオイムノアッセイ. ホルモンと臨床, 33 (4), 365-370 (1985). Kazuwa Nakao, Akira Sugawara, Narito Morii, Makoto Sakamoto, Mitsuaki Suda, Masahiro Kihara, Yukio Yamori, Masanori Shimokura, Yoshiaki Kiso, Kazunobu Nishimura, Junichi Soneda, Toshihiko Ban, Mitsuhiro Kawata, Yutaka Sano, Hiroo Imura. Radioimmunoassay of atrial natriuretic polypeptide (ANP). Horumon to Rinsho, 33 (4), 365-370 (1985). 98 Kazuwa Nakao, Akira Sugawara, Narito Morii, Makoto Sakamoto, Takayuki Yamada, Hiroshi Ito, Shozo Shiono, Kazunobu Nishimura, Toshihiko Ban, Masahiro Kihara, Yukio Yamori, Masanori Shimokura, Yoshiaki Kiso, Kenji Kangawa, Hisayuki Matsuo, Hiroo Imura, Pharmacokinetic study on a-human atrial natriuretic polypeptide in man. Peptide Chemistry 1985, 23-26 (1986). 99 Yoshiaki Kiso, Masanori Shimokura, Makoto Yoshida, Yoichi Fujiwara, Satoshi Hosoi, Toshio Fujisaki, Todd W. Rockway, Peter J. Connolly, William H. Holleman, Eugene N. Bush, Thomas J. Perun, Syntheses and activities of atrial natriuretic polypeptide (ANP) analogs. Peptide Chemistry 1985, 33-38 (1986). 100 Yoshiaki Kiso, Masanori Shimokura, Takatomo Narukami, Akihiro Nakamura, Hirohito Shiomi, Properties of Nin-(2,4,6-triisopropylphenylsulfonyl)tryptophan and its application to the synthesis of delta-sleep inducing peptide. Peptide Chemistry 1985, 131-136 (1986). 101 Yoshiaki Kiso, Toshio Fujisaki, Masanori Shimokura, Deprotection procedure using methyltrichlorosilane: Synthesis of an opioid peptide, amidorphin. Peptide Chemistry 1985, 137-142 (1986). 102 Makoto Sakamoto, Kazuwa Nakao, Akira Sugawara, Narito Morii, Yoshihiko Saito, Hiroshi Itoh, Takayuki Yamada, Shozo Shiono, Masanori Shimokura, Yoshiaki Kiso, Masahiro Kihara, Yukio Yamori, Hiroo Imura, Effects of DOCA and salt loading on atrial and plasma levels of atrial natriuretic polypeptide. Peptide Chemistry 1985, 373-378 (1986). 103 Akira Sugawara, Kazuwa Nakao, Makoto Sakamoto, Narito Morii, Takayuki Yamada, Hiroshi Itoh, Shozo Shiono, Kazunobu Nishimura, Toshihiko Ban, Masahiro Kihara, Yukio Yamori, Masanori Shimokura, Yoshiaki Kiso, Hiroo Imura, Plasma concentration of atrial natriuretic polypeptide in human disorders. Peptide Chemistry 1985, 379-384 (1986). 104 L. D. Artman, E. N. Bush, V. Sarin, T. W. Rockway, P. J. Connolly, Y. Kiso, W. H. Holleman, Characterization of natriuretic diuretic and hypotensive effects of atrial natriuretic hormone analogues in the anesthetized rat. Fed. Proc., 45 (3), 198 (1986). 105 E. N. Bush, E. M. Green, L. D. Artman, E. M. Devine, V. Sarin, T. W. Rockway, P. J. Connolly, Y. Kiso, W. H. Holleman. Vasorelaxant potencies and receptor binding affinities of atrial natriuretic hormone (ANH) analogues. Fed. Proc., 45 (3), 657 (1986). 106 Masanori Shimokura, Yoshiaki Kiso, Akihiko Nagata, Masabumi Tsuda, Hitoshi Seki, Yoshiyuki Kai, Nobutaka Fujii, Haruaki Yajima, Studies on peptides. CXXXVII. Conventional solution synthesis of porcine hypothalamic growth hormone releasing factor (pGRF). Chem. Pharm. Bull., 34 (4), 1814-1820 (1986). 107 Narito Morii, Kazuwa Nakao, Masahiro Kihara, Makoto Sakamoto, Akira Sugawara, Masanori Shimokura, Yoshiaki Kiso, Yukio Yamori, Hiroo Imura, Effects of water deprivation and sodium load on atrial natriuretic polypeptide in rat brain. Hypertension, 8 (4, part 2), 61-65 (1986). 108 Akira Sugawara, Kazuwa Nakao, Narito Morii, Makoto Sakamoto, K. Horii, M. Shimokura, Y. Kiso, K. Nishimura, T. Ban, M. Kihara, Y. Yamori, K. Kangawa, H. Matsuo, H. Imura: Significance of a-human atrial natriuretic polypeptide as a hormone in humans. Hypertension, 8 (4, part 2), 151-155 (1986). 109 Masanori Shimokura, Yoshiaki Kiso, Akihiko Nagata, Masabumi Tsuda, Hitoshi Seki, Yoshiyuki Kai, Nobutaka Fujii, Haruaki Yajima, Studies on peptides. CXXXVIII. Conventional solution synthesis of bovine hypothalamic growth hormone releasing factor (pGRF). Chem. Pharm. Bull., 34 (5), 2218-2223 (1986). 110 木曽良明, 心房性ナトリウム利尿ホルモン関連ペプチドの合成. 日本腎臓学会雑誌, 28 (7), 915-916 (1986). Yoshiaki Kiso. Synthesis of atrial natriuretic hormone related peptides. Nippon Jinzo Gakkai Zasshi, 28 (7), 915-916 (1986). 111 Y. Kobayashi, M. Kihara, K. Nakao, M. Shimokura, Y. Kiso, H. Imura, Y. Yamori, K. Hattori, Effects of atrial natriuretic polypeptide on vascular strips of spontaneously hypertensive rats and Wister-Kyoto rats. J. Hypertension, 4 (suppl. 3), S335-338 (1986). 112 N. Yonehara, J. Nakamae, T. Kudo, Y. Kiso, R. Inoki, Anti-inflammatory effects of opiates and opioid peptides on the dextran-induced edema in the rat hind paw. Asia Pacific J. Pharmacol., 1, 69-72 (1986). 113 Yoshiaki Kiso, Masanori Shimokura, Yoichi Fujiwara, Makoto Yoshida, Akiko Nishitani, Tooru Kimura, Toshio Fujisaki, Todd W. Rockway, William H. Holleman, Eugene N. Bush, Thomas J. Perun, Syntheses and biological activities of atrial natriuretic peptide (ANP) analogs. Peptide Chemistry 1986, 57-62 (1987). 114 Yoshiaki Kiso, Makoto Yoshida, Toshio Fujisaki, Tsutomu Mimoto, Tooru Kimura, Masanori Shimokura, Deprotecting methods by the use of silyl compounds in peptide synthesis. Peptide Chemistry 1986, 205-210 (1987). 115 Yoshiaki Kiso, Masanori Shimokura, Tooru Kimura, Tsutomu Mimoto, Makoto Yoshida, Toshio Fujisaki, ß-Carboxyl protecting groups of aspartic acid and synthesis of a novel tachykinin peptide, scyliorhinin I. Peptide Chemistry 1986, 211-216 (1987). 116 Yoshiaki Kiso, Masanori Shimokura, Takatomo Narukami, Akihiro Nakamura, Hirohito Shiomi, Synthesis and analgesic activities of delta-sleep inducing peptide (DSIP) derivatives. Peptide Chemistry 1986, 299-304 (1987). 117 Yoshiaki Kiso, Masanori Shimokura, Satoshi Hosoi, Toshio Fujisaki, Yoichi Fujiwara, Makoto Yoshida, Syntheses and biological activities of atrial natriuretic polypeptide analogs. J. Protein Chem., 6 (2), 147-162 (1987). 118 Yoshiaki Kiso, Masanori Shimokura, Yoichi Fujiwara, Makoto Yoshida, Akiko Nishitani, Tooru Kimura, Toshio Fujisaki, Todd W. Rockway, William H. Holleman, Eugene N. Bush, Thomas J. Perun, Syntheses and structure-activity relationships of atrial natriuretic peptide (ANP) derivatives. J. Pharmacobio-Dyn., 10 (6), s-151 (1987). 119 Tsuyoshi Kono, Yoshiaki Kiso, Mahesh C. Khosla, Naoki Sakura, Tyrosine in position 4 is the key amino acid for the binding of angiotensin II to human arteriolar receptor. Endocrinol. Jpn., 34 (5), 737-743 (1987). 120 Yoshiaki Kiso, Takatomo Narukami, Tsutomu Mimoto, Hideo Nakamura, Atsuko Kita, Synthesis and opioid activity of dermorphin-related peptides. J. Pharm. Sci., 76 (11), S160 (1987). 121 Y. Kiso, M. Shimokura, Y. Fujiwara, M. Yoshida, A. Nishitani, T. Kimura, T. Mimoto, T. W. Rockway, W. H. Holleman, E. N. Bush, T. J. Perun, Syntheses and biological activities of atrial natriuretic peptide (ANP) derivatives. J. Pharm. Sci., 76 (11), S172 (1987). 122 Yoshiaki Kiso, Makoto Yoshida, Tooru Kimura, Tsutomu Mimoto, Masanori Shimokura, Syntheses of scyliorhinin peptides using tetrachlorosilane-trifluoroacetic acid-scavengers by a reductive acidolysis mechanism. J. Pharm. Sci., 76 (11), S252 (1987). 123 Yoshiaki Kiso, Makoto Yoshida, Tooru Kimura, Tsutomu Mimoto, Masanori Shimokura, Toshio Fujisaki, A deprotection method using tetrachlorosilane-trifluoroacetic acid-scavengers by a “reductive acidolysis” mechanism: application to the synthesis of a novel tachykinin peptide, scyliorhinin I. PEPTIDES: Chem. Biol., Proc. Tenth Amer. Peptide Symp., 229-231 (1988). 124 Yoshiaki Kiso, Masanori Shimokura, Takatomo Narukami, Tooru Kimura, Protection of the tryptophan indole ring with the diphenylphosphinothioyl (Ppt) group in peptide synthesis. Peptide Chemistry 1987, 219-222 (1988). 125 Yoshiaki Kiso, Akiko Nishitani, Masanori Shimokura, Yoichi Fujiwara, Tooru Kimura, Use of dilute methanesulfonic acid for removal of N-a-amino protecting groups during solid phase peptide synthesis. Peptide Chemistry 1987, 291-294 (1988). 126 Yoshiaki Kiso, Tsutomu Mimoto, Tooru Kimura, Makoto Yoshida, Masanori Shimokura, Synthesis and activities of scyliorhinin peptides. Peptide Chemistry 1987, 347-350 (1988). 127 Yoshiaki Kiso, Masanori Shimokura, Makoto Yoshida, Yoichi Fujiwara, Tooru Kimura, Akiko Nishitani, Tsutomu Mimoto, Todd W. Rockway, William H. Holleman, Eugene N. Bush, Thomas J. Perun, Synthesis of atrial natriuretic peptide (ANP) fragments with hypertensive action. Peptide Chemistry 1987, 513-516 (1988). 128 Yoshiaki Kiso, Tooru Kimura, Masanori Shimokura, Takatomo Narukami, Nin-Diphenylphosphinothioyltryptophan, a useful derivative for peptide synthesis by the methanesulphonic acid-thioanisole system and fluoride ion deprotection methods. J. Chem. Soc., Chem. Commun., (4), 287-289, (1988). 129 Kinji Iizuka, Tetsuhide Kamijo, Tetsuhiro Kubota, Kenji Akahane, Hideaki Umeyama, Yoshiaki Kiso, New human renin inhibitors containing an unnatural amino acid norstatine. J. Med. Chem., 31 (4), 701-704 (1988). 130 Kinji Iizuka, Tetsuhide Kamijo, Hiromu Harada, Kenji Akahane, Tetsuhiro Kubota, Iwao Shimaoka, Hideaki Umeyama, Yoshiaki Kiso, New human renin inhibitory peptides: angiotensinogen transition-state analogues containing novel Leu-Val replacement and a retro-inverso amide bond. Chem. Pharm. Bull., 36 (6), 2278-2281 (1988). 131 Kenji Akahane, Tetsuhide Kamijo, Kinji Iizuka, Takeo Taguchi, Yoshiro Kobayashi, Yoshiaki Kiso, Hideaki Umeyama. Structure-activity relationship of fluorine-containing renin inhibitory peptides based upon the tertiary structure of human renin. Chem. Pharm. Bull., 36 (9), 3447-3452 (1988). 132 木曽良明, オピオイド ペプチドの合成及びその構造活性相関研究. 薬学研究の進歩. 研究成果報告集4, 79-93 (1988). Yoshiaki Kiso. Synthesis and structure-activity relationship study on opioid peptides. Yakugaku Kenkyuu no Shinpo. 4, 79-93 (1988). 133 Yoshiaki Kiso, Makoto Yoshida, Tooru Kimura, Masanori Shimokura, Tsutomu Mimoto, A “reductive acidolytic” deprotection method in peptide synthesis. Proc. 2nd Akabori Conf., Jpn. Ger. Symp. Peptide Chem., 11-16 (1988) 134 Yoshiaki Kiso, Tooru Kimura, Yoichi Fujiwara, Masanori Shimokura, Akiko Nishitani, A fluoride ion deprotection strategy in peptide synthesis. Combination with selective deprotection using the dilute methanesulfonic acid of a-amino protecting groups. Chem. Pharm. Bull., 36 (12), 5024-5027(1988). 135 Muneaki Hashimoto, Kanji Takada, Yoshiaki Kiso, Shozo Muranishi, Synthesis of palmitoyl derivatives of insulin and their biological activities. Pharmaceut. Res. 6 (2) 171-176 (1989) 136 Kinji Iizuka, Tetsuhide Kamijo, Hiromu Harada, Kenji Akahane, Tetsuhiro Kubota, Hideaki Umeyama, Yoshiaki Kiso, Renin inhibitors designed on the basis of angiotensinogen transition-state. J Pharmacobio-Dyn, 12 (6), s-132 (1989). 137 Yoshiaki Kiso, Yoichi Fujiwara, Tooru Kimura, Makoto Yoshida, A new method for solid phase peptide synthesis by a-amino deprotecting procedure using methanesulfonic acid. Peptide Chemistry 1988, 123-128 (1989) 138 Yoshiaki Kiso, Yoichi Fujiwara, Tooru Kimura, Masanori Shimokura, Akiko Nishitani, A fluoride ion final deprotection method in peptide synthesis. Peptide Chemistry 1988, 129-134 (1989) 139 Yoshiaki Kiso, Makoto Yoshida, Yoichi Fujiwara, Tooru Kimura, Masanori Shimokura, Synthesis of a porcine brain natriuretic peptide using a new thiol protecting group. Peptide Chemistry 1988, 201-206 (1989). 140 Yoshiaki Kiso, Makoto Yoshida, Tooru Kimura, Yoichi Fujiwara, Masanori Shimokura, A new thiol protecting trimethylacetamidomethyl group. Synthesis of a new porcine brain natriuretic peptide using the S-trimethylacetamidomethyl-cysteine. Tetrahedron Letters, 30 (15), 1979-1982 (1989). 141 T. Nakazawa, M. Ikeda, T. Kaneko, K. Yamatsu, K. Kitagawa, Y. Kiso, Bestatin potentiates the antinociception but not the motor dysfunction induced by intracerebrally administered dynorphin-B in mice. Neuropeptides, 13 (4), 277-283 (1989). 142 Yoshiaki Kiso, Makoto Yoshida, Tooru Kimura, Masanori Shimokura, Tsutomu Mimoto, Deprotection procedures in peptide synthesis. A “reductive acidolytic” deprotection method and fluoride ion deprotection method. Peptides 1988, Proc. 20th Eur Peptide Symp., 55-57 (1989). 143 Yoshiaki Kiso, Tooru Kimura, Makoto Yoshida, Masanori Shimokura, Kenichi Akaji, Tsutomu Mimoto, A new class of amino protecting group removable by reductive acidolysis: 4-methylsulphinyl-benzyloxycarbonyl (Msz) group. J. Chem. Soc., Chem. Commun., (20) 1511-1513 (1989). 144 Hiromu Harada, Atsushi, Tsubaki, Tetsuhide Kamijo, Kinji Iizuka, Yoshiaki Kiso, A simple diastereoselective synthesis of cyclohexylnorstatine and allocyclohexylnorstatine. Chem. Pharm. Bull., 37 (9), 2570-2572 (1989) 145 Kinji Iizuka, Tetsuhide Kamijo, Hiromu Harada, Kenji Akahane, Tetsuhiro Kubota, Hideaki Umeyama, Yoshiaki Kiso, Design and synthesis of an orally potent human renin inhibitor containing a novel amino acid, cyclohexylnorstatine. J. Chem. Soc. Chem. Commun., (21) 1678-1680 (1989) 146 Kouki Kitagawa, Tatsuhiko Kawamoto, Shiroh Futaki, Shinya Kiyama, Tadashi Akita, Hideki Moritoki, Yoshiaki Kiso, Solution syntheses of two enkephalin-containing peptides, peptide E and dynorphin (1-24), using Nin-(2,4,6-triisopropylphenylsulfonyl)tryptophan. Chem. Pharm. Bull., 37 (10), 2631-2638 (1989). 147 Yoshiaki Kiso, Makoto Yoshida, Tadashi Tatsumi, Tooru Kimura, Yoichi Fujiwara, Kenichi Akaji, Tetrafluoroboric acid, a useful deprotecting reagent in peptide synthesis. Chem. Pharm. Bull., 37 (12) 3432-3434 (1989). 148 Yoshiaki Kiso, Tooru Kimura, Yoichi Fujiwara, Hiroshi Sakikawa, Kenichi Akaji, An efficient peptide synthesis on a phenacyl-resin by methanesulfonic acid deprotecting procedure. Proc. 3rd Akabori Conf., Ger.-Jpn. Symp. Peptide Chem., 25-29 (1989). 149 木曽良明, アミノ酸及びペプチド. 生体分子の化学40-58 (1989広川書店) Yoshiaki Kiso. Amino acids and peptides. Seitai Bunshi no Kagaku. 40-58 (1989 Hirokawa Shoten) 150 G. P. Budzik, Y. Kiso, T. P. Dillon, W. H. Holleman. Identification of a potent peptide antagonist of atriopeptin-III (AP-III) stimulation of cGMP synthesis. Am. J. Hypertension, 2 (5-2), 49A (1989). 151 Yoshiaki Kiso, Tooru Kimura, Yoichi Fujiwara, Hiroshi Sakikawa, Kenichi Akaji, Efficient solid phase peptide synthesis on a phenacyl-resin by a methanesulfonic acid a-amino deprotecting procedure. Chem. Pharm. Bull. 38 (1), 270-272 (1990). 152 Makoto Yoshida, Kenichi Akaji, Tadashi Tatsumi, Satoshi Iinuma, Yoichi Fujiwara, Tooru Kimura, Yoshiaki Kiso, Synthesis of porcine brain natriuretic peptide-32 using silver tetrafluoroborate as a new deprotecting reagent of the S-trimethylacetamidomethyl group. Chem. Pharm. Bull., 38 (1) 273-275 (1990). 153 Makoto Yoshida, Masanori Shimokura, Yoichi Fujiwara, Toshio Fujisaki, Kenichi Akaji, Yoshiaki Kiso, Solution-phase synthesis of a-human atrial natriuretic peptide (a-hANP). Chem. Pharm. Bull., 38 (2), 382-388 (1990). 154 Kenichi Akaji, Makoto Yoshida, Tadashi Tatsumi, Tooru Kimura, Yoichi Fujiwara, Yoshiaki Kiso, Tetrafluoroboric acid as a useful deprotecting reagent in Fmoc-based solid-phase peptide syntheses. J. Chem. Soc., Chem. Commun., (4), 288-290 (1990). 155 Hiromu Harada, Toshiaki Yamaguchi, Akira Iyobe, Atsushi Tsubaki, Tetsuhide Kamijo, Kinji Iizuka, Katsuyuki Ogura, Yoshiaki Kiso, A practical synthesis of (2R)-3-morpholinocarbonyl-2-(1-naphthylmethyl)propionyl-L-histidine moiety (P4-P2) in renin inhibitors. J. Org. Chem., 55 (5), 1679-1682(1990). 156 Yoshiaki Kiso, Makoto Yoshida, Yoichi Fujiwara, Tooru Kimura, Masanori Shimokura, Kenichi Akaji, Trimethylacetamidomethyl (Tacm) group, a new protecting group for the thiol function of cysteine. Chem. Pharm. Bull., 38 (3), 673-675 (1990). 157 Makoto Yoshida, Kenichi Akaji, Tadashi Tatsumi, Yoichi Fujiwara, Tooru Kimura, Yoshiaki Kiso, Deprotection of S-trimethylacetamidomethyl group using silver tetrafluoroborate. Peptide Chemistry 1989, 33-38 (1990) 158 Yoshiaki Kiso, Hiroshi Sakikawa, Yoichi Fujiwara, Tooru Kimura, Kenichi Akaji, A fluoride ion final deprotection method in solid phase peptide synthesis. Peptide Chemistry 1989, 153-158 (1990). 159 Yoshiaki Kiso, Yoichi Fujiwara, Tooru Kimura, Hisatomi Itoh, Kenichi Akaji, “Reductive acidolysis” deprotection in solid phase peptide synthesis. Peptide Chemistry 1989, 159-164 (1990). 160 Kenichi Akaji, Makoto Yoshida, Tadashi Tatsumi, Tooru Kimura, Yoichi Fujiwara, Satoshi Iinuma, Yoshiaki Kiso, Tetrafluoroboric acid as a final deprotecting reagent in Fmoc-based solid-phase peptide synthesis. Peptide Chemistry 1989, 165-170 (1990). 161 T. W. Rockway, P. J. Connolly, E. M. Devine Jr., G. P. Budzik, A. M. Thomas, Y. Kiso, W. H. Holleman. Structure-activity relationships of atrial natriuretic factor (ANF) receptor agonists. Peptides: Chem. Str. Biol.: Proc. 11th Am. Peptide Symp., 244-246 (1990). 162 Yoshiaki Kiso, Yoichi Fujiwara, Tooru Kimura, Makoto Yoshida, Kenichi Akaji. Efficient solid-phase peptide synthesis using an a-amino deprotecting procedure with methanesulfonic acid. Peptides: Chem. Str. Biol.: Proc. 11th Am. Peptide Symp., 931-932 (1990). 163 Makoto Yoshida, Masanori Shimokura, Yoichi Fujiwara, Toshio Fujisaki, Kenichi Akaji, Yoshiaki Kiso. Solution-phase synthesis of a-rat atrial natriuretic peptide (a-rANP). Chem. Pharm. Bull. 38 (4), 1072-1074 (1990). 164 Yoshiaki Kiso, Makoto Yoshida, Tooru Kimura, Yoichi Fujiwara, Masanori Shimokura, Kenichi Akaji. Solution-phase synthesis of porcine brain natriuretic peptide (pBNP) using the S-trimethylacetamidomethyl-cysteine. Chem. Pharm. Bull., 38 (5) 1192-1199 (1990). 165 Kenichi Akaji, Yoshiaki Kiso, Louis A. Carpino. Fmoc-based solid-phase peptide synthesis using a new t-alcohol type 4-(1’,1’-dimethyl-1’-hydroxypropyl)phenoxyacetyl handle (DHPP)-resin (Fmoc = fluoren-9-ylmethoxycarbonyl). J. Chem. Soc., Chem. Commun., (7), 584-586 (1990). 166 木曽良明, 神経ペプチドをめぐる新薬開発の動向と問題点. 日本臨床48 (5), 1066-1070 (1990). Yoshiaki Kiso. Trends and problems in the development of neuropeptide drugs. Nippon Rinsho, 48 (5), 1066-1070 (1990). 167 Makoto Yoshida, Tadashi Tatsumi, Yoichi Fujiwara, Satoshi Iinuma, Tooru Kimura, Kenichi Akaji, Yoshiaki Kiso. Deprotection of the S-trimethylacetamidomethyl (Tacm) group using silver tetrafluoroborate: application to the synthesis of porcine brain natriuretic peptide-32 (pBNP-32). Chem. Pharm. Bull. 38 (6), 1551-1557 (1990). 168 Hiroshi Katsuki, Satoru Nakai, Yoshikatsu Hirai, Ken-ichi Akaji, Yoshiaki Kiso, Masamichi Satoh, Interleukin-1b inhibits long-term potentiation in the CA3 region of mouse hippocampal slices. Eur J Pharmacol., 181 (3) 323-326 (1990). 169 木曽良明．ペプチド誘導体の分子設計．医薬品の開発第7巻分子設計第４章93-135. 1990.6(広川書店)． Yoshiaki Kiso. Molecular design of peptide derivatives. Iyakuhin no Kaihatsu, Vol.7 Chap.4, pp93-135 (1990 Hirokawa Shoten). 170 Yoshiaki Kiso, Yoichi Fujiwara, Makoto Yoshida, Masanori Shimokura, Kenichi Akaji, William H. Holleman, Thomas J Perun, Todd W. Rockway, Syntheses and structure-activity relationships of small-sized atrial natriuretic peptide (ANP) derivatives. J. Pharmacobio-Dyn., 13 (8), s-140 (1990). 171 Kinji Iizuka, Tetsuhide Kamijo, Hiromu Harada, Kenji Akahane, Tetsuhiro Kubota, Yasui Etoh, Iwao Shimaoka, Atsushi Tsubaki, Makoto Murakami, Toshiaki Yamaguchi, Akira Iyobe, Hideaki Umeyama, Yoshiaki Kiso, Synthesis and structure-activity relationships of human renin inhibitors designed from angiotensinogen transition state. Chem. Pharm. Bull., 38 (9), 2487-2493 (1990). 172 Kinji Iizuka, Tetsuhide Kamijo, Hiromu Harada, Kenji Akahane, Tetsuhiro Kubota, Hideaki Umeyama, Toshimasa Ishida, Yoshiaki Kiso. Orally potent human renin inhibitors derived from angiotensinogen transition state: design, synthesis, and mode of interaction. J. Med. Chem., 33 (10), 2707-2714 (1990). 173 Hiromu Harada, Akira Iyobe, Atsushi Tsubaki, Toshiaki Yamaguchi, Kazuma Hirata, Tetsuhide Kamijo, Kinji Iizuka, Yoshiaki Kiso. A practical synthesis of an orally potent renin inhibitor, isopropyl (2R,3S)-4-cyclohexyl-2-hydroxy-3-{N-[(2R)-2-morpholinocarbonylmethyl-3-(1-naphthyl)propionyl]-L-histidyl} aminobutyrate. J. Chem. Soc., Perkin Trans. I, (9), 2497-2500 (1990). 174 木曽良明. メディシナルケミストリー−創薬のための有機化学. 1990.10 (広川書店). Yoshiaki Kiso, Medicinal Chemistry -Role of Organic Chemistry. (1990 Hirokawa Shoten). Translation work. 175 Hiromu Harada, Kinji Iizuka, Tetsuhide Kamijo, Kenji Akahane, Ryoji Yamamoto, Yasushi Nakano, Atsushi Tsubaki, Tetsuhiro Kubota, Iwao Shimaoka, Hideaki Umeyama, Yoshiaki Kiso. Synthesis of human renin inhibitory peptides, angiotensinogen transition-state analogs containing a retro-inverso amide bond. Chem. Pharm. Bull., 38 (11), 3042-3047 (1990). 176 木曽良明, 木村徹．ペプチド縮合剤 ｢BOP｣．有機合成化学協会誌48 (11),1032-1033 (1990). Yoshiaki Kiso, Toru Kimura, Peptide Coupling Reagent “BOP”. J. Syn. Org. Chem. Jpn., 48 (11),1032-1033 (1990). 177 木曽良明, 木村徹. 脱保護剤｢SiCl4-CF3COOH-Scavenger｣. 有機合成化学協会誌48 (11), 1046-1047 (1990). Yoshiaki Kiso, Toru Kimura, Deprotection reagent “SiCl4-CF3COOH-Scavenger”. J. Syn. Org. Chem. Jpn., 48 (11),1046-1047 (1990) 178 Kenichi Akaji, Hideo Tanaka, Hisatomi Ito, Junya Imai, Yoichi Fujiwara, Tooru Kimura, Yoshiaki Kiso. Fluoren-9-ylmethoxycarbonyl (Fmoc) amino acid chloride as an efficient reagent for anchoring Fmoc amino acid to 4-alkoxybenzyl alcohol resin. Chem. Pharm. Bull., 38 (12), 3471-3472 (1990). 179 Thomas W. von Geldern, Gerald P. Budzik, Terry P. Dillon, William H. Holleman, Mark A. Holst, Yoshiaki Kiso, Eugene I. Novosad, Terry J. Opgenorth, Todd W. Rockway, Alford M. Thomas, Sionhan Yeh. Atrial natriuretic peptide antagonists: Biological evaluation and structural correlations. Mol. Pharmacol., 38(6), 771-778 (1990). 180 Tooru Kimura, Shigeki Tanaka, Hisatomi Itoh, Yoichi Fujiwara, Kenichi Akaji, Yoshiaki Kiso. Solid phase peptide synthesis using reductive acidolysis deprotection. Peptide Chemistry 1990, 5-10 (1991). 181 Kenichi Akaji, Tadashi Tatsumi, Makoto Yoshida, Tooru Kimura, Yoichi Fujiwara, Yoshiaki Kiso. A new disulfide-bond forming reaction using silylchloride-sulfoxide system. Peptide Chemistry 1990, 11-14 (1991). 182 Kenichi Akaji, Hideo Tanaka, Hisatomi Itoh, Junya Imai, Yoichi Fujiwara, Tooru Kimura, Yoshiaki Kiso. An efficient method for anchoring Fmoc-amino acids to 4-alkoxybenzyl alcohol resin. Peptide Chemistry 1990, 67-70 (1991). 183 Yoichi Fujiwara, Tadashi Tatsumi, Junya Imai, Tooru Kimura, Makoto Yoshida, Kenichi Akaji, Yoshiaki Kiso. Syntheses of several newly isolated natriuretic peptides. Peptide Chemistry 1990, 89-94 (1991). 184 Kenichi Akaji, Tadashi Tatsumi, Makoto Yoshida, Tooru Kimura, Yoichi Fujiwara, Yoshiaki Kiso. Synthesis of cystine-peptide by a new disulphide bond-forming reaction using the silyl chloride-sulphoxide system. J. Chem. Soc., Chem. Commun., (3) 167-168 (1991). 185 Yoichi Fujiwara, Tadashi Tatsumi, Junya Imai, Yoshihito Nakagawa, Tooru Kimura, Kenichi Akaji, Yoshiaki Kiso, Synthesis and biological activities of several newly isolated natriuretic peptides. J. Pharmacobio-Dyn., 14 (5), s-105 (1991). 186 Yoshiaki Kiso, Kenichi Akaji, Makoto Yoshida, Tadashi Tatsumi, Yoichi Fujiwara, Tooru Kimura, Yoko Matsuda, A new deprotecting procedure in peptide synthesis. Peptides 1990, Proc. 21st Eur. Peptide Symp., Eds. E. Giralt & D. Andreu, ESCOM Sci. Publishers, 92-93 (1991). 187 Yoshiaki Kiso. New methods in peptide synthesis. Peptides: Biol. Chem., Proc. Chinese Peptide Symp., 1990, Ed. Y.-C.Du, Sci.Press., Beijing, China, 218-221 (1991). 188 木曽良明：続医薬品の開発．第14巻ペプチド合成．第4章アミノ酸側鎖官能基の保護基．75-99, 106-108 (1991.広川書店)5． Yoshiaki Kiso. Protecting groups for side chain functional groups of amino acids. Zoku Iyakuhinnno Kaihatsu. Vol. 14. Chap.4, pp75-99, pp106-108 (1991 Hirokawa Shoten). 189 木曽良明：続医薬品の開発．第14巻ペプチド合成．第5章酸アミド形成反応．135-204 (1991広川書店)5 Yoshiaki Kiso. Amide Forming Reactions. Zoku Iyakuhinnno Kaihatsu. Vol. 14. Chap.5, pp135-204 (1991 Hirokawa Shoten). 190 Mitsunobu Doi, Yasuko In, Masatoshi Inoue, Toshimasa Ishida, Kinji Iizuka, Kenji Akahane, Hiromu Harada, Hideaki Umeyama, Yoshiaki Kiso. Conformational study of a potent human renin inhibitor: X-ray crystal structure of isopropyl (2R, 3S)-4-cyclohexyl-2-hydroxy-3-{N-[(2R)-2-morpholinocarbonylmethyl-3-(1-naphthyl)propionyl]-L-histidylamino}butyrate (KRI-1314), a pentapeptide analogue with amino acid sequence corresponding to the cleavage site of angiotensinogen. J. Chem. Soc., Perkin Trans. 1, (5) 1153-1158 (1991). 191 Shozo Muranishi, Atsushi Sakai, Keigo Yamada, Masahiro Murakami, Kanji Takada, Yoshiaki Kiso. Lipophilic peptides: Synthesis of lauroyl thyrotropin-releasing hormone and its biological activity. Pharmac. Res., 8 (5), 649-652 (1991).5 192 Tsutomu Mimoto, Junya Imai, Shigeki Tanaka, Naoko Hattori, Osamu Takahashi, Sumitsugu Kisanuki, Yuichi Nagano, Makoto Shintani, Hideya Hayashi, Hiroshi Sakikawa, Kenichi Akaji, Yoshiaki Kiso, Rational design and synthesis of a novel class of active site-targeted HIV protease inhibitors containing a hydroxymethylcarbonyl isostere. Use of phenylnorstatine or allophenylnorstatine as a transition-state mimic. Chem. Pharm. Bull., 39 (9), 2465-2467 (1991). 193 木曽良明, 三本勤, エイズ治療薬をめざしたプロテアーゼインヒビターの開発. BIO INDUSTRY, 8 (10), 704-710 (1991). Yoshiaki Kiso, Tsutomu Mimoto, Development of protease inhibitors as AIDS therapeutics. BIO INDUSTRY, 8 (10), 704-710 (1991). 194 Yoshiaki Kiso, Satoshi Iinuma, Tsutomu Mimoto, Hideo Saji, Akira Yokoyama, Kenichi Akaji, A synthetic method suitable for the rapid preparation of 13N-labeled dermorphin analogue, H-Tyr-D-Met(O)-Phe-Gly-NH2 (SD-62). Chem. Pharm. Bull., 39 (10), 2734-2736 (1991). 195 木曽良明，経口ペプチド医薬品の吸収．日本医事新報，(3525), 138 (1991). Yoshiaki Kiso. Absorption of orally administered peptide drugs. Nippon Iji Shimpo. (3525), 138 (1991). 196 Tsutomu Mimoto, Junya Imai, Shigeki Tanaka, Naoko Hattori, Sumitsugu Kisanuki, Kenichi Akaji, Yoshiaki Kiso, KNI-102, a novel tripeptide HIV protease inhibitor containing allophenylnorstatine as a transition-state mimic. Chem. Pharm. Bull., 39 (11), 3088-3090 (1991). 197 Yoshiaki Kiso, Shigeki Tanaka, Tooru Kimura, Hisatomi Itoh, Kenichi Akaji, New hydroxyl protecting groups of a safety-catch type removable by reductive acidolysis. Chem. Pharm. Bull., 39 (11) 3097-3099 (1991). 198 木曽良明．ペプチド化学を基盤とした医薬品のデザイン−レセプターと酵素をターゲットとして．ファルマシア, 28(2), 151-155 (1992). Yoshiaki Kiso, Drug design based on peptide chemistry. Receptors and enzymes as targets. Farumashia, 28(2), 151-155 (1992). 199 Kenichi Akaji, Kenji Fujino, Tadashi Tatsumi, Yoshiaki Kiso, Regioselective double disulfide formation using silylchloride-sulfoxide system. Tetrahedron Letters, 33(8), 1073-1076 (1992). 200 Yoshiaki Kiso, Tooru Kimura, Hisatomi Itoh, Shigeki Tanaka, Kenichi Akaji, A new two-dimensional protection strategy for solid phase peptide synthesis: Use of a safety-catch type of ester linkage-resin cleavable by reductive acidolysis. Peptides: Chemistry and Biology., Proc. 12th Amer. Peptide Symp., Ed by J. A. Smith & J. E. Rivier, ESCOM, Leiden, The Netherlands (1992), p533-534. 201 Kenichi Akaji, Kenji Fujino, Tadashi Tatsumi, Tooru Kimura, Yoichi Fujiwara, Yoshiaki Kiso, A new method for the regioselective formation of disulfide-bonds using silylchloride-sulfoxide system. Peptide Chemistry 1991: A. Suzuki Ed., Protein Research Foundation, Osaka Japan (1992) p125-128. 202 Yoshiaki Kiso, Toshio Fukui, Shigeki Tanaka, Tooru Kimura, Kenichi Akaji, Solid phase peptide synthesis using a safety-catch protection strategy. Peptide Chemistry 1991: A. Suzuki Ed., Protein Research Foundation, Osaka Japan (1992) p187-192. 203 Kenichi Akaji, Naohiro Kuriyama, Tooru Kimura, Yoichi Fujiwara, Yoshiaki Kiso, Anchoring of Fmoc-amino acids to 4-alkoxybenzyl alcohol resin using new esterification reagents. Peptide Chemistry 1991: A. Suzuki Ed., Protein Research Foundation, Osaka Japan (1992) p193-196. 204 Tsutomu Mimoto, Junya Imai, Sumitsugu Kisanuki, Shigeki Tanaka, Naoko Hattori, Osamu Takahashi, Ryohei Katoh, Takuya Yumisaki, Hiroshi Sakikawa, Kenichi Akaji, Yoshiaki Kiso, Design and synthesis of HIV protease inhibitors containing a hydroxymethylcarbonyl isostere as a transition state mimic. Peptide Chemistry 1991: A. Suzuki Ed., Protein Research Foundation, Osaka Japan (1992) p395-400. 205 Kenichi Akaji, Naohiro Kuriyama, Tooru Kimura, Yoichi Fujiwara, Yoshiaki Kiso, Anchoring of Fmoc amino acid to 4-alkoxybenzyl alcohol resin using a new esterification reagent. Tetrahedron Letters, 33 (22), 3177-3180 (1992). 206 Kenichi Akaji, Tadashi Tatsumi, Makoto Yoshida, Tooru Kimura, Yoichi Fujiwara, Yoshiaki Kiso, Disulfide bond formation using the silyl chloride-sulfoxide system for the synthesis of a cystine peptide. J. Am. Chem. Soc., 114 (11), 4137-4143 (1992). 207 Yoshiaki Kiso, Yoichi Fujiwara, Tooru Kimura, Akiko Nishitani, Kenichi Akaji, Efficient solid phase peptide synthesis: use of methanesulfonic acid a-amino deprotecting procedure and new coupling reagent, 2-(benzotriazol-1-yl)oxy-1,3-dimethylimidazolidinium hexafluorophosphate (BOI). Int. J. Peptide & Protein Res., 40 (3/4), 308-314 (1992). 208 Yoshiaki Kiso. Design and synthesis of aspartic protease inhibitors. Proc. 4th Akabori. Conf., Jpn.-Ger. Symp. Peptide Chem.; N. Yanaihara., Ed., Protein Research Foundation, Osaka Japan (1992) p108-113. 209 Kenichi Akaji, Kenji Fujino, Tadashi Tatsumi, Tooru Kimura, Yoichi Fujiwara, Yoshiaki Kiso; Syntheses of cystine-peptides by a new disulphide bond forming reaction. J. Pharmacobio-Dyn., 15 (3), s-44 (1992). 210 Hideo Saji, Daisuke, Tsutsumi, Yoshiaki Kiso, Satoshi Iinuma, Tsutomu Mimoto, Kenichi Akaji, Yasuhiro Magata, Hideo Nakamura, Atsuko Kita, Junji Konishi, Akira Yokoyama; Synthesis and biological evaluation of a 13N-labeled opioid peptide. Nucl. Med. Biol., 19 (4), 455-460 (1992). 211 S. Muranishi, M. Murakami, M. Hashidzume, K. Yamada, S. Tajima, Y. Kiso, Trials of lipid modification of peptide hormones for intestinal delivery. J. Control. Release, 19 (1-3), 179-188 (1992). 212 木曽良明．論理的にデザインされた本格的抗エイズ薬への期待．エイズウイルス(HIV)プロテアーゼ阻害剤．モダンメディシン，21 (7) 51-52 (1992). Yoshiaki Kiso. Anticipation for rationally designed genuine anti-AIDS drugs. HIV protease inhibitors. Modern Medicine, 21 (7) 51-52 (1992). 213 Tsutomu Mimoto, Junya Imai, Sumitsugu Kisanuki, Hiroshi Enomoto, Naoko Hattori, Kenichi Akaji, Yoshiaki Kiso, Kynostatin (KNI)-227 and -272, highly potent anti-HIV agents: Conformationally constrained tripeptide inhibitors of HIV protease containing allophenylnorstatine. Chem. Pharm. Bull., 40(8), 2251-2253 (1992). 214 Yoichi Fujiwara, Tooru Kimura, Kenichi Akaji, Yoshiaki Kiso, W. H. Holleman, T. J. Perun, T. W. Rockway, T. W. von Geldern, Syntheses and structure-activities relationships of small-sized atrial natriuretic peptide (ANP) derivatives with potent activity. J. Pharmacobio-Dyn., 15 (7), s-86 (1992). 215 Tsutomu Mimoto, Junya Imai, Sumitsugu Kisanuki, Shigeki Tanaka, Naoko Hattori, Osamu Takahashi, Ryohei Katoh, Takuya Yumisaki, Hiroshi Sakikawa, Kenichi Akaji, Yoshiaki Kiso, Design of HIV protease inhibitors based on the Transition-state analogue concept. J. Pharmacobio-Dyn., 15 (7), s-91 (1992). 216 木曽良明．生理活性ペプチド．医薬化学．生物学への橋かけ．三木卓一，高木修造編集．155-159 (1992).4. Yoshiaki Kiso. Physiologically active peptides. Iyaku Kagaku, Ed by T. Miki and S. Takagi. pp155-159 (1992). 217 木曽良明．レセプターと薬物との相互作用．医薬化学．生物学への橋かけ．三木卓一，高木修造編集．225-234 (1992). Yoshiaki Kiso. Interaction of receptors with drugs. Iyaku Kagaku, Ed by T. Miki and S. Takagi. pp225-234 (1992). 218 木曽良明．エイズ治療薬の開発に挑む．化学47 (11), 726-732 (1992). Yoshiaki Kiso. Challenge to development of AIDS therapeutics. Kagaku, 47 (11), 726-732 (1992). 219 Takaaki Yoshimasa, Kazuwa Nakao, Shin-ichi Suga, Ichiro Kishimoto, Yoshiaki Kiso, Hiroo Imura, Identification and endothelin-induced activation of multiple extracellular signal-regulated kinases in aortic smooth muscle cells. FEBS Letters , 311 (3), 195-198 (1992). 220 木曽良明．AIDS. 化学と薬学の教室 (107), 33-36 (1992). Yoshiaki Kiso．AIDS. Kagaku to Yakugaku no Kyoushitsu, (107), 33-36 (1992). 221 林秀也，景山誠二，木曽良明，満屋裕明．AIDS治療薬としてのHIVプロテアーゼ阻害剤．実験医学，11(5), 661-667 (1993)． Hideya Hayashi, Seiji Kageyama, Yoshiaki Kiso, Hiroaki Mitsuya. HIV protease inhibitors as AIDS therapeutics. Jikken Igaku, 11(5), 661-667 (1993)． 222 Kenichi Akaji, Naohiro Kuriyama, Tooru Kimura, Yoichi Fujiwara, Yoshiaki Kiso. CIP and CIB: Two new reagents for the esterification or difficult coupling of sterically hindered amino acids. Peptides 1992, Proc. 23nd Eur. Peptide Symp. (ed. by Schneider, C. H. and Eberle, A. N.), p220-221, ESCOM Sci. Publishers B.V., Leiden, 1993. 223 Tsutomu Mimoto, Junya Imai, Sumitsugu Kisanuki, Naoko Hattori, Osamu Takahashi, Hiroshi Enomoto, Kenichi Akaji, Yoshiaki Kiso. Structure-activity relationships of HIV protease inhibitors containing hydroxymethylcarbonyl isostere as a transition state mimic. Peptides 1992, Proc. 23nd Eur. Peptide Symp. (ed. by Schneider, C. H. and Eberle, A. N.), p631-632, ESCOM Sci. Publishers B.V., Leiden, 1993. 224 Yoshiaki Kiso, Tsutomu Mimoto, Junya Imai, Sumitsugu Kisanuki, Naoko Hattori, Hiroshi Enomoto, Kenichi Akaji, Seiji Kageyama, Hiroaki Mitsuya. Design of HIV protease inhibitors with effective antiviral activity: Use of allophenylnorstatine as a transition-state mimic. Peptides 1992, Proc. 23nd Eur. Peptide Symp. (ed. by Schneider, C. H. and Eberle, A. N.), p805-807, ESCOM Sci. Publishers B.V., Leiden, 1993. 225 Kenichi Akaji, Kenji Fujino, Yoshiaki Kiso. Disulfide bond formation in peptides by silylchloride-sulfoxide: scope and applications. Peptide Chemistry 1992, Proc. 2nd Jpn. Symp. Peptide Chem. (ed. by N. Yanaihara), p27-29, ESCOM Sci. Publishers B.V., Leiden, 1993. 226 Kenichi Akaji, Kenji Fujino, Naohiro Kuriyama, Tooru Kimura, Yoshiaki Kiso. Two new reagents for the coupling of sterically hindered amino acids. Peptide Chemistry 1992, Proc. 2nd Jpn. Symp. Peptide Chem. (ed. by N. Yanaihara), p51-53, ESCOM Sci. Publishers B.V., Leiden, 1993. 227 Yoichi Fujiwara, Tooru Kimura, Kenichi Akaji, Yoshiaki Kiso, W. H. Holleman, T. W. Rockway, T. W. von Geldern. Syntheses and structure-activity relationships of natriuretic peptides. Peptide Chemistry 1992, Proc. 2nd Jpn. Symp. Peptide Chem. (ed. by N. Yanaihara), p434-436, ESCOM Sci. Publishers B.V., Leiden, 1993. 228 Sumitsugu Kisanuki, Tsutomu Mimoto, Junya Imai, Hiroshi Enomoto, Naoko Hattori, Osamu Takahashi, Ryohei Katoh, Shigeki Tanaka, Hiroshi Sakikawa, Tooru Kimura, Kenichi Akaji, Yoshiaki Kiso. Structure-activity relationships of HIV protease inhibitors containing allophenylnorstatine as a transition-state mimic. Peptide Chemistry 1992, Proc. 2nd Jpn. Symp. Peptide Chem. (ed. by N. Yanaihara), p439-441, ESCOM Sci. Publishers B.V., Leiden, 1993. 229 Tsutomu Mimoto, Sumitsugu Kisanuki, Junya Imai, Hiroshi Enomoto, Naoko Hattori, Seiji Kageyama, Hiroaki Mitsuya, Kenichi Akaji, Yoshiaki Kiso. Design and activity of protease active site-targeted anti-HIV agents containing allophenylnorstatine. Peptide Chemistry 1992, Proc. 2nd Jpn. Symp. Peptide Chem. (ed. by N. Yanaihara), p544-546, ESCOM Sci. Publishers B.V., Leiden, 1993. 230 Seiji Kageyama, Tsutomu Mimoto, Yohko Murakawa, Motoyoshi Nomizu, Harry Ford, Jr., Takuma Shirasaka, Sergei Gulnik, John Erickson, Kanji Takada, Hideya Hayashi, Samuel Broder, Yoshiaki Kiso, Hiroaki Mitsuya. In vitro anti-HIV activity of transition-state mimetic HIV protease inhibitors containing allophenylnorstatine. Antimicrob. Agent Chemother., 37 (4), 810-817 (1993). 231 A. Kiriyama, T. Mimoto, Y. Kiso, K. Takada, Pharmacokinetic study of a tripeptide HIV-1 protease inhibitor, KNI-174, in rats after intravenous and intraduodenal administrations. Biopharmaceut. Drug Disposition, 14 (3), 199-207 (1993). 232 木曽良明．キノスタチン(KNI)-272—論理的にデザインされたトリペプチドHIVプロテアーゼ阻害剤— 日本臨床51, 139-145 (1993). Yoshiaki Kiso. Kynostatine (KNI)-272. Rationally designed tripeptide HIV protease inhibitor. Nippon Rinsho, 51, 139-145 (1993). 233 木曽良明, 木佐貫純嗣．その他の抗HIV活性物質．日本臨床51, 235-240 (1993). Yoshiaki Kiso, Sumitsugu Kisanuki. Other anti-HIV compounds. Nippon Rinsho, 51, 139-145 (1993). 234 Kenichi Akaji, Yoshihito Nakagawa, Yoichi Fujiwara, Kenji Fujino, Yoshiaki Kiso, Synthesis of rat brain natriuretic peptide 45 using tetrafluoroboric acid deprotection and silyl chloride disulfide formation. Chem. Pharm. Bull., 41 (7), 1244-1248 (1993). 235 Kenichi Akaji, Kenji Fujino, Tadashi Tatsumi, Yoshiaki Kiso. Total synthesis of human insulin by regioselective disulfide formation using the silyl chloride-sulfoxide. J. Am. Chem. Soc. 115 (24), 11384-11392 (1993). 236 Yoshiaki Kiso, Hisatomi Itoh, Shigeki Tanaka, Tooru Kimura, Kenichi Akaji. A new stepwise deprotection method using reductive acidolysis followed by fluoride ion in solid phase peptide synthesis. Tetrahedron Letters, 34 (47) 7599-7602 (1993). 237 A. Kiriyama, T. Mimoto, S. Kisanuki, Y. Kiso, K. Takada, Comparison of a new orally potent tripeptide HIV-protease inhibitor (anti-AIDS drug) based on pharmacokinetic characteristics in rats after intravenous and intraduodenal administrations. Biopharmaceut. Drug Disposition, 14 (8), 697-707 (1993). 238 Yoshiaki Kiso. Design of HIV protease inhibitors based on the transition state concept. Peptides; Biology and Chemistry, Proc. 1992 Chinese Peptide Symp., Ed. by Y.-C. Du, J. P. Tam and Y.-S. Zhang, 87-92, ESCOM Sci. Publishers B.V., Leiden, 1993. 239 木曽良明．論理的にデザインされたHIVプロテアーゼ阻害剤．Mol. Med., 31 (1), 98-100 (1994). Yoshiaki Kiso. Rationally designed HIV protease inhibitors. Mol. Med., 31 (1), 98-100 (1994). 240 Ryohei Kato, Osamu Takahashi, Yoshiaki Kiso, Ikuo Moriguchi, Shuichi Hirono, Solution structure of HIV-1 protease-allophenylnorstatine derivative inhibitor complex obtained from molecular dynamics simulation. Chem. Pharm. Bull., 42 (1), 176-178 (1994). 241 木曽良明．HIVプロテアーゼ阻害剤の理論的なデザイン−ペプチド化学を基盤とした創薬研究．ファルマシア30 (3), 246-248 (1994). Yoshiaki Kiso. Rational design of HIV protease inhibitors - Medicinal chemistry study based on peptide chemistry. Farumashia, 30 (3), 246-248 (1994). 242 Yoichi Fujiwara, Kenichi Akaji, Yoshiaki Kiso, Racemization-free synthesis of C-terminal cysteine-peptide using 2-chlorotrityl resin. Chem. Pharm. Bull., 42 (3), 724-726 (1994). 243 Seiji Kageyama, Bradley D. Anderson, Barbara L. Hoesterery, Hideya Hayashi, Yoshiaki Kiso, Karl P. Flora, Hiroaki Mitsuya, Protein binding of human immunodeficiency virus protease inhibitor KNI-272 and alteration of its in vitro antiretroviral activity in the presence of high concentrations of proteins. Antimicrob. Agents Chemother., 38 (5), 1107-1111 (1994). 244 Yoichi Fujiwara, Kenichi Akaji, Yoshiaki Kiso, Studies on racemization of C-terminal cysteine in Fmoc-based solid phase peptide synthesis. Peptide Chemistry 1993, Ed. by Y. Okada, Protein Res. Found., Osaka, p29-32 (1994). 245 Hiroshi Enomoto, Tsutomu Mimoto, Sumitsugu Kisanuki, Tooru Kimura, Naoko Hattori, Seiji Kageyama, Hiroaki Mitsuya, Kenichi Akaji, Yoshiaki Kiso, Structure-activity relationships of tripeptide HIV protease inhibitors containing the hydroxymethylcarbonyl isostere. Peptide Chemistry 1993, Ed. by Y. Okada, Protein Res. Found., Osaka, p181-184 (1994). 246 木曽良明．ペプチドリード医薬のデザインと合成−HIVプロテアーゼ阻害剤を例として−．有機合成化学協会誌52 (5), 403-412 (1994). Yoshiaki Kiso. Design and synthesis of peptide lead drugs - HIV protease inhibitors as an example. J. Syn. Org. Chem. Jpn., 52 (5), 403-412 (1994). 247 木曽良明．レトロウイルス．有機合成化学協会誌52 (5), 461 (1994). Yoshiaki Kiso. Retrovirus. J. Syn. Org. Chem. Jpn., 52 (5), 461 (1994). 248 Kenichi Akaji, Naohiro Kuriyama, Yoshiaki Kiso, Efficient coupling of a, a-dimethyl amino acid using a new chloro imidazolidium reagent, CIP. Tetrahedron Letters, 35 (20), 3315-3318 (1994). 249 Yoshiaki Kiso, Toshio Fukui, Shigeki Tanaka, Tooru Kimura, Kenichi Akaji, A new reductive acidolysis final deprotection strategy in solid phase peptide synthesis. Use of a new safety-catch linker. Tetrahedron Letters, 35 (21), 3571-3574 (1994). 250 木曽良明．エイズ治療薬(抗HIV薬). 毎日ライフ，(6), 70-73 (1994). Yoshiaki Kiso. AIDS therapeutics (Anti-HIV drugs). Mainichi Life, (6), 70-73 (1994). 251 Yoshiaki Kiso, Makoto Yoshida, Yoichi Fujiwara, Tooru Kimura, Kenichi Akaji, Haruaki Yajima, Synthesis of natriuretic peptides using a new S-protecting group, S-trimethylacetamidomethyl (Tacm) group. Peptides: Design, Synthesis, and Biological Activity. Ed. by Channa Basava and G. M. Anantharamaiah, Birhauser, Boston, pp27-pp37 (1994). 252 Y. Kiso, T. Mimoto, J. Imai, S. Kisanuki, H. Enomoto, N. Hattori, K. Takada, K. Akaji, S. Kageyama, H. Mitsuya. The promising anti-HIV agent kynostatin (KNI)-272: A highly selective and super-active HIV protease inhibitor containing allophenylnorstatine. Peptides: Chemistry, Structure & Biology, Proc. 13th Amer. Peptide Symp., Ed by R. S. Hodges & J. A. Smith, ESCOM, Leiden, 1994, pp619-621. 253 A Kiriyama, K. Fujita, S. Takemura, H. Kuramoto, Y. Kiso, K. Takada. Plasma pharmacokinetics and urinary and biliary excretion of a new potent tripeptide HIV-1 protease inhibitor, KNI-272, in rats after intravenous administration. Biopharmaceut. Drug Disposition, 15 (7), 617-626 (1994). 254 Y. Kiso, N. Fujii, H. Yajima: New disulfide bond-forming reactions for peptide and protein synthesis. Brazilian J. Med. Biol. Res., 27 (12), 2733-2744 (1994). 255 Tsutomu Mimoto, Sumitsugu Kisanuki, Junya Imai, Hiroshi Enomoto, Naoko Hattori, Seiji Kageyama, Hiroaki Mitsuya, Kenichi Akaji, Kanji Takada, Yoshiaki Kiso: A potent tripeptide HIV protease inhibitor, kynostatin (KNI)-272: the potential anti-AIDS drug for oral administration. AIDS Research Newsletter, Proc. 7th Congr. Jpn. Soc. AIDS Res., 146 (1994). 256 Y. Kiso: Kynostatin (KNI)-272: a highly selective and superpotent HIV protease inhibitor containing allophenylnorstatine. Proc. 5th Akabori. Conf., Jpn.-Ger. Symp., p158-163 (1994). 257 Tooru Kimura, Jun Ohtake, Shingo Nakata, Hiroshi Enomoto, Hiroki Moriwaki, Kenichi Akaji, Yoshiaki Kiso. Synthesis of prodrugs of HIV protease inhibitors. Peptide Chemistry 1994, M. Ohno Ed., Protein Res. Found., Osaka, p157-160 (1995). 258 Hajime Nishiuchi, Kenichi Akaji, Yoshiaki Kiso, Synthesis of human endothelin by regioselective disulfide formation using the silyl chloride-sulfoxide system. Peptide Chemistry 1994, M. Ohno Ed., Protein Res. Found., Osaka, p225-228 (1995). 259 Mahamoud M. Sheha, Shingo Nakata, Hiroshi Enomoto, Tooru Kimura, Tsutomu Mimoto, Naoko Hattori, Nadia M. Mahfouz, Hoda Y. Hassan, Adel F. Youssef, Kenichi Akaji, Yoshiaki Kiso. SAR of HIV protease inhibitors: P2 and P3 structural requirements. Peptide Chemistry 1994, M. Ohno Ed., Protein Res. Found., Osaka, p349-352 (1995). 260 Yoshiaki Kiso, Penetration enhancement of peptide drugs: Palmitoyl derivatives of insulin and a transition-state mimic tripeptide inhibitor of HIV protease as a potential anti-AIDS drug for oral administration. Drug Targeting & Delivery, vol.4: Trends and Future Perspectives in Peptide & Protein Delivery, ed. by V. H. L. Lee, M. Hashida, and Y. Mizushima, Harwood Academic Publishers GmbH, Switzerland, p 71-82 (1995). 261 Y. Kiso, T. Mimoto, H. Enomoto, S. Kisanuki, H. Moriwaki, T. Kimura, N. Hattori, H. Hayashi, K. Takada, K. Akaji, S. Kageyama, H. Mitsuya, Kynostatins, highly selective and superpotent HIV protease inhibitors: Conformationally constrained tripeptides containing allophenylnorstatine as a transition-state mimic. Peptides 1994: Proc. 23rd Eur. Peptide Symp., ed by H. L. S. Maia, ESCOM, Leiden, p71-72 (1995). 262 Kenichi Akaji, Hajime Nishiuchi, Yoshiaki Kiso. Synthesis of human endothelin-1 by regioselective disulfide formation using the silyl chloride-sulfoxide system. Tetrahedron Lett., 36 (11), 1875-1878 (1995). 263 Yoshiaki Kiso. Design and synthesis of HIV protease inhibitors containing allophenylnorstatine as a transition-state mimic. Adv. Exp. Med. Biol., 362, 413-423 (1995). 264 Baldwin, E. T., Bhat, T. N., Gulnik, S., Liu, B., Kiso, Y., Mitsuya, H., & Erickson, J. W. Structure of HIV-1 protease with KNI-272: A transition state mimetic inhibitor containing allophenylnorstatine. Adv. Exp. Med. Biol., 362, 445-449, (1995). 265 M. Sugahara, A. Kiriyama, Y. Hamada, Y. Kiso, K. Takada. Absorption of new HIV-1 protease inhibitor, KNI-272, after intraduodenal and intragastric administrations to rats: Effect of solvent. Biopharmaceut. Drug Disp., 16 (4), 269-277 (1995). 266 Eric T. Baldwin, T. Narayana Bhat, Sergei Gulnik, Beishan Liu, Igor A. Topol, Yoshiaki Kiso, Tsutomu Mimoto, Hiroaki Mitsuya, John W. Erickson. Structure of HIV-1 protease with KNI-272, a tight-binding transition-state analog containing allophenylnorstatine. Structure, 3 (6), 581-590 (1995). 267 木曽良明．ウイルス蛋白プロセッシングの阻害，HIVプロテアーゼインヒビター．Mebio，12 (9), 78-86 (1995). Yoshiaki Kiso. Inhibition of viral protein processing, HIV protease inhibitors. Mebio，12 (9), 78-86 (1995). 268 Yoshiaki Kiso, Haruaki Yajima, Amide formation, deprotection and disulfide formation in peptide synthesis. In: Peptides: Syntheses, Structures, and Applications. (B. Gutte, Ed.). Academic Press, USA, p39-91 (1995). 269 Kenichi Akaji, Yasunori Tamai, Yoshiaki Kiso. Efficient synthesis of alamethicin F-30 using a chloro imidazolidium coupling reagent, CIP. Tetrahedron Letters, 36 (51), 9341-9344 (1995). 270 木村徹，木曽良明．市販エルカトニン製剤の化学的分析評価．基礎と臨床，29(6), 1625-1629 (1995). Tooru Kimura, Yoshiaki Kiso. Results of chemical analysis of commercially available elcatonin preparations. Kiso to Rinsho, 29(6), 1625-1629 (1995). 271 Kenichi Akaji, Naohiro Kuriyama, Yasunori Tamai, Yoshiaki Kiso. Efficient Coupling of dialkyl amino acid using a chloro imidazolidium reagent, CIP. Peptide Chemistry 1995, ed by N. Nishi, Protein Res. Found., Osaka, p33-36, (1996). 272 Takeaki Fujiwara, Naoki Nishizawa, Tooru Kimura, Kenichi Akaji, Yoshiaki Kiso. Solid phase synthesis of a mercaptoamide peptide using new linkers. Peptide Chemistry 1995, ed by N. Nishi, Protein Res. Found., Osaka, p53-56, (1996). 273 Kenichi Akaji, Yasunori Tamai, Yoshiaki Kiso. Efficient synthesis of alamethicin using a newly developed coupling reagent, CIP. Peptide Chemistry 1995, ed by N. Nishi, Protein Res. Found., Osaka, p121-124, (1996). 274 Takatoshi Mitoguchi, Shingo Nakata, Hiroshi Enomoto, Tooru Kimura, Kenichi Akaji, Naoko Hattori, Ryohei Kato, Tutomu Mimoto, Yoshiaki Kiso. Small-sized HIV protease inhibitors containing allophenylnorstatine as a substrate transition-state mimic. Peptide Chemistry 1995, ed by N. Nishi, Protein Res. Found., Osaka, p373-376, (1996). 275 Y. Kiso, T. Kimura, J. Ohtake, S. Nakata, H. Enomoto, H. Moriwaki, M. Nakatani, K. Akaji. “O®N intramolecular acyl migration”-type prodrugs of tripeptide inhibitors of HIV protease. Peptides: Chem. Str. Biol., ed by Pravin T. P. Kaumaya & Robert S. Hodges, Mayflower Sci. Ltd., p157-159 (1996). 276 A. Kiriyama, M. Sugahara, Y. Yoshikawa, Y. Kiso, K. Takada. The bioavailability of oral dosage forms of a new HIV-1 protease inhibitor, KNI-272, in beagle dogs. Biopharmaceut. Drug Disp. 17 (2), 125-134 (1996). 277 Yoshiaki Kiso, Design and synthesis of substrate-based peptidomimetic HIV protease inhibitors containing the hydroxymethylcarbonyl isostere. Biopolymers 40 (2), 235-244 (1996). 278 Kenichi Akaji, Naohiro Kuriyama, Yoshiaki Kiso. Convergent synthesis of (-)-mirabazole C using a chloroimidazolidium coupling reagent, CIP. J. Org. Chem. 61 (10), 3350-3357 (1996). 279 Michael A. Ussery, Owen L. Wood, Dennis D. Broud, Matthew Bacho, Steven C. Kunder, Susan Papermaster, Yoshiaki Kiso, Paul L. Black. Antiviral activity of the protease inhibitor KNI-272 in vivo in the HIV-infected HuPBMC-SCID mouse model. Antiviral Res. 30 (1), A18 (1996). 280 Y. Kiso, T. Mimoto, R. Kato, T. Mitoguchi, S. Nakata, T. Kimura, J. W. Erickson, M. A. Ussery. Small-sized HIV protease inhibitors containing allophenylnorstatine exhibit antiviral activities. Antiviral Res. 30 (1), A57 (1996). 281 木曽良明，AIDS治療薬としてのHIVプロテアーゼ阻害薬—変異ウイルスと人類の共生は可能か—．医学のあゆみ177 (13), 962-968 (1996). Yoshiaki Kiso. HIV protease inhibitors as AIDS therapeutics. Igaku no Ayumi, 177 (13), 962-968 (1996). 282 Yoichi Fujiwara, Junichi Yokotani, Kenichi Akaji, Yoshiaki Kiso. Synthesis of human C-type natriuretic peptide 22 using chlorotrityl resin and tetrafluoroboric acid deprotection. Chem. Pharm. Bull. 44 (7) 1326-1331 (1996). 283 Yun-Xing Wang, Darön I. Freedberg, Toshimasa Yamazaki, Paul T. Wingfield, Stephen J. Stahl, Joshua D. Kaufman, Yoshiaki Kiso, Dennis A. Torchia, Solution NMR evidence that the HIV-1 protease catalytic aspartyl groups have different ionization states in the complex formed with the asymmetric drug KNI-272. Biochemistry, 35 (31) 9945-9950 (1996). 284 Yoshiaki Kiso. Design and synthesis of substrate-based peptidomimetic HIV protease inhibitors containing allophenylnorstatine. Proc. 6th Akabori Conf., 100-105 (1996). 285 Y. Ohno, Y. Kiso, Y. Kobayashi, Solution conformations of KNI-272, a tripeptide HIV protease inhibitor designed on the basis of substrate transition state: Determined by NMR spectroscopy and simulated annealing calculations. Bioorg. Med. Chem. 4 (9) 1565-1572 (1996). 286 木曽良明．ナトリウム利尿ペプチド(ANP, BNP, CNP)とその前駆体．廣川タンパク質化学第11巻，ホルモン系タンパク質およびポリアミンII，279-289 (1996). Yoshiaki Kiso. Natriuretic peptides (ANP, BNP, CNP) and their precursors. Hirokawa Tanpakushitsu Kagaku, Vol. 11, pp279-189 (1996 Hirokawa Shoten). 287 木曽良明．エンドセリンとその前駆体．廣川タンパク質化学第11巻，ホルモン系タンパク質およびポリアミンII，291-297 (1996).10.30. Yoshiaki Kiso. Endothelins and their precursors. Hirokawa Tanpakushitsu Kagaku, Vol. 11, pp291-297 (1996 Hirokawa Shoten). 288 向山政志，道端英雄，木曽良明，中尾一和．アドレノメデュリンに対するモノクローナル抗体の開発と応用．現代医療，28 (11), 2769-2772 (1996). Masashi Mukoyama, Hideo Michibata, Yoshiaki Kiso, Kazuwa Nakao. Preparation and application of monoclonal antibodies against adrenomedulins. Gendai Iryo, 28 (11), 2769-2772 (1996). 289 木曽良明．HIVプロテアーゼインヒビター．Modern Physician, 16 (12), 1551-1552 (1996). Yoshiaki Kiso. HIV protease inhibitors. Modern Physician, 16 (12), 1551-1552 (1996). 290 Yun-Xing Wang, Daron I. Freedberg, Paul T. Wingfield, Stephen J. Stahl, Joshua D. Kaufman, Yoshiaki Kiso, T. Narayana Bhat, John W. Erickson, Dennis A. Torchia: Bound water molecules at the interface between the HIV-1 protease and a potent inhibitor, KNI-272, determined by NMR. J. Am. Chem. Soc., 118 (49), 12287-12290 (1996). 291 A. Kiriyama, T. Nishiura, M. Ishido, Y. Yamamoto, I Ogita, Y. Kiso, K. Takada. Binding characteristics of KNI-272 to plasma proteins, a new potent tripeptide HIV protease inhibitor. Biopharmaceut. Drug Disp., 17 (9), 739-751 (1996). 292 木曽良明．論理的にデザインされたHIVプロテアーセ阻害剤．学士会会報No.814, 113-118 (1997). Yoshiaki Kiso. Rationally designed HIV protease inhibitors. Gakushikai Kaiho No. 814, 113-118 (1997). 293 Tooru Kimura, Toshio Fukui, Shigeki Tanaka, Kenichi Akaji, Yoshiaki Kiso. A reductive acidolysis final deprotection strategy in solid phase peptide synthesis based on safety-catch protection. Chem. Pharm. Bull., 45 (1), 18-26 (1997). 294 Kenichi Akaji, Yasunori Tamai, Yoshiaki Kiso: Efficient synthesis of peptaibol using a chloroimidazolidium coupling reagent, CIP. Tetrahedron, 53 (2), 567-584 (1997). 295 木曽良明．[AIDSの治療] 抗HIV剤(2)プロテアーゼ阻害剤．臨床科学，33 (1), 10-19 (1997). Yoshiaki Kiso. Therapy of AIDS. Anti-HIV drugs (2) Protease inhibitors. Rinsho Kagaku, 33 (1), 10-19 (1997). 296 木曽良明．HIVプロテアーゼ阻害剤：HIV感染症治療における位置づけ．化学療法の領域, 13 (3), 465-472 (1997). Yoshiaki Kiso. HIV protease inhibitors. Role in treatment of HIV infection. Kagaku Ryoho no Ryoiki, 13 (3), 465-472 (1997). 297 Kenichi Akaji, Naohiro Kuriyama, Yoshiaki Kiso: Total synthesis of (-)-mirabazole B using a chloroimidazolidium reagent, CIP. Peptide Chemistry 1996: C. Kitada (Ed.) Protein Research Foundation, Osaka, pp53-56 (1997). 298 Naoki Nishizawa, Tooru Kimura, Hikaru Matsumoto, Takeaki Fujiwara, Haruo Takaku, Kenichi Akaji, Yoshiaki Kiso: Synthesis of an HIV-1 protease analogue by the chemoselective ligation method using a new disulfide type linker. Peptide Chemistry 1996: C. Kitada (Ed.) Protein Research Foundation, Osaka, pp61-64 (1997). 299 Satoshi Yamaguchi, Takatoshi Mitoguchi, Shingo Nakata, Tooru Kimura, Kenichi Akaji, Satoshi Nojima, Haruo Takaku, Tsutomu Mimoto, Yoshiaki Kiso: Synthesis of HIV protease dipeptide inhibitors and prodrugs. Peptide Chemistry 1996: C. Kitada (Ed.) Protein Research Foundation, Osaka, pp297-300 (1997). 300 Yamazaki, T., Kiso, Y., Wang, Y. X., Freedberg, D. I., Torchia, D. A., Wingfield, P., Stahl, S. J., Kaufman, J. D., Solution NMR studies of the HIV-1 protease/inhibitor complex: The HIV-1 protease catalytic aspartyl side-chain carboxyl groups have distinct protonation states in the complex formed with the asymmetric inhibitor KNI-272. Peptide Chemistry 1996: C. Kitada (Ed.) Protein Research Foundation, Osaka, pp337-340 (1997). 301 木曽良明．次世代エイズ治療薬としてのHIVプロテアーゼ阻害薬の登場．日本臨牀, 55 (5), 1287-1295 (1997). Yoshiaki Kiso. Approval of HIV protease inhibitors as the AIDS therapeutics of next generation. Nippon Rinsho, 55 (5), 1287-1295 (1997). 302 Yasushi Arano, Hiromichi Akizawa, Takashi Uezono, Kenichi Akaji, Masahiro Ono, Susumu Funakoshi, Mitsuru Koizumi, Akira Yokoyama, Yoshiaki Kiso, Hideo Saji. Conventional and high-yield synthesis of DTPA-conjugated peptides: Application of a monoreactive DTPA to DTPA-D-Phe1-octerotide synthesis. Bioconjugate Chem. 8 (3), 442-446 (1997). 303 Naohiro Kuriyama, Kenichi Akaji, Yoshiaki Kiso. Convergent synthesis of (-)-mirabazole B using a chloroimidazolidium coupling reagent, CIP. Tetrahedron, 53 (25), 8323-8334 (1997). 304 Kenichi Akaji, Yoshiaki Kiso. Macrocyclization on solid support using Heck reaction. Tetrahedron Lett., 38 (29), 5185-5188 (1997). 305 木曽良明．グラフィックスを用いるプロテアーゼ・阻害剤系の構造解析．蛋白質 核酸 酵素，42 (14), 2465-2473 (1997). Yoshiaki Kiso, Structural analysis of protease-inhibitor system using graphics. Tanpakushitsu Kakusan Koso, 42 (14), 2465-2473 (1997). 306 木曽良明．ウイルスプロテアーゼ．メディカル用語ライブラリー：ウイルス・細菌感染newファイル．28-31頁 羊土社（東京）(1997).7 Yoshiaki Kiso. Viral proteases. Medical Term Library: Viral and Bacterial Infection New File, p28-31, Yodo Sha, Tokyo (1997). 307 木曽良明．ウイルスプロテアーゼ阻害剤．メディカル用語ライブラリー：ウイルス・細菌感染newファイル．106-108頁 羊土社（東京）(1997).7 Yoshiaki Kiso. Viral protease inhibitors. Medical Term Library: Viral and Bacterial Infection New File, p106-108, Yodo Sha, Tokyo (1997). 308 木曽良明．薬剤耐性機構と多剤併用療法．メディカル用語ライブラリー：ウイルス・細菌感染newファイル．109-110頁 羊土社（東京）(1997).7 Mechanism of drug resistance and combination therapy. Medical Term Library: Viral and Bacterial Infection New File, p109-110, Yodo Sha, Tokyo (1997). 309 木曽良明．ヒトとHIVの共生をめざした抗エイズ薬．HIV／AIDS研究はいま．基礎研究の現場から．156-169頁（1997） Yoshiaki Kiso: Anti-AIDS drugs aiming at coexistence of human and HIV. Current HIV/AIDS Research. From the Basic Research. pp156-169 (1997) 310 310 木曽良明．エイズ治療薬としてのHIVプロテアーゼ阻害薬．京薬會誌，NO.107, 1-7 (1997).12 Yoshiaki Kiso: HIV protease inhibitors as therapeutics for AIDS. Kyouyaku Kaishi, No. 107, p1-7 (1997). 311 Toshiyuki Goto, Kikuko Nishizato, Takashi Nakano, Shinichi Morimatsu, Kouichi Sano, Yoshiaki Kiso, Masuyo Nakai. Inhibition sites in HIV-infected cells by a protease inhibitor, KNI-272. AIDS Res. Newsletter, 153 (1997). 312 Yoshiaki Kiso, Tsutomu Mimoto, Ryohei Kato, Takatoshi Mitoguchi, Shingo Nakata, Tooru Kimura, John W. Erickson, Michael A. Ussery. Small peptidomimetic HIV protease inhibitors containing allophenylnorstatine exhibit antiviral activities. Peptides 1996, R. Ramage & R. Epton (Eds.), The European Peptide Society, p541-542 (1997). 313 Yoshiaki Kiso, Satoshi Yamaguchi, Hikaru Matsumoto, Tsutomu Mimoto, Ryohei Kato Satoshi Nojima, Haruo Takaku, Tominaga Fukazawa, Tooru Kimura, Kenichi Akaji: KNI-577, a potent small-sized HIV protease inhibitor based on the dipeptide containing the hydroxymethylcarbonyl isostere as an ideal transition-state mimic. Arch. Pharm. Pharm. Med. Chem. 331 (3), 87-89 (1998). 314 木曽良明．プロテアーゼ阻害剤とその耐性機序．診断と治療，86 (4), 542-546 (1998).4Yoshiaki Kiso. Protease inhibitors and their resistance mechanism. Shindan To Chiryo, 86 (4), 542-546 (1998). 315 木曽良明．エイズ治療薬としてのHIVプロテアーゼ阻害剤の開発．−基質遷移状態に基づく分子設計−蛋白質 核酸 酵素，43 (6), 725-733 (1998).5. Yoshiaki Kiso. Development of HIV protease inhibitors as anti-AIDS drugs; Molecular design based on substrate transition state. Tanpakushitsu Kakusan Koso, 43 (6), 725-733 (1998). 316 木曽良明．HIVプロテアーゼの働きとプロテアーゼ阻害薬の作用機構．Confronting HIV 98, No. 7, 5-7 (1998).2. Yoshiaki Kiso. Role of HIV protease and reaction mechanism of protease inhibitors. Confronting HIV 98, No. 7, 5-7 (1998). 317 Hideo Michibata, Masashi Mukoyama, Issei Tanaka, Shin-ichi Suga, Masayo Nakagawa, Rieko Ishibashi, Masahisa Goto, Kenichi Akaji, Yoichi Fujiwara, Yoshiaki Kiso, Kazuwa Nakao, Autocrine/paracrine role of adrenomedullin in cultured endothelial and mesangial cells. Kidney International, 53 (4), 979-985 (1998). 318 後藤俊幸，中野隆史，河野武弘，森田智津子，森松伸一，木曽良明，中井益代，佐野浩一．プロテアーゼ阻害剤KNI-272のHIV-1粒子形成に及ぼす作用．Minophagen Medical Review, 43 (2), 61-63 (1998).3. Toshiyuki Goto, Takafumi Nakano, Takehiro Kohno, Chizuko Morita, Shinichi Morimatsu, Yoshiaki Kiso, Masuyo Nakai, Koichi Sano. Effect of protease inhibitor KNI-272 on HIV-1 particle formation. Minophagen Medical Review, 43 (2), 61-63 (1998). 319 木曽良明．International Conference on Protease Inhibitors ‘97（国際プロテアーゼインヒビター会議’９７）重点領域研究「蛋白分解のニューバイオロジー」ニュース・ぷろておりしす，No.6, 25-29 (1998).2. Yoshiaki Kiso: International Conference on Protease Inhibitors ’97. Neurobiology of Proteolysis Newsletter, No. 6, p25-29 (1998). 320 Masatoshi Tanaka, Tsutomu Mimoto, Barry D. Anderson, Sergei Gulnik, Tien N. Bhat, Mark F. Kavlick, Keisuke Yusa, Hideya, Hayashi, Yoshiaki Kiso, John W. Erickson, Hiroaki Mitsuya. Identification of protease inhibitors containing allophenylnorstatine active against both wild type and KNI-272-resistant HIV-1. AIDS Research Newsletter, Proceedings of the 11th Congress of the Japanese Society for AIDS Research, pp48 (1998).5. 321 木曽良明，青柳高明，水谷栄彦，豊岡照彦．座談会・プロテアーゼインヒビター：プロテアーゼインヒビターが医科学に与えたインパクト．治療学，32 (8), 659-670 (1998) Yoshiaki Kiso, Takaaki Aoyagi, Shigehiko Mizutani, Terhiko Toyooka. Discussions: Protease inhibitors: the impact of protease inhibitors on medical science. Chiryogaku, 32 (8), 659-670 (1998) 322 木曽良明．序説／プロテアーゼインヒビター：プロテアーゼインヒビター研究の最近の動向．治療学，32 (8), 964-967 (1998). Yoshiaki Kiso. Protease inhibitors: Recent trends of protease inhibitor studies. Chiryogaku, 32 (8), 964-967 (1998). 323 三本勤，木曽良明．プロテアーゼインヒビターの基礎と応用６．ウイルスプロテアーゼインヒビター．治療学，32 (8), 1001-1004 (1998). Tsutomu Mimoto, Yoshiaki Kiso. Basic and clinical studies on protease inhibitors. Viral protease inhibitors. Chiryogaku, 32 (8), 1001-1004 (1998). 324 Daron I. Freedberg, Yun-Xing Wang, Stephen J. Stahl, Joshua D. Kaufman, Paul T. Wingfield, Yoshiaki Kiso, Dennis A. Torchia. Flexibility and function in HIV protease: Dynamics of the HIV-1 protease bound to the asymmetric inhibitor kynostatin 272 (KNI-272). J. Am. Chem. Soc., 120 (31), 7916-7923 (1998).8. 325 Yoshiaki Kiso. Design and synthesis of a covalently linked HIV-1 protease dimer analog and peptidomimetic inhibitors. J. Synthetic Org. Chem., 56 (11), 896-907 (1998).11. 326 木曽良明：酵素活性中心をターゲットとしてデザインされたエイズ治療薬の開発．平成９年度エイズ医薬品等開発推進事業・国際研究グラント事業研究報告書，43-53 (1998).6. Yoshiaki Kiso: Development of Anti-AIDS Drugs Designed Using Enzyme Active Site as the Target. Research Report: FY1997 Promoting Project of AIDS Therapeutics / International Research Grants, 43-53 (1998). 327 Yoshiaki Kiso, Synthesis of HIV protease analogs and inhibitors. Proceedings of the 7th Akabori Conference: Japanese - German Symposium on Peptide Chemistry, (ed. by Horst Kunz), p46-49 (1998). 328 Hiromichi Akizawa, Yasushi Arano, Takashi Uezono, Masahiro Ono, Yasushi Fujioka, Tomoya Uehara, Akira Yokoyama, Kenichi Akaji, Yoshiaki Kiso, Mitsuru Koizumi, Hideo Saji. Renal metabolism of 111In-DTPA-D-Phe1-octerotide in vivo. Bioconjugate Chem., 9 (6), 662-670 (1998).11. 329 Kenichi Akaji, Yuzo Hayashi, Yoshiaki Kiso, Naohiro Kuriyama. Convergent synthesis of dolastatin 15 by solid phase coupling of an N-methylamino acid. J. Org. Chem., 64 (2), 405-411 (1999). 330 Tooru Kimura, Hikaru Matsumoto, Takashi Matsuda, Tomonori Hamawaki, Kenichi Akaji, Yoshiaki Kiso. A new class of anti-HIV agents: synthesis and activity of conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor. Bioorg. Med. Chem. Lett., 9 (6), 803-806 (1999). 3. 331 木曽良明．新刊紹介「２１世紀の創薬科学」月刊薬事，41 (4) 816 (1999)3. 332 Yoshiaki Kiso, Tooru Kimura, Yoichi Fujiwara, Naoki Nishizawa, Hikaru Matsumoto, Masamichi Kishida, Kenichi Akaji, Haruo Takaku. Synthesis of HIV-1 protease analog by ligation of bromoacetyl and mercaptoethylamide peptide prepared using disulfide linkage to solid-support. Peptides: Frontiers of peptide science (ed. by J. P. Tam and P. T. P. Kaumaya) Kluwer Academic Publishers, Dordrecht, The Netherlands, pp333-334 (1999). 333 Yoshiaki Kiso, Satoshi Yamaguchi, Hikaru Matsumoto, Tsutomu Mimoto, Ryohei Kato, Satoshi Nojima, Haruo Takaku, Tominaga Fukazawa, Tooru Kimura, Kenichi Akaji. Potent dipeptide HIV protease inhibitors containing the hydroxymethylcarbonyl isostere as an ideal transition-state mimetic. . Peptides: Frontiers of peptide science (ed. by J. P. Tam and P. T. P. Kaumaya) Kluwer Academic Publishers, Dordrecht, The Netherlands, pp667-669 (1999). 334 Yoshiaki Kiso, Satoshi Yamaguchi, Hikaru Matsumoto, Tooru Kimura, Kenichi Akaji. “O, N-Acyl migration”-type prodrugs of dipeptide HIV protease inhibitors. Peptides: Frontiers of peptide science (ed. by J. P. Tam and P. T. P. Kaumaya) Kluwer Academic Publishers, Dordrecht, The Netherlands, pp678-679 (1999). 335 Kenichi Akaji, Yuzo Hayashi, Yoshiaki Kiso, Naohiro Kuriyama. Convergent synthesis of dolastatin 15 by solid phase coupling of N-methylamino acid. Peptide Science 1998 (ed. by M. Kondo) Protein Research Foundation, Osaka, Japan, pp9-12 (1999). 336 Yoichi Fujiwara, Tooru Kimura, Kenichi Akaji, Yoshiaki Kiso. Studies on Nin-protecting groups during the synthesis of Trp-containing cystine peptide by silyl chloride-sulfoxide method. Peptide Science 1998 (ed. by M. Kondo) Protein Research Foundation, Osaka, Japan, pp129-132 (1999). 337 Takashi Matsuda, Hikaru Matsumoto, Tomonori Hamawaki, Tooru Kimura, Kenichi Akaji, Yoshiaki Kiso. Synthesis and activity of a new type of anti-HIV agents, conjugate of HIV protease inhibitor with reverse transcriptase inhibitor. Peptide Science 1998 (ed. by M. Kondo) Protein Research Foundation, Osaka, Japan, pp305-308 (1999). 338 Etsuko Katoh, Toshimasa Yamazaki, Yoshiaki Kiso, Paul T. Wingfield, Stephen J. Stahl, Joshua D. Kaufman, Dennis A. Torchia. Determination of the Rate of Monomer Interchange in a Ligand-Bound Homodimeric Protein from NOESY Cross Peaks: Application to the HIV Protease/KNI-529 Complex. J. Amer. Chem. Soc., 121 (11), 2607-2608 (1999). 339 Tsutomu Mimoto, Ryohei Kato, Haruo Takaku, Satoshi Nojima, Keisuke Terashima, Satoru Misawa, Tominaga Fukazawa, Takamasa Ueno, Hideharu Sato, Makoto Shintani, Yoshiaki Kiso, Hideya Hayashi. Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine. J. Med. Chem., 42 (10), 1789-1802 (1999). 340 Yoshiaki Kiso. Editorial: Protease inhibitors. Biopolymers, 51 (1) 1 (1999). 341 Yoshiaki Kiso, Hikaru Matsumoto, Sota Mizumoto, Tooru Kimura, Yoichi Fujiwara, Kenichi Akaji. Small dipeptide-based HIV protease inhibitors containing the hydroxymethylcarbonyl isostere as an ideal transition-state mimic. Biopolymers, 51 (1) 59-68 (1999). 342 Y. Kiso. Developments in peptide synthesis and peptidomimetic chemistry: HIV protease analogs and substrate-based inhibitors. Peptide Science - Present & Future, (Y. Shimonishi, ed), p475-479, Kluwer Academic Publishers (1999). 343 T. Mimoto, R. Kato, H. Takaku, S. Misawa, T. Fukazawa, S. Nojima, K. Terashima, H. Sato, M. Shintani, Y. Kiso, H. Hayashi. KNI-764, a novel dipeptide-based HIV protease inhibitor containing allophenylnorstatine. Peptide Science - Present & Future, (Y. Shimonishi, ed), p652-653, Kluwer Academic Publishers (1999). 344 A. A. Bekhit, H. Matsumoto, H. M. M. Abdel-Rahman, T. Mimoto, S. Nojima, H. Takaku, T. Kimura, K. Akaji, Y. Kiso. Allophenylnorstatine containing HIV-1 protease inhibitors: design, synthesis and structure-activity relationships for selected P2 and P2’ ligands. Peptide Science - Present & Future, (Y. Shimonishi, ed), p660-661, Kluwer Academic Publishers (1999). 345 H. M. M. Abdel-Rahman, H. Matsumoto, A. A. Bekhit, T. Mimoto, S. Nojima, H. Takaku, T. Kimura, K. Akaji, Y. Kiso. Allophenylnorstatine containing HIV-1 protease inhibitors: design, synthesis and structure-activity relationships for selected P2 ligands. Peptide Science - Present & Future, (Y. Shimonishi, ed), p662-664, Kluwer Academic Publishers (1999). 346 Kenichi Akaji, Yoshiaki Kiso. Total synthesis of thiangazole. Tetrahedron, 55 (35), 10685-10694 (1999). 347 Yoshiaki Kiso, Hikaru Matsumoto, Satoshi Yamaguchi, Tooru Kimura. Design of small peptidomimetic HIV-1 protease inhibitors and prodrug forms. Letters in Peptide Science, 6(5), 275-281 (1999).9. 348 木曽良明．蛋白質・ペプチドの化学．生体内での働き者．化学と教育．47 (9) 623- 627 (1999). Yoshiaki Kiso, Chemistry of proteins & peptides. Hard workers in the body. Kagaku to Kyoiku, 47 (9) 623- 627 (1999). 349 木曽良明，板井昭子．コンピュータ支援によるドラッグデザイン．廣川書店(1999) Yoshiaki Kiso, Akiko Itai: Computer-aided Drug Design, Hirokawa Shoten (1999) translation work. 350 Yoshio Hayashi, Kiyoko Iijima, Jun Katada, Yoshiaki Kiso. Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors. Bioorg. Med. Chem. Lett., 10 (3) 199-201 (2000). 351 木曽良明．HIVプロテアーゼ阻害剤．廣川有機薬科学実験講座第１巻．創薬指向の分子設計−基礎と展開（梅山秀明，福原健一編集）p224-233(2000).2.25. Yoshiaki Kiso: HIV Protease Inhibitors. Hirokawa Organic Pharmaceutical Science Laboratory Manuals, Vol. 1. Molecular Design Directed Toward Drug Discovery - Basics and Application (H. Umeyama, K. Fukuhara Eds) pp224-233 (2000). 352 Toshimasa Yamazaki, Etsuko Katoh, Yoshiaki Kiso, Dennis A. Torchia. NMR studies on reorientation process of the inhibitor tightly bound to HIV protease. Peptide Science 1999, N. Fujii Ed. The Japanese Peptide Society, p75-78 (2000). 353 Hikaru Matsumoto, Tooru Kimura, Tomonori Hamawaki, Yoshiaki Kiso. New type prodrugs of anti-HIV agents consisting of the HIV protease inhibitor and reverse transcriptase inhibitor. Peptide Science 1999, N. Fujii Ed. The Japanese Peptide Society, p187-188 (2000). 354 Kaneo Kanoh, Yoshio Hayashi, Shinkichi Kohno, Jun Katada, Isao Uno, Yoshiaki Kiso. Synthesis and biological activities of phenylahistin derivatives. Peptide Science 1999, N. Fujii Ed. The Japanese Peptide Society, p409-412 (2000). 355 Hikaru Matsumoto, Tomonori Hamawaki, Hisashi Ota, Tooru Kimura, Toshiyuki Goto, Kouichi Sano, Yoshio Hayashi, Yoshiaki Kiso. “Double-drugs”-A new class of prodrug forms of an HIV protease inhibitor conjugated with a reverse transcriptase inhibitor by a spontaneously cleavable linker. Bioorg. Med. Chem. Lett.,10 (11), 1227-1231 (2000).6.5 356 木曽良明：アミノ酸の略号の由来．ファルマシア36 (7), 652-653 (2000). Yoshiaki Kiso: Origin of Amino Acid Code. Farumashia, 36 (7), 652-653 (2000). 357 Tsutomu Mimoto, Naoko Hattori, Haruo Takaku, Shumitsugu Kisanuki, Tominaga Fukazawa, Keisuke Terashima, Ryohei Kato, Satoshi Nojima, Satoru Misawa, Takamasa Ueno, Junya Imai, Hiroshi Enomoto, Shigeki Tanaka, Hiroshi Sakikawa, Makoto Shintani, Hideya Hayashi, Yoshiaki Kiso. Structure-activity relationship of orally potent tripeptide-based HIV protease inhibitors containing hydroxymethylcarbonyl isostere. Chem. Pharm. Bull., 48 (9), 1310-1326 (2000). 358 A. Velazquez-Campoy, I. Luque, M. J. Todd, M. Milutinovich, Y. Kiso, E. Freire. Thermodynamic dissection of the binding energetics of KNI-272, a potent HIV-1 protease inhibitor. Protein Sci., 9 (9), 1801-1809 (2000).9. 359 Yoshio Hayashi, Sumie Orikasa, Koji Tanaka, Kaneo Kanoh, Yoshiaki Kiso. Total synthesis of anti-microtubule diketopiperazine derivatives: phenylahistin and aurantiamine. J. Org. Chem. 65 (24) 8402-8405 (2000). 12.1 360 木曽良明：HIVプロテアーゼ阻害剤．ウイルス感染症との戦い—現状と２１世紀への展望—．p344-357, , 医薬ジャーナル社2000.11.10 Yoshiaki Kiso: HIV Protease Inhibitors. Strategy against Viral Infection - Present Status and Scope in 21st Century. pp344-357, Iyaku Journal Sha (2000). 361 Sheha, M.M., Mahfouz, N.M., Hassan, H.Y., Youssef, A.F., Mimoto, T., Kiso, Y., Synthesis of di- and tripeptide analogues containing alpha-ketoamide as a new core structure for inhibition of HIV-1 protease. Eur. J. Med. Chem., 35 (10), 887-894 (2000). 362 Tomomi Uchiyama, Atsushi Kotani, Hiroyuki Tatsumi, Takeshi Kishida, Aya Okamoto, Naoki Okada, Masahiro Murakami, Takuya Fujita, Yoichi Fujiwara, Yoshiaki Kiso, Shozo Muranishi, Akira Yamamoto: Development of novel lipophilic derivatives of DADLE (Leucine enkephalin analogue): Intestinal permeability characteristics of DADLE derivatives in rats. Pharm. Res., 17 (12), 1461-1467 (2000). 363 木曽良明：薬剤耐性をいかに克服するか—分子認識に基づく耐性克服エイズ治療薬のデザインと開発を例として—．臨床と微生物，28(1), 65-72 (2001). Yoshiaki Kiso: How to Overcome Drug Resistance - Design and Development of Resistance-Surmountable Anti-AIDS Drugs Based on Molecular Recognition. Rinsho To Biseibutsu, 28(1), 65-72 (2001). 364 Hikaru Matsumoto, Takashi Matsuda, Shingo Nakata, Takatoshi Mitoguchi, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso. Synthesis and biological evaluation of prodrug-type anti-HIV agents: Ester conjugates of carboxylic acid-containing dipeptide HIV protease inhibitors and a reverse transcriptase inhibitor. Bioorg. Med. Chem., 9(2), 417-430 (2001). 365 Hikaru Matsumoto, Youhei Sohma, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso. Controlled drug release: new water-soluble prodrugs of an HIV protease inhibitor. Bioorg. Med. Chem. Lett., 11 (4), 605-609 (2001). 366 Toshiyuki Goto, Takashi Nakano, Takehiro Kohno, Shinichi Morimatsu, Chizuko Morita, Wu Hong, Yoshiaki Kiso, Masuyo Nakai, Kouichi Sano: Targets of a protease inhibitor, KNI-272, in HIV-1-infected cells. J. Med. Virol., 63 (3), 203-209 (2001). 367 Yoshio Hayashi, Sumie Orikasa, Koji Tanaka, Kaneo Kanoh, Yoshiaki Kiso. Synthetic study of anti-microtubule diketopepirazines: phenylahistin and aurantiamine. Peptide Science 2000, T. Shioiri Ed. The Japanese Peptide Society, 73-76 (2001). 368 Yoshiaki Kiso, Hikaru Matsumoto, Tomonori Hamawaki, Hisashi Ota, Tooru Kimura, Toshiyuki Goto, Kouichi Sano, Yoshio Hayashi. Design of Double-Drug-Type Anti-HIV agents. Peptide Science 2000, T. Shioiri Ed. The Japanese Peptide Society, 213-216 (2001). 369 Hikaru Matsumoto, Youhei Sohma, Daisuke Shuto, Tomonori Hamawaki, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso. Spontaneously regenerable prodrug: Design and synthesis of water-soluble prodrugs of HIV protease inhibitors. Peptide Science 2000, T. Shioiri Ed. The Japanese Peptide Society, 237-240 (2001). 370 Hikaru Matsumoto, Tooru Kimura, Tomonori Hamawaki, Akira Kumagai, Toshiyuki Goto, Kouichi Sano, Yoshio Hayashi, Yoshiaki Kiso. Design, synthesis, and biological evaluation of anti-HIV double-drugs: conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor through spontaneously cleavable linkers. Bioorg. Med. Chem., 9 (6), 1589-1600 (2001).6 371 Adrian Velazquez-Campoy, Yoshiaki Kiso, Ernesto Freire. The binding energetics of first- and second-generation HIV-protease inhibitors: implications for drug design. Arch. Biochem. Biophys., 390 (2), 169-175 (2001).6/15 372 木曽良明：分子認識を基盤とする創薬科学研究．化学工業，52(6), 409-415 (2001). Yoshiaki Kiso: Medicinal Science Research Based on Molecular Recognition. Kagaku Kogyo, 52(6), 409-415 (2001). 373 松本光，相馬洋平，木曽良明：生体内で自発的に再生可能な水溶性プロドラッグ．化学工業，52(6), 439-443 (2001).Hikaru Matsumoto, Youhei Sohma, Yoshiaki Kiso: Spontaneously Bioregenerable Water-Soluble Prodrugs. Kagaku Kogyo, 52(6), 439-443 (2001). 374 Hiromichi Akizawa, Yasushi Arano, Masaki Mifune, Akimasa Iwado, Yutaka Saito, Tomoya Uehara, Masahiro Ono, Yasushi Fujioka, Kazuma Ogawa, Yoshiaki Kiso, Hideo Saji. Significance of 111In-DTPA chelate in renal radioactivity levels of 111In-DTPA-conjugated peptides. Nuclear Med. Biol., 28 (4), 459-468 (2001). 375 木村徹，松本光，木曽良明：自発的に再生可能な水溶性プロドラッグ：薬物放出時間の制御．MED CHEM NEWS, 11(3), 15-19 (2001). Tooru Kimura, Hikaru Matasumoto, Yoshiaki Kiso: Spontaneously Regenerable Water-soluble Prodrug. Control of Drug Release Time. MED CHEM NEWS, 11(3), 15-19 (2001). 376 Yoshio Hayashi, Yuko Kinoshita, Koushi Hidaka, Aiko Kiso, Hirokazu Uchibori, Tooru Kimura, Yoshiaki Kiso: Analysis of amide bond formation with an a-hdroxy-ß-amino acid derivative, 3-amino-2-hydroxy-4-phenylbutanoic acid, as an acyl component: Byproduction of Homobislactone. J. Org. Chem., 66 (16) 5537-5544 (2001). 377 Myeong-cheol Song, S. Rajesh, Yoshio Hayashi, Yoshiaki Kiso: Design and synthesis of new inhibitors of HIV-1 protease dimerization with conformationally constrained templates. Bioorg. Med. Chem. Lett., 11 (18), 2465-2468 (2001). 378 木曽良明：HIVプロテアーゼ阻害剤の開発．遺伝子医学，5(3), 477-482 (2001).2001.8 Yoshiaki Kiso: Development of HIV Protease Inhibitors. Idenshi Igaku, 5(3), 477-482 (2001). 379 木曽良明：HIVプロテアーゼ阻害剤のデザイン．特定領域研究「生物マシナリー」ニュースレター，No. 5, 24-30 (2001). Yoshiaki Kiso: Design of HIV Protease Inhibitors. Biological Machinery Newsletters, No. 5, 24-30 (2001). 380 Hiromichi Akizawa, Yasushi Arano, Masaki Mifune, Akimasa Iwado, Yutaka Saito, Takahiro Mukai, Tomoya Uehara, Masahiro Ono, Yasushi Fujioka, Kazuma Ogawa, Yoshiaki Kiso, Hideo Saji: Effect of molecular charges on renal uptake of 111In-DTPA-conjugated peptides. Nuclear Med. Biol., 28 (7), 761-768 (2001). 381 木曽良明：エイズと治療薬．タンパク質分解の不思議：こわれなくてもこわれすぎてもいけない．（クバプロ）p120-131 (2001) Yoshiaki Kiso: AIDS and Therapeutic Drugs. Mystery of Proteolysis. Kubapuro, pp120-131 (2001). 382 Mitsunobu Doi, Toshimasa Ishida, Yoshio Katsuya, Masahiro Sasaki, Taizo Taniguchi, Hiroshi Hasegawa, Tsutomu Mimoto, Yoshiaki Kiso: KNI-272, a highly selective and potent petidic HIV protease inhibitor. Acta Crystallogr. C, 57 (11), 1333-1335 (2001). 383 Toshiyuki Goto, Yoshiaki Kiso, Kouichi Sano: Targets of an HIV-1 protease inhibitor, KNI-272. International Antiviral News, 9 (8), 125-126 (2001). 384 Yoshio Hayashi, Sumie Orikasa, Koji Tanaka, Kaneo Kanoh, Yoshiaki Kiso: Phenylahistin, a Small Dipeptidic Colchicine-Like Anti-Microtubule Agent: Total Synthesis and SAR Study of the Derivatives. Peptides: The Wave of the Future. (Michal Lebl and Richard A. Houghten (Editors)), American Peptide Society, p638-639 (2001). 385 Yoshiaki Kiso, Hikaru Matsumoto, Tomonori Hamawaki, Youhei Sohma, Tooru Kimura, Yoshio Hayashi: Prodrug Forms of Peptidomimetic HIV Protease Inhibitors Using Intramolecular Cyclization Reaction. Peptides: The Wave of the Future. (Michal Lebl and Richard A. Houghten (Editors)), American Peptide Society, p650-651 (2001). 386 Azin Nezami, Irene Luque, Tooru Kimura, Yoshiaki Kiso, Ernest Freire: Identification and characterization of allophenylnorstatine-based inhibitors of plasmepsin II, an antimalarial target. Biochemistry,41 (7), 2273-2280 (2002). 387 Yoshio Hayashi, Yuko Kinoshita, Koushi Hidaka, Aiko Kiso, Hirokazu Uchibori, Tooru Kimura, Yoshiaki Kiso: Analysis of side reaction in the amide bond formation with an a-hydroxy-ß-amino acid as an acyl component. Peptide Science 2001, H. Aoyagi (Ed.), The Japanese Peptide Society, 37-40 (2002). 388 Myeong-cheol Song, S. Rajesh, Yoshio Hayashi, Yoshiaki Kiso: Design and synthesis of conformationally constrained dimerization inhibitors of HIV-1 protease. Peptide Science 2001, H. Aoyagi (Ed.), The Japanese Peptide Society, 211-212 (2002). 389 Youhei Sohma, Hikaru Matsumoto, Masato Sasaki, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Controlled drug release: design and application of new water-soluble prodrugs. Peptide Science 2001, H. Aoyagi (Ed.), The Japanese Peptide Society, 249-252 (2002). 390 木曽良明：ウイルスの薬剤耐性とその克服．ウイルス学からみた医療の安全性．メディカルレビュー社，44-50 (2002). Yoshiaki Kiso: Viral Drug Resistance and Solutions. Medical Safety from the Viewpoint of Virology. Medical Review, pp44-50 (2002). 391 Ei’ichi Ami, S. Rajesh, Jung Wang, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso, Toshimasa Ishida. Synthesis of novel amino acid, L-bis-tetrahydrofuranylglycines. Tetrahedron Letters, 43 (16), 2931-2934 (2002). 392 木曽良明，相馬洋平：新しいHIVプロテアーゼ阻害剤—大量投与や薬剤耐性などの問題克服をめざして．医学のあゆみ，201 (4), 231-235 (2002). 2002.4. Yoshiaki Kiso, Youhei Sohma: Novel HIV Protease Inhibitors. To Overcome Problems Such As High Dose and Drug Resistance. Igaku No Ayumi, 201 (4), 231-235 (2002). 393 Toshiyuki Goto, Chizuko Morita, Yoshihiko Fujioka, Takehiro Kohno, Sharad Mohan, Kouichi Sano, Hikaru Matsumoto, Tooru Kimura, Yoshiaki Kiso. Inhibition mechanism of a new prodrug, a conjugate of two anti-HIV-1 inhibitors. Proceedings of 15th International Congress on Electron Microscopy, 83-84 (2002). 394 Yoshio Hamada, Jun Ohtake, Youhei Sohma, Tooru Kimrua, Yoshio Hayashi, Yoshiaki Kiso. New water-soluble prodrugs of HIV protease inhibitors based on O→N intramolecular acyl migration. Bioorg. Med. Chem., 10 (12) 4155-4167 (2002). 395 相馬洋平，木村徹，木曽良明：水溶性プロドラッグ．化学工業，53 (6), 465-471 (2002). Youhei Sohma, Tooru Kimura, Yoshiaki Kiso: Water-Soluble Prodrugs. Kagaku Kogyo, 53 (6), 465-471 (2002). 396 S. Rajesh, Ei’ichi Ami, Tomoya Kotake, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso. An expedient synthesis of Nα-protected-L-tetrahydrofuranylglycine and its application in the synthesis of novel substrate based inhibitors of HIV-1 protease. Bioorg. Med. Chem. Lett., 12 (24), 3615-3617 (2002). 397 Hamdy M. Abdel-Rahman, Gamal S. Alkaramany, Nawal A. El-Koussi, Adel F. Youssef, Yoshiaki Kiso. HIV protease inhibitors: Peptidomimetic drugs and future perspectives. Curr. Med. Chem. 9(21), 1905-1922 (2002). 398 Kenichi Akaji, Yoshiaki Kiso. Synthesis of cystine peptide. Methods of Organic Chemistry (Houben-Weyl) Vol.E22b, Synthesis of Peptides and Peptidomimetics, Georg Thieme Verlag, 101-141 (2002). 399 後藤俊幸，河野武弘，森田智津子，中野隆史，Sharad Mohan, 松本光，木村徹，木曽良明，佐野浩一：逆転写酵素阻害剤とプロテアーゼ阻害剤を結合させた新しいプロドラッグ(Double drug) KNI-1039の作用機序．Minophagen Medical Review, 47 (2), 87-88 (2002). Toshiyuki Goto, Takehiro Kohno, Chizuko Morita, Takafumi Nakano, Sharad Mohan, Hikaru Matsumoto, Tooru Kimura, Yoshiaki Kiso, Kouichi Sano: Action Mechanism of New Type Prodrug (Double Drug) KNI-1039 of HIV Protease Inhibitors Conjugated with Reverse Transcriptase and Protease Inhibitors. Minophagen Medical Review, 47 (2), 87-88 (2002). 400 Yoshiaki Kiso, Tooru Kimura: Development of New Methods in Peptide Synthesis. My Favorite Organic Synthesis (K. Tatsuta et al., Eds.)(The Society of Synthetic Organic Chemistry, Japan) p74-75 (2002). 401 Hikoichiro Maegawa, Tooru Kimura, Yasuhiro Arii, Yasuko Matsui, Yoshio Hayashi, Yoshiaki Kiso: Identification of peptidomimetic HTLV-1 protease inhibitors containing allophenylnorstatine as a transition-state isostere. PEPTIDES 2002, E. Benedetti, C. Pedone Eds. Edizioni Ziino, Napoli Italy, pp548-549 (2002) 402 Youhei Sohma, Hikaru Matsumoto, Masato Saasaki, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Spontaneously regenerable water-soluble prodrugs: application to HIV protease inhibitors and anti-cancer drug paclitaxel. PEPTIDES 2002, E. Benedetti, C. Pedone Eds. Edizioni Ziino, Napoli Italy, pp612-613 (2002) 403 Koushi Hidaka, Tooru Kimura, Yoshio Hayashi, Keith F. McDaniel, Tatyana Dekhtyar, Lynn Colletti, Yoshiaki Kiso: Design and synthesis of pseudo-symmetric HIV protease inhibitors containing a novel hydroxymethylcarbonyl (HMC)-hydrazide isostere. Bioorg. Med. Chem. Lett., 13(1), 93-96 (2003). 404 林良雄，木曽良明：プロテアーゼインヒビター．ファルマシア，39(1), 33-37 (2003). Yoshio Hayashi, Yoshiaki Kiso: Protease Inhibitors. Farumashia, 39(1), 33-37 (2003). 405 Youhei Sohma, Yoshio Hayashi, Tomoko Ito, Hikaru Matsumoto, Tooru Kimura, Yoshiaki Kiso: Development of spontaneously regenerable water-soluble prodrugs based on the peptide chemistry: Importance of drug release time for the improvement of gastrointestinal absorption. Peptide Science 2002, T. Yamada ed, The Japanese Peptide Society, 81-84 (2003). 406 S. Rajesh, Ei’ichi Ami, Tomoya Kotake, Hiroko Tsukamoto, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Development of a new synthetic method for L-tetrahydrofuranylglycine and its application for substrate-based HIV-1 protease inhibitors. Peptide Science 2002, T. Yamada ed, The Japanese Peptide Society, 151-152 (2003). 407 Yoshio Hamada, Jun Ohtake, Youhei Sohma, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Structure-migration rate relationship of water-soluble prodrugs of HIV-1 protease inhibitors based on O®N intramolecular acyl migration. Peptide Science 2002, T. Yamada ed, The Japanese Peptide Society, 291-294 (2003). 408 Yoshio Hayashi, Chintala V. Ramesh, Miyako Okamoto, Yasuko Matsui, Saeko Shibakawa, Koushi Hidaka, Tooru Kimura, Yoshiaki Kiso: An approach for peptidic aspartic protease inhibitors using Ala-containing oligopeptides independent of the substrate sequence. Peptide Science 2002, T. Yamada ed, The Japanese Peptide Society, 295-296 (2003). 409 Aiko Kiso, Koushi Hidaka, Tooru Kimura, Yoshio Hayashi, Azin Nezami, Ernesto Freire, Yoshiaki Kiso: Substrate transition-state analogue inhibitors of plasmepsin II as antimalarial drugs. Peptide Science 2002, T. Yamada ed, The Japanese Peptide Society, 297-300 (2003). 410 Yoshio Hamada, Hikaru Matsumoto, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Effect of the acyl groups on O→N acyl migration in the water-soluble prodrugs of HIV-1 protease inhibitor. Bioorg. Med. Chem. Lett., 13 (16) 2727-2730 (2003). 411 Azin Nezami, Tooru Kimura, Koushi Hidaka, Aiko Kiso, Jun Liu, Yoshiaki Kiso, D. E. Goldberg, Ernesto Freire: High affinity inhibition of a family of Plasmodium falciparum proteases by a designed adaptive inhibitor. Biochemistry, 42 (28), 8459-8464 (2003). 412 Y. Kiso, S. Kasai, D. Shuto, P. Liu, S. Rajesh, T. Kotake, K. Hidaka, T. Hamada, S. Shibakawa, T. Kimura, Y. Hayashi: Design and synthesis of substrate-based ß-secretase inhibitors. Biopolymers, 71 (3), 290 (2003) 413 Yoshio Hayashi, Mariusz Skwarczynski, Yoshio Hamada, Youhei Sohma, Tooru Kimura, Yoshiaki Kiso: A novel approach of water-soluble paclitaxel prodrug with no auxiliary and no byproduct: Design and synthesis of isotaxel. J. Med. Chem., 46 (18), 3782-3784 (2003). 414 Youhei Sohma, Yoshio Hayashi, Tomoko Ito, Hikaru Matsumoto, Tooru Kimura, Yoshiaki Kiso: Development of water-soluble prodrugs of the HIV-1 protease inhibitor KNI-727: Importance of the conversion time for higher gastrointestinal absorption of prodrugs based on spontaneous chemical cleavage. J. Med. Chem., 46 (19), 4124-4135 (2003). 415 相馬洋平，木曽良明：抗エイズ薬の現状は？ 化学 58(12), 24-26 (2003) Youhei Sohma, Yoshiaki Kiso: Present Situation of Anti-AIDS Drugs. Kagaku, 58(12), 24-26 (2003) 416 Daisuke Shuto, Soko Kasai, Tooru Kimura, Ping Liu, Koushi Hidaka, Takashi Hamada, Saeko Shibakawa, Yoshio Hayashi, Chinatsu Hattori, Beata Szabo, Shoichi Ishiura, and Yoshiaki Kiso: KMI-008, a novel ß-secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-state mimic: design and synthesis of substrate-based octapeptides. Bioorg. Med. Chem. Lett., 13 (24), 4273-4276 (2003). 417 Mariusz Skwarczynski, Youhei Sohma, Maiko Kimura, Yoshio Hayashi, Tooru Kimura and Yoshiaki Kiso: O-N Intramolecular acyl migration strategy in water-soluble prodrugs of taxoids. Bioorg. Med. Chem. Lett., 13 (24), 4441-4444 (2003). 418 濱田芳男，木曽良明：プロテアーゼインヒビターの設計と新機能．新規治療薬創製のアプローチ．化学と生物41 (12), 796-803 (2003). Yoshio Hamada, Yoshiaki Kiso: Design and New Function of Protease Inhibitors. Approach towards Novel Therapeutic Drug Discovery. Kagaku To Seibutsu, 41 (12), 796-803 (2003). 419 Youhei Sohma, Masato Sasaki, Yoshio Hayashi, Tooru Kimura, and Yoshiaki Kiso: Novel and efficient synthesis of difficult sequence-containing peptides through O-N intramolecular acyl migration reaction of O-acyl isopeptides. Chem. Commun., (1), 124-125 (2004). 420 Yoshio Hamada, Hikaru Matsumoto, Satoshi Yamaguchi, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Water-soluble prodrugs of dipeptide HIV protease inhibitors based on O-N intramolelcular acyl migration: design, synthesis and kinetic study. Bioorg. Med. Chem., 12 (1), 159-170 (2004) 421 木曽良明：平成15年度日本ペプチド学会学会賞を受賞して．PEPTIDE NEWSLETTER JAPAN, No. 51, 1-4 (2004). 422 Tooru Kimura, Daisuke Shuto, Soko Kasai, Ping Liu, Koushi Hidaka, Takashi Hamada, Yoshio Hayashi, Chinatsu Hattori, Masashi Asai, Shinobu Kitazume, Takaomi C. Saido, Shoichi Ishiura, Yoshiaki Kiso. KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine. Bioorg. Med. Chem. Lett., 14 (6), 1527-1531 (2004). 423 木曽良明，長野哲雄：ドラッグデザインの実際．創薬化学（長野哲雄，夏苅英昭，原博，編）pp139-179 (2004) Yoshiaki Kiso, Tetsuo Nagano: Practice of Drug Design. Medicinal Chemistry (T. Nagano, H. Natsugari, H. Hara, Eds) Tokyo Kagaku Dojin, pp139-179 (2004). 424 Yoshiaki Kiso: Medicinal science studies based on synthetic peptide chemistry. Peptide Science 2003, M. Ueki (Ed.), The Japanese Peptide Society, pp 1-4 (2004). 425 Tooru Kimura, Daisuke Shuto, Koushi Hidaka, Soko Kasai, Ping Liu, Hamdy M. Abdel-Rahman, Naoto Igawa, Ayaka Nagamine, Yoshio Hayashi, Chinatsu Hattori, Beata Szabo, Shoichi Ishiura, Yoshiaki Kiso: Design and synthesis of b-secretase inhibitors containing hydroxymethylcarbonyl isostere as a transition state mimic. Peptide Science 2003, M. Ueki (Ed.), The Japanese Peptide Society, pp 69-72 (2004). 426 Yoshio Hayashi, Mariusz Skwarczynski, Yoshio Hamada, Youhei Sohma, Tooru Kimura, Yoshiaki Kiso: Development of new water-soluble prodrugs based on intramolecular nucleophilic reactions in peptide chemistry. Peptide Science 2003, M. Ueki (Ed.), The Japanese Peptide Society, pp 73-76 (2004). 427 Youhei Sohma, Masato Sasaki, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: A novel method for the synthesis of difficult sequence-containing peptides via O-acyl isopeptides: the use of O-N intramolecular acyl migration reaction. Peptide Science 2003, M. Ueki (Ed.), The Japanese Peptide Society, pp 173-176 (2004). 428 Aiko Kiso, Koushi Hidaka, Yumi Tsuchiya, Tooru Kimura, Yoshio Hayashi, Azin Nezami, Jun Liu, Daniel E. Goldberg, Ernesto Freire, Yoshiaki Kiso: Dipeptide-type inhibitors targeting plasmepsins from Plasmodium falciparum. Peptide Science 2003, M. Ueki (Ed.), The Japanese Peptide Society, pp 235-238 (2004). 429 Tooru Kimura, Koushi Hidaka, Hamdy M. Abdel-Rahman, Hikaru Matsumoto, Yoshiaki Tanaka, Yasuko Matsui, Yoshio Hayashi, Yoshiaki Kiso: Design and synthesis of dipeptide-type HIV-1 protease inhibitors with high antiviral activity. Peptide Science 2003, M. Ueki (Ed.), The Japanese Peptide Society, pp 241-244 (2004). 430 Tomoya Kotake, S. Rajesh, Yoshio Hayashi, Yoshie Mukai, Mitsuhiro Ueda, Tooru Kimura, and Yoshiaki Kiso: A new polymer-supported Evans-type chiral auxiliary derived from a-hydroxy-ß-amino acid, phenylnorstatine: Synthesis and application in solid-phase asymmetric alkylation reactions. Tetrahedron Letters, 45 (18), 3651-3654 (2004). 431 木曽良明：セクレターゼ阻害剤の開発について．第125回日本医学会シンポジウム記録集「アルツハイマー病」p61-67 (2004) Yoshiaki Kiso: Development of Secretase Inhibitors. Proceedings of 125th Japanese Association of Medical Science Symposium “Alzheimer’s Disease”. pp61-67 (2004). 432 Sonia Vega, Lin-Woo Kang, Adrian Velazquez-Campoy, Yoshiaki Kiso, Mario Amzel, and Ernesto Freire: A structural and thermodynamic escape mechanism from a drug resistant mutation of the HIV-1 protease. Proteins: Str., Funct. & Bioinformatics, 55 (3), 594-602 (2004). 433 Youhei Sohma, Masato Sasaki, Yoshio Hayashi, Tooru Kimura, Yoshiaki Kiso: Design and synthesis of a novel water-soluble Aß 1-42 isopeptide: an efficient strategy for the preparation of Alzheimer’s disease-related peptide, Aß1-42, via O-N intramolecular acyl migration reaction. Tetrahedron Letters, 45 (31), 5965-5968 (2004). 434 Mitsunobu Doi, Tooru Kimura, Toshimasa Ishida, Yoshiaki Kiso: Rigid backbone moiety of KNI-272, a highly selective HIV protease inhibitor: methanol, acetone and dimethylsulfoxide solvated forms of 3-[3-benzyl-2-hydroxy-9-(isoquinolin-5-yloxy)-6-methylsulfanylmethyl-5,8-dioxo-4,7-diazanonanoyl]-N-tert-butyl-1,3-thiazolidine-4-carboxamide. Acta Crystallographica Sect. B., B60 (4), 433-437 (2004). 435 Youhei Sohma, Yoshio Hayashi, Mariusz Skwarczynski, Yoshio Hamada, Masato Sasaki, Tooru Kimura, Yoshiaki Kiso: O-N Intramolecular acyl migration reaction in the development of prodrugs and the synthesis of difficult sequence-containing bioactive peptides. Biopolymers, 76 (4), 344-356 (2004). 436 Hikoichiro Maegawa, Tooru Kimura, Yasuhiro Arii, Yasuko Matsui, Soko Kasai, Yoshio Hayashi, Yoshiaki Kiso: Identification of peptidomimetic HTLV-1 protease inhibitors containing hydroxymethylcarbonyl (HMC) isostere as the transition-state mimic. Bioorg. Med. Chem. Lett., 14 (23), 5925-5929 (2004). 437 Aiko Kiso, Koushi Hidaka, Tooru Kimura, Yoshio Hayashi, Azin Nezami, Ernesto Freire, Yoshiaki Kiso: Search for substrate-based inhibitors fitting the S2’ space of malarial aspartic protease plasmepsin II. J. Peptide Sci., 10 (11), 641-647 (2004) 438 Hamdy M. Abdel-Rahman, Tooru Kimura, Koushi Hidaka, Aiko Kiso, Azin Nezami, Ernesto Freire, Yoshio Hayashi, Yoshiaki Kiso: Design of inhibitors against HIV, HTLV-I, and Plasmodium falciparum aspartic proteases. Biological Chemistry, 385 (11), 1035-1039 (2004). 439 Hamdy M. Abdel-Rahman, Nawal A. El-Koussi, Gamal S. Alkaramany, Adel F. Youssef, Yoshiaki Kiso: A novel dipeptide-based HIV protease inhibitor containing allophenylnorstatine. Arch. Pharm. Pharm. Med. Chem. 337 (11), 587-598 (2004). 440 木曽良明，木村徹：統合創薬の開拓−生物分子基盤の革新的難病治療薬の創製−月刊OHM，(12)12-13 (2004). Yoshiaki Kiso, Tooru Kimura: Integrated drug discovery - Biomolecule-based innovative drug discovery for difficult diseases. OHM, (12), 12-13 (2004) 441 Tooru Kimura, Daisuke Shuto Yoshio Hamada, Naoto Igawa, Soko Kasai, Ping Liu, Koushi Hidaka, Takashi Hamada, Yoshio Hayashi, Yoshiaki Kiso: Design and synthesis of highly active Alzheimer’s ß-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability. Bioorg. Med. Chem. Lett., 15 (1), 211-215 (2005). 442 木曽良明、林良雄、日高興士：統合創薬を開拓する．MED CHEM NEWS 15(1), 11-14 (2005). 2005.2 443 Youhei Sohma, Yoshio Hayashi, Yousuke Chiyomori, Maiko Kimura, Masato Sasaki, Atsuhiko Taniguchi, Fukue Fukao, Tooru Kimura, Yoshiaki Kiso: “O-acyl isopeptide method” for the synthesis of difficult sequence-containing peptides: application to the synthesis of amyloid ß peptide (Aß) 1-42. Peptide Science 2004, Y. Shimohigashi (Ed.), The Japanese Peptide Society, pp 175-178 (2005). 444 Mariusz Skwarczynski, Youhei Sohma, Mayo Noguchi, Maiko Kimura, Yoshio Hayashi, Yoshio Hamada, Tooru Kimura, Yoshiaki Kiso: O-N Intramolecular acyl and acyloxy migration reaction in the development of water-soluble prodrugs of taxoids. Peptide Science 2004, Y. Shimohigashi (Ed.), The Japanese Peptide Society, pp 309-312 (2005). 445 Yoshio Hayashi, Benjamin Nicholson, Koji Tanaka, Akiko Oda, G. Kenneth Lloyd, Miki Akamatsu, Michael A. Palladino, Yoshiaki Kiso: Effect of the phenyl ring modification on the antitumor activity of anti-microtubule agent dehydrophenylahistin. Peptide Science 2004, Y. Shimohigashi (Ed.), The Japanese Peptide Society, pp 405-406 (2005). 446 Yumi Tsuchiya, Koushi Hidaka, Aiko Kiso, Tooru Kimura, Yoshio Hayashi, Azin Nezami, Ernesto Freire, Yoshiaki Kiso: Evaluation of peptidomimetic inhibitors against malarial protease plasmepsin. Peptide Science 2004, Y. Shimohigashi (Ed.), The Japanese Peptide Society, pp 527-530 (2005). 447 Yoshio Hamada, Tooru Kimura, Daisuke Shuto, Naoto Igawa, Soko Kasai, Ping Liu, Koushi Hidaka, Takashi Hamada, Yoshio Hayashi, Yoshiaki Kiso: Design and synthesis of highly active ß-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability. Peptide Science 2004, Y. Shimohigashi (Ed.), The Japanese Peptide Society, pp 541-544 (2005). 448 Tomoya Kotake, Yoshio Hayashi, Yuka Takiguchi, Tooru Kimura, Yoshiaki Kiso: Conversion of polymer-bound dipeptide to Evans-type chiral auxiliary: a new tool for efficient solid-phase asymmetric reactions. Peptide Science 2004, Y. Shimohigashi (Ed.), The Japanese Peptide Society, pp 629-632 (2005). 449 Panasda Isarangkura N.A., Gui-Mei Li, Jiranan Warachit, Yukie Iwabu, Shoutaro Tsuji, Wattana Auwanit, Daisuke Yamamoto, Toshiyuki Goto, Yoshio Hayashi, Yoshiaki Kiso and Kazuyoshi Ikuta: Different susceptibility of human immunodeficiency virus type 1 to Env gp41-derived synthetic peptides corresponding to the C-terminal heptad repeat region. Microbes & Infection, 7 (3), 356-364 (2005).2005.3 450 Tomoya Kotake, Yoshio Hayashi, S. Rajesh, Yoshie Mukai, Yuka Takiguchi, Tooru Kimrua, Yoshiaki Kiso: Design and synthesis of a new polymer-supported Evans-type oxazolidinone: an efficient chiral auxiliary in the solid-phase asymmetric alkylation reactions. Tetrahedron, 61 (15) 3819-3833 (2005).2005.4.11. 451 Mariusz Skwarczynski, Youhei Sohma, Mayo Noguchi, Maiko Kimura, Yoshio Hayashi, Yoshio Hamada, Tooru Kimura, Yoshiaki Kiso: No auxiliary, no byproduct strategy for water-soluble prodrugs of taxoids: scope and limitation of O-N intramolelcular acyl and acyloxy migration reaction. J. Med. Chem. 48 (7), 2655-2666 (2005).2005.4.7. 452 林良雄，木曽良明：α−ヒドロキシ−β−アミノ酸を基盤とした有機化学・創薬化学研究．有機合成化学協会誌，63(6), 640-651 (2005). Yoshio Hayashi, Yoshiaki Kiso: Organic chemistry and medicinal chemistry research based on a-hydroxy-b-amino acids. J. Syn. Org. Chem. Jpn., 63 (6), 640-651 (2005). 453 Akiko Yoshida, Ahmad Piroozmand, Akiko Sakurai, Mikako Fujita, Tsuneo Uchiyama, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso, Akio Adachi: Establishment of a biological assay system for human retroviral protease activity. Microbes and Infection, 7(5/6), 820-824 (2005). 2005.5. 454 Youhei Sohma, Yoshio Hayashi, Maiko Kimura, Yousuke Chiyomori, Atsuhiko Taniguchi, Masato Sasaki, Tooru Kimura, Yoshiaki Kiso: The ‘O-acyl isopeptide method’ for the synthesis of difficult sequence-containing peptides: application to the synthesis of Alzheimer’s disease-related amyloid ß-peptide (Aß) 1-42. J. Peptide Sci.,11(8), 441-451 (2005). 455 木曽良明：アミロイド生成阻害薬開発の展望．第19回「大学と科学」公開シンポジウム講演収録集:アルツハイマー病：治療の可能性を探る，pp160-172，クバプロ(2005). Yoshiaki Kiso: Scope of development of amyloid formation inhibiting drugs. Proceedings of the 19th University and Science Open Symposium “Alzheimer’s Disease: Searching for Remedies”, pp160-172 (2005). 456 Hamdy M. Abdel-Rahman, Nawal A. El-Koussi, Gamal S. Alkaramany, Adel Youssef, Yoshiaki Kiso: Allophenylnorstatine-containing HIV-1 protease inhibitors: design, synthesis and structure-activity relationships for selected P2 ligands. Bull. Pharm. Sci., Assiut Univ., 28 (1), 95-103 (2005). 457 Youhei Sohma, Yousuke Chiyomori, Maiko Kimura, Fukue Fukao, Atsuhiko Taniguchi, Yoshio Hayashi, Tooru Kimura and Yoshiaki Kiso: “O-Acyl isopeptide method” for the efficient preparation of amyloid b peptide (Ab) 1-42 mutants. Bioorg. Med. Chem., 13 (22), 6167-6174 (2005). 458 Sharad Mohan, Toshiyuki Goto, Takehiro Kohno, Takashi Nakano, Fumie Harada, Yoshiaki Kiso, Sinji Yoshioka, Kouichi Sano: Evidence for the cellular uptake of anti-HIV-1 double drug KNI-1039. Bull. Osaka Med. Coll. 51 (2), 50-60 (2005) 459 Yoshiaki Kiso: Design of peptidomimetic inhibitors of aspartic proteases: prodrug forms and their application. in Peptides: Biology & Chemistry, Proc. 2004 Chinese Peptide Symp. (Ed. Ke-Liang Liu, James P. Tam), Science Press USA, pp3-7 (2005). 460 Tomoya Kotake, Yoshio Hayashi, S. Rajesh, Tooru Kimura, Yoshiaki Kiso: Development of Wang resin supported Evans-type oxazolidinone for asymmetric reaction. in Understanding Biology Using Peptides (Sylvie E. Blondelle Ed.) American Peptide Society, 96-97 (2005). 461 Yoshio hayashi, Akiko Oda, Yuri Yamazaki, Yuka Okuno, Yoshiaki Kiso: A convenient synthetic method for monodehydro-2,5-diketopiperazines. in Understanding Biology Using Peptides (Sylvie E. Blondelle Ed.) American Peptide Society, 98-99 (2005). 462 Youhei Sohma, Maiko Kimura, Yousuke Chiyomori, Yoshio Hayashi, Atsuhiko Taniguchi, Masato Sasaki, Tooru Kimura, Yoshiaki Kiso: The “O-acyl isopeptide method” for the synthesis of Alzheimer’s disease-related amyloid ß peptide (Aß) 1-42. in Understanding Biology Using Peptides (Sylvie E. Blondelle Ed.) American Peptide Society, 104-105 (2005). 463 Yousuke Chiyomori, Youhei Sohma, Maiko Kimura, Yoshio Hayashi, Fukue Fukao, Atsuhiko Taniguchi, Tooru Kimura, Yoshiaki Kiso: The “O-acyl isopeptide method” for the synthesis of difficult sequence-containing peptides: application to the synthesis of Alzheimer’s disease-related amyloid ß peptide (Aß) 1-42 mutants. in Understanding Biology Using Peptides (Sylvie E. Blondelle Ed.) American Peptide Society, 106-107 (2005). 464 Koushi Hidaka, Tooru Kimura, Yumi Tsuchiya, Aiko Kiso, Yoshio Hayshi, Azin Nezami, Ernesto Freire, Yoshiaki Kiso: Evaluation of malarial protease plasmepsin inhibitors containing hydroxymethylcarbonyl isostere. in Understanding Biology Using Peptides (Sylvie E. Blondelle Ed.) American Peptide Society, 597-598 (2005). 465 Yoshio Hamada, Daisuke Shuto, Naoto Igawa, Soko Kasai, Ping Liu, Koushi Hidaka, Tooru Kimura, Yoshio Hayashi, Shoichi Ishiura, Yoshiaki Kiso: Design and synthesis of ß-secretase inhibitors: optimization at the P4 and P1’ positions. in Understanding Biology Using Peptides (Sylvie E. Blondelle Ed.) American Peptide Society, 599-600 (2005). 466 Benjamin Nicholson, G. Kenneth Lloyd, Brian R. Miller, Michael A. Palladino, Yoshiaki Kiso, Yoshio Hayashi, Saskia T. C. Neulteboom: NPI-2358 is a tubulin-depolymerizing agent: in-vitro evidence for activity as a tumor vascular-disrupting agent. Anti-Cancer Drugs, 17(1), 25-31 (2006). 467 Masashi Asai, Chinatsu Hattori, Nobuhisa Iwata, Takaomi C. Saido, Noboru Sasagawa, Beata Szabo, Yasuhiro Hashimoto, Kei Maruyama, Sei-ichi Tanuma, Yoshiaki Kiso, Shoichi Ishiura: The novel ß-secretase inhibitor KMI-429 reduces amyloid ß peptide production in amyloid precursor protein transgenic and wild-type mice J. Neurochem., 96(2), 533-540 (2006). 468 Adam J. Ruben, Yoshiaki Kiso, Ernesto Freire: Overcoming roadblocks in lead optimization: a thermodynamic perspective. Chem. Biol. Drug. Des., 67 (1) 2-4 (2006) 469 Atsuhiko Taniguchi, Youhei Sohma, Maiko Kimura, Takuma Okada, Keisuke Ikeda, Yoshio Hayashi, Tooru Kimura, Shun Hirota, Katsumi Matsuzaki, Yoshiaki Kiso: “Click peptide” based on the “O-acyl isopeptide method”: control of Aß1-42 production from a photo-triggered Aß1-42 analogue. J. Am. Chem. Soc., 128 (3), 696-697 (2006). 470 木曽良明：統合創薬の開拓．BIO Clinica, 21 (3), 216-218 (2006). Yoshiaki Kiso: Integrated Drug Discovery. BIO Clinica, 21 (3), 216-218 (2006). 471 Jose Clemente, Lakshmanan Govindasamy, Amrita Madabushia, S. Zo Fisher, Rebecca E. Moose, Charles A Yowell, Koushi Hidaka, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso, Mavis Agbandje-McKenna, John B. Dame, Ben M. Dunn, Robert McKenna: X-ray crystal structure of the aspartic protease plasmepsin 4 from the malarial parasite Plasmodium malariae bound to an allophenylnorstatine based inhibitor. Acta Crystallographica, D, 62(3), 246-252 (2006). 472 Mariusz Skwarczynski, Youhei Sohma, Mayo Noguchi, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: O-N Intramolecular acyloxy migration of typical protective groups in hydroxyamino acids. J. Org. Chem., 71 (6), 2542-2545 (2006). 473 Zyta Ziora, Tooru Kimura and Yoshiaki Kiso, Small-sized BACE1 inhibitors. Drugs of the Future, 31 (1), 53-63 (2006). 474 石浦章一，木曽良明：アルツハイマー病の治療薬をつくる．日経サイエンス，36 (4), 64-69 (2006). Shoichi Ishiura, Yoshiaki Kiso: Making therapeutic drugs for Alzheimer’s disease. Nikkei Science, 36 (4), 64-69 (2006). 475 Youhei Sohma, Atsuhiko Taniguchi, Mariusz Skwarczynski, Taku Yoshiya, Fukue Fukao, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: “O-Acyl isopeptide method” for the efficient synthesis of difficult sequence-containing peptides: use of “O-acyl isodipeptide unit”. Tetrahedron Letters, 47 (18), 3013-3017 (2006). 476 Tooru Kimura, Yoshio Hamada, Monika Stochaj, Hayato Ikari, Ayaka Nagamine, Hamdy Abdel-Rahman, Naoto Igawa, Koushi Hidaka, Jeffrey-Tri Nguyen, Kazuki Saito, Yoshio Hayashi, Yoshiaki Kiso: Design and synthesis of potent ß-secretase (BACE1) inhibitors with P1’ carboxylic acid bioisosteres. Bioorg. Med. Chem. Lett., 16 (9), 2380-2386 (2006).2006.5 477 日高興士，木曽良明：今エイズ薬研究はどうなっているか．化学，61 (5), 25-29 (2006) Koushi Hidaka, Yoshiaki Kiso: Current status of AIDS drug research. Kagaku, 61 (5), 25-29 (2006) 478 Youhei Sohma, Atsuhiko Taniguchi, Maiko Kimura, Yousuke Chiyomori, Fukue Fukao, Takuma Okada, Keisuke Ikeda, Yoshio Hayashi, Tooru Kimura, Shun Hirota, Katsumi Matsuzaki, Yoshiaki Kiso: “Click peptide” based on the “O-acyl isopeptide method”: development of chemical biology-oriented Alzheimer’s disease-related Aß1-42 analogues. Peptide Science 2005, 25-28 (2006). 479 Yoshio Hayashi, Yuri Yamazaki, Akiko Oda, Yuka Okuno, Yoshiaki Kiso: Development of a new synthetic method for monodehydro-2,5-diketopiperazines. Peptide Science 2005, 149-150 (2006). 480 Yousuke Chiyomori, Youhei Sohma, Maiko Kimura, Atsuhiko Taniguchi, Fukue Fukao, Yoshio Hayashi, Tooru Kimura, Yoshiaki Kiso: “Click peptide” based on the “O-acyl isopeptide method”: an efficient preparation of amyloid ß peptide 1-42 mutants. Peptide Science 2005, 151-154 (2006). 481 Mariusz Skwarczynski, Youhei Sohma, Mayo Noguchi, Maiko Kimura, Yoshio Hayashi, Yoshio Hamada, Tooru Kimura, Yoshiaki Kiso: O-N intramolecular acyloxy migration reaction: from the prodrug strategy to the migration of protective groups in amino acids. Peptide Science 2005, 169-172 (2006). 482 Ayako Itami, Hikoichiro Maegawa, Keiji Nishiyama, Koushi Hidaka, Yasuhiro Arii, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Evaluation of peptidomimetic HTLV-1 protease inhibitors containing hydroxymethylcarbonyl as a transition-state isostere. Peptide Science 2005, 237-240 (2006). 483 Yoshio Hamada, Monika Stochaj, Hayato Ikari, Ayaka Nagamine, Hamdy Abdel-Rahman, Naoto Igawa, Koushi Hidaka, Tooru Kimura, Yoshio Hayashi, Shoichi Ishiura, Yoshiaki Kiso: Design of ß-secretase (BACE1) inhibitors with carboxylic acid bioisosteres. Peptide Science 2005, 309-312 (2006). 484 Zyta Ziora, Daisuke Shuto, Soko Kasai, Ping Liu, Koushi Hidaka, Naoto Igawa, Ayaka Nagamine, Monika Stochaj, Takashi Hamada, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Modification of P4 position in ß-secretase (BACE1) inhibitors containing phenylnorstatine. Peptide Science 2005, 321-324 (2006). 485 Yoshio Hamada, Naoto Igawa, Hayato Ikari, Zyta Ziora, Jeffrey-Tri Nguyen, Abdellah Yamani, Koushi Hidaka, Tooru Kimura, Kazuki Saito, Yoshio Hayashi, Maiko Ebina, Shoichi Ishiura, Yoshiaki Kiso: ß-Secretase inhibitors: Modification at the P4 position and improvement of inhibitory activity in cultured cell. Bioorg. Med. Chem. Lett., 16 (16), 4354-4359 (2006). 486 Mariusz Skwarczynski, Mayo Noguchi, Shun Hirota, Youhei Sohma, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Development of first photoresponsive prodrug of paclitaxel. Bioorg. Med. Chem. Lett., 16 (17), 4492-4496 (2006). 487 Magne O. Sydnes, Yoshio Hayashi, Vinay K. Sharma, Takashi Hamda, Usman Bacha, Jennifer Barrila, Ernesto Freire, Yoshiaki Kiso: Synthesis of glutamic acid and glutamine peptides possessing a trifluoromethyl ketone group as SARS-CoV 3CL protease inhibitors. Tetrahedron, 62 (36), 8601-8609 (2006). 488 Taku Yoshiya, Youhei Sohma, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: “O-Acyl isopeptide method”: racemization-free segment condensation in solid phase peptide synthesis. Tetrahedron Letters, 47(45), 7905-7909 (2006). 489 Youhei Sohma, Yoshiaki Kiso: “Click peptide”: Chemical biology-oriented synthesis of Alzheimer’s disease-related amyloid ß peptide (Aß) analogues based on the “O-acyl isopeptide method”. ChemBioChem., 7(10), 1549-1557 (2006). 490 Masatoshi Inden, Takahiro Taira, Yoshihisa Kitamura, Takashi Yanagida, Daiju Tsuchiya, kazuyuki Takata, Daijiro Yanagisawa, Kaneyasu Nishimura, Takashi Taniguchi, Yoshiaki Kiso, Kanji Yoshimoto, Tomohiro Agatsuma, Shizuyo Koide-Yoshida, Sanae M. m. Iguchi-Ariga, Shun Shimoharam Hiroyoshi Ariga: PARK7 DJ-1 protects against degeneration of nigral dopaminergic neurons in Parkinson’s disease rat model. Neurobiology of Disease, 24(1), 144-158 (2006). 491 Jeffrey-Tri Nguyen, Abdellah Yamani and Yoshiaki Kiso: Views on amyloid hypothesis and secretase inhibitors for treating Alzheimer’s disease: Progress and problems. Current Pharmaceutical Design, 12 (33), 4295-4312 (2006). 492 Youhei Sohma, Atsuhiko Taniguchi, Taku Yoshiya, Yousuke Chiyomori, Fukue Fukao, Setsuko Nakamura, Mariusz Skwarczynski, Takuma Okada, Keisuke Ikeda, Yoshio Hayashi, Tooru Kimura, Shun Hirota, Katsumi Matsuzaki, Yoshiaki Kiso: “Click peptide”: a novel “O-acyl isopeptide method” for peptide synthesis and chemical biology-oriented synthesis of amyloid ß peptide analogues. J. Peptide Science, 12 (12), 823-828 (2006). 493 Mariusz Skwarczynski, Yoshio Hayashi, Yoshiaki Kiso: Paclitaxel prodrugs: toward smarter delivery of anticancer agents. J. Med. Chem.,49 (25), 7253-7269 (2006). 494 Mariusz Skwarczynski, Mayo Noguchi, Youhei Sohma, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Application of intramolecular carbonate-carbamate migration. Chemistry Today, 24 (6), 30-32 (2006). 495 Atsuhiko Taniguchi, Youhei Sohma, Taku Yoshiya, Fukue Fukao, Setsuko Nakamura, Yousuke Chiyomori, Yoshio Hayashi, Tooru Kimura, Shun Hirota, Katasumi Matsuzaki, Yoshiaki Kiso: “Click peptide”: the “O-acyl isopeptide method” for peptide synthesis and development of chemical biology-oriented Aß analogues. Peptide Science 2006, 6-7 (2006) 496 Taku Yoshiya, Youhei Sohma, Fukue Fukao, Atsuhiko Taniguchi, Setsuko Nakamura, Mariusz Skwarczynski, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Development of racemization-free “O-acyl isopeptide method” utilizing the “O-acyl isodipeptide unit”. Peptide Science 2006, 43-44 (2006) 497 Yoshio Hayashi, Kentaro Takayama, Yuka Suehisa, Takuya Fujita, Akira Yamamoto, Shiroh Futaki, Yoshiaki Kiso: Design and synthesis of oligoarginine-fluorescein conjugates possessing novel self-cleavable spacers as a model for effective intestinal absorption. Peptide Science 2006, 116 (2006) 498 Mami Kamiya, Koushi Hidaka, Yumi Tsuchiya, Tooru Kimura, Yoshio Hayashi, Adam J. Ruben, Ernesto Freire, Yoshiaki Kiso: Tripeptide mimetics with potent inhibitory activity against malarial aspartic protease plasmepsin II. Peptide Science 2006, 157-158 (2006) 499 Yoshio Hayashi, Yuri Yamazaki, Kyoto Kohno, Akiko Oda, Koji Tanaka, Saskia Neuteboom, Ana M. Baraal, Benjamin Nicholson, Barbara Potts, G. Kenneth Lloyd, Yoshiaki Kiso: New aspects of potent anti-microtubule agents phenylahistin and tubulin photoaffinity labeling. Peptide Science 2006, 159 (2006) 500 Yoshio Hamada, Hamdy Abdel-Rahman, Abdellah Yamani, Jeffrey-Tri Nguyen, Monika Stochaj, Koushi Hidaka, Tooru Kimura, Yoshio Hayashi, Kazuki Saito, Shoichi Ishiura, Yoshiaki Kiso: Design of BACE1 inhibitors: replacing the P1’ residue with non-acidic moiety. Peptide Science 2006, 235-236 (2006) 501 Zyta Ziora, Soko Kasai, Koushi Hidaka, Ayaka Nagamine, Tooru Kimura, Kazuki Saito, Yoshio Hayashi, Yoshiaki Kiso: phenylthionorstatine as a transition-state mimetic in BACE1 inhibitors. Peptide Science 2006, 237-238 (2006) 502 Mariusz Skwarczynski, Mayo Noguchi, Shun Hirota, Youhei Sohma, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Phototaxel: development of first photoresponsive prodrug of paclitaxel via modification of phenylisoserine moiety. Peptide Science 2006, 251-252 (2006) 503 Miho Tsukuda, Takuma Okada, Masaki Wakabayashi, Youhei Sohma, Yousuke Chiyomori, Yoshio Hayashi, Yoshiaki Kiso, Katsumi Matsuzaki: Inhibition of amyloid ß-protein Aß-(1-42) induced cytotoxicity by helical Aß analog. Peptide Science 2006, 280 (2006) 504 Keisuke Ikeda, Yoshiaki Yano, Masaru Hoshino, Kazuhiro Hasegawa, Hironobu Naiki, Youhei Sohma, Yoshio Hayashi, Yoshiaki Kiso, Katsumi Matsuzaki: Structural analysis of amyloid-ß protein fibrils formed in raft-like model membranes. Peptide Science 2006, 281 (2006) 505 Yuka Suehisa, Kentaro Takayama, Mamiko Hayashi, Shiroh Futaki, Akira Yamamoto, Yoshio Hayashi, Yoshiaki Kiso, Takuya Fujita: Uptake mechanisms of FITC-oligoarginine conjugates in HeLa cells. Peptide Science 2006, 366 (2006) 506 Zyta Ziora, Soko Kasai, Koushi Hidaka, Ayaka Nagamine, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Design and synthesis of BACE1 inhibitors containing a novel norstatine derivative (2R, 3R)-3-amino-2-hydroxy-4-(phenylthio)butyric acid. Bioorg. Med. Chem. Lett., 17 (6), 1629-1633 (2007). 507 Youhei Sohma, Taku Yoshiya, Atsuhiko Taniguchi, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Development of “O-Acyl Isopeptide Method”. Biopolymers Peptide Science, 88(2), 253-262 (2007). 508 Koushi Hidaka, Tooru Kimura, Yumi Tsuchiya, Mami Kamiya, Adam J. Ruben, Ernesto Freire, Yoshio Hayashi and Yoshiaki Kiso: Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. Bioorg. Med. Chem. Lett., 17 (11), 3048-3052 (2007). 509 Taku Yoshiya, Atsuhiko Taniguchi, Youhei Sohma, Fukue Fukao, Setsuko Nakamura, Naoko Abe, Nui Ito, Mariusz Skwarczynski, Tooru Kimura, Yoshio Hayashi and Yoshiaki Kiso: “O-Acyl isopeptide method” for peptide synthesis: synthesis of forty kinds of “O-acyl isodipeptide unit” Boc-Ser/Thr(Fmoc-Xaa)-OH. Org. Biomol. Chem. 5 (11), 1720-1730 (2007). 510 Tooru Kimura, Jeffrey-Tri Nguyen, Hikoichiro Maegawa, Keiji Nishiyama, Yasuhiro Arii, Yasuko Matsui, Yoshio Hayashi and Yoshiaki Kiso: Chipping at large, potent human T-cell leukemia virus type 1 protease inhibitors to uncover smaller, equipotent inhibitors. Bioorg. Med. Chem. Lett., 17 (12), 3276-3280 (2007). 511 Virginie Lafont, Anthony A. Armstrong, Hiroyasu Ohtaka, Yoshiaki Kiso, L. Mario Amzel, Ernesto Freire: Compensating enthalpic and entropic changes hinder binding affinity optimization. Chemical Biology & Drug Design, 69 (6), 413-422 (2007). 512 Ei’ichi Ami, Koichiro Nakahara, Akihiko Sato, Jeffrey-Tri Nguyen, Koushi Hidaka, Yoshio Hamada, Shingo Nakatani, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating D-cysteine derivatives as P2/P3 moieties. Bioorg. Med. Chem. Lett., 17 (15), 4213-4217 (2007). 513 木曽良明、濱田芳男：プロテアーゼインヒビターからの創薬．遺伝子医学MOOK, 8「ペプチドと創薬」193-199 (2007). Yoshiaki Kiso, Yoshio Hamada: Drug discovery from protease inhibitors. Idenshi Igaku MOOK, 8 “Peptide and Drug Discovery” 193-199 (2007). 514 木曽良明：アルツハイマー病はどこまで克服されたか−創薬・治療の最前線を聞く．平成19年版 人類とバイオ−知の大競争時代をいかに勝ち抜くか−（東京テクノ・フォーラム２１編）381-402 (2007). 515 木曽良明、日高興士：ペプチドと創薬研究．化学フロンティア１９，創薬をめざす有機合成戦略−進化する医薬品づくり（宍戸宏造、新藤充 編）125-132 (2007). Yoshiaki Kiso, Koushi Hidaka: Peptide and medicinal research. In Kagaku Frontier 19, Organic Synthetic Strategy for Drug Discovery. (Eds. Kozo Shishido, M. Shindo) 125-132 (2007). 516 Yoshio Hayashi, Kentaro Takayama, Yuka Suehisa, Takuya Fujita, Jeffrey-Tri Nguyen, Shiroh Futaki, Akira Yamamoto, Yoshiaki Kiso: Development of oligoarginine-drug conjugates linked to new peptide self-cleavable spacers toward effective intestinal absorption. Bioorg. Med. Chem. Lett., 17 (18), 5129-5132 (2007) 517 濱田芳男、木曽良明：プロテアーゼ阻害剤：蛋白質核酸酵素 増刊号「ケミカルバイオロジー」（長野哲雄、長田裕之、菊地和也、上杉志成編）1702-1707 (2007). Yoshio Hamada, Yoshiaki Kiso: Protease inhibitors. Protein, Nucleic Acid and Enzymes Special Issue: Chemical Biology (Eds by T. Nagano, H. Osada, K. Kikuchi, M. Uesugi) 1702-1707 (2007). 518 山崎有理、林良雄、木曽良明：アビジン-ビオチンアフィニティー科学の先駆け。蛋白質核酸酵素 増刊号「ケミカルバイオロジー」（長野哲雄、長田裕之、菊地和也、上杉志成編）1784-1785 (2007). Yuri Yamazaki, Yoshio Hayashi, Yoshiaki Kiso: Front runner in Avidin-Biotin Affinity Science: An approach to the targeted attachment of peptides and proteins to solid supports. Protein, Nucleic Acid and Enzymes Special Issue: Chemical Biology (Eds by T. Nagano, H. Osada, K. Kikuchi, M. Uesugi) 1784-1785 (2007). 519 Mariusz Skwarczynski, Yoshiaki Kiso: Application of O-N intramolecular acyl migration reaction in medicinal chemistry. Current Medicinal Chemistry, 14 (26). 2813-2823 (2007). 520 Atsuhiko Taniguchi, Taku Yoshiya, Naoko Abe, Fukue Fukao, Youhei Sohma, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: “O-Acyl isopeptide method” for peptide synthesis: Solvent effects in the synthesis of Aß1-42 isopeptide using “O-acyl isodipeptide unit”. J. Peptide Sci., 13 (12), 868-874 (2007). 521 石浦章一、木曽良明：アルツハイマー病の治療薬をつくる。別冊日経サイエンス：脳から見た心の世界part 3. pp.108-113 (2007). 522 Jeffrey-Tri Nguyen, Meihui Zhang, Henri-Obadja Kumada, Ayako Itami, Keiji Nishiyama, Tooru Kimura, Maosheng Cheng, Yoshio Hayashi, Yoshiaki Kiso: Truncation and non-natural amino acid substitution studies on HTLV-I protease hexapeptidic inhibitors. Bioorg. Med. Chem. Lett., 18(1), 366-370 (2008). 523 Taeko Kakizawa, Shizuyo Koide-Yoshida, Tooru Kimura, Hiromasa Uchimura, Yoshio Hayashi, Kazuki Saito, Yoshiaki Kiso: Fmoc-based solid phase chemical synthesis of 71-meric neuroregulin 1-ß1, an epidermal growth factor-like domain. J. Peptide Sci., 14(3), 261-266 (2008). 524 Yoshio Hamada, Hamdy Abdel-Rahman, Abdellah Yamani, Jeffrey-Tri Nguyen, Koushi Hidaka, Tooru Kimura, Yoshio Hayashi, Kazuki Saito, Shoichi Ishiura, Yoshiaki Kiso: BACE1 inhibitors: Optimization by replacing the P1’ residue with non-acidic moiety. Bioorg. Med. Chem. Lett., 18 (5),1649-1653 (2008) 525 Yoshio Hamada, Hiroko Ohta, Naoko Miyamoto, Ryoji Yamaguchi, Abdellah Yamani, Koushi Hidaka, Tooru Kimura, Kazuki Saito, Yoshio Hayashi, Shoichi Ishiura, Yoshiaki Kiso: Novel non-peptidic and small-sized BACE1 inhibitors. Bioorg. Med. Chem. Lett., 18 (5), 1654-1658 (2008). 526 Yoshio Hayashi, Shigenobu Nishiguchi, Daisuke Hashimoto, Magne O. Sydnes, Thomas Regnier, Junya Hasegawa, Takahiro Kato, Tetsuya Kajimoto, Masataka Shiozuka, Ryoichi Matsuda, Manabu Node, Yoshiaki Kiso: Synthesis of negamycin and its derivatives as potential therapeutic agents for Duchenne muscular dystrophy. Peptide Science 2007, S. Aimoto & S. Ono (Eds.), Japanese Peptide Society, pp.163-164 (2008). 527 Naoko Abe, Atsuhiko Taniguchi, Taku Yoshiya, Setsuko Nakamura, Nui Ito, Fukue Fukao, Youhei Sohma, Mariusz Skwarczynski, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: The synthesis of bioactive peptides based on O-acyl isopeptide method: application of O-acyl isodipeptide units. Peptide Science 2007, S. Aimoto & S. Ono (Eds.), Japanese Peptide Society, pp.187-190 (2008). 528 Taku Yoshiya, Youhei Sohma, Yoshio Hamada, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Racemization-free segment condensation based on isopeptide method: an efficient preparation of peptides on solid support. Peptide Science 2007, S. Aimoto & S. Ono (Eds.), Japanese Peptide Society, pp.191-192 (2008). 529 Meihui Zhang, Jeffrey-Tri Nguyen, Henri-Obadja Kumada, Tooru Kimura, Maosheng Cheng, Yoshio Hayashi, Yoshiaki Kiso: Synthesis and activity of tetrapeptidic human T-cell leukemia virus type I protease inhibitors possessing different P1’- and P3-cap moieties. Peptide Science 2007, S. Aimoto & S. Ono (Eds.), Japanese Peptide Society, pp.351-352 (2008). 530 Ryoji Yamaguchi, Yoshio Hamada, Koushi Hidaka, Abdellah Yamani, Jeffrey-Tri Nguyen, Zyta Ziora, Hiroko Ohta, Naoko Miyamoto, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Structure-activity relationship study of BACE1 inhibitors containing chelidonamide. Peptide Science 2007, S. Aimoto & S. Ono (Eds.), Japanese Peptide Society, pp.353-356 (2008). 531 Yoshio Hamada, Ryoji Yamaguchi, Hiroko Ohta, Naoko Miyamoto, Abdellah Yamani, Koushi Hidaka, Henri-Obadja Kumada, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Novel BACE1 inhibitors: design approach focused on inhibitor’s conformer. Peptide Science 2007, S. Aimoto & S. Ono (Eds.), Japanese Peptide Society, pp.357-360 (2008). 532 Hidehito Mukai, Nobuhiko Ueki, Masanori Kawanami, Mayumi Kiyama, Yoshiaki Kiso, Kaori Wakamatsu: Investigation of signaling mechanisms induced by mitocryptides in neurophilic/granulocytic cells. Peptide Science 2007, S. Aimoto & S. Ono (Eds.), Japanese Peptide Society, pp.375-376 (2008). 533 Mayo Noguchi, Mariusz Skwarczynski, Halan Prakash, Shun Hirota, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Development of new photoresponsive paclitaxel prodrug. Peptide Science 2007, S. Aimoto & S. Ono (Eds.), Japanese Peptide Society, pp.493-496 (2008). 534 Mayo Noguchi, Mariusz Skwarczynski, Halan Prakash, Shun Hirota, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Development of novel water-soluble photocleavable protective group and its application for design of tumor-targeting paclitaxel prodrugs. Bioorg. Med. Chem., 16 (10), 5389-5397 (2008). 535 Meihui Zhang, Jeffrey-Tri Nguyen, Henri-Obadja Kumada, Tooru Kimura, Maosheng Cheng, Yoshio Hayashi, and Yoshiaki Kiso: Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties. Bioorg. Med. Chem., 16 (10), 5795-5802 (2008). 536 Shingo Nakatani, Koushi Hidaka, Ei’ichi Ami, Koichiro Nakahara, Akihiko Sato, Jeffrey-Tri Nguyen, Yoshio Hamada, Yasuko Hori, Nobuyuki Ohnishi, Akinori Nagai, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Combination of non-natural D-amino acid derivatives and allophenylnorstatine-dimethylthioproline scaffold in HIV protease inhibitors have high efficacy in Mutant HIV. J. Med. Chem., 51 (10), 2992-3004 (2008). 537 Yoshio Hayashi, Thomas Regnier, Shigenobu Nishiguchi, Magne O. Sydnes, Daisuke Hashimoto, Junya Hasegawa, Takahiro Katoh, Tetsuya Kajimoto, Masataka Shiozuka, Ryoichi Matsuda, Manabu Node, Yoshiaki Kiso: Efficient total synthesis of (+)-negamycin, a potential chemotherapeutic agent for genetic diseases. Chem. Commun., (20), 2379-2381 (2008). 538 Katsumi Matsuzaki, Takuma Okada, Miho Tsukuda; Keisuke Ikeda; Youhei Sohma; Yousuke Chiyomori; Atsuhiko Taniguchi; Setsuko Nakamura; Nui Ito; Yoshio Hayashi; Yoshiaki Kiso: Design, synthesis and biophysical properties of a helical Aß1-42 analog: inhibition of fibrillogenesis and cytotoxicity. Biochem. Biophys. Res. Commun. 371 (4), 777-780 (2008). 539 Usman Bacha, Jennifer Barrila, Sandra B. Gabelli, Yoshiaki Kiso, L. Mario Amzel, Ernesto Freire: Development of broad-spectrum halomethyl ketone inhibitors against coronavirus main protease 3CLpro. Chem. Biol. Drug Design, 72 (7), 34-49 (2008). 540 Meihui Zhang, Jeffrey-Tri Nguyen, Henri-Obadja Kumada, Tooru Kimura, Maosheng Cheng, Yoshio Hayashi, Yoshiaki Kiso: Locking the two ends of tetrapeptidic HTLV-1 protease inhibitors inside the enzyme. Bioorg. Med. Chem., 16(14), 6880-6890 (2008). 541 Hidehito Mukai, Miharu Kikuchi, Shigetomo Fukuhara, Yoshiaki Kiso, Eisuke Munekata: Cryptide signaling: Amphiphilic peptide-induced exocytotic mechanisms in mast cells. Biochem. Biophys. Res. Commun., 375 (1), 22-26 (2008). 542 Jeffrey-Tri Nguyen, Yoshio Hamada, Tooru Kimura, Yoshiaki Kiso: Design of potent aspartic protease inhibitors to treat various diseases. Arch. Pharm. Chem. Life Sci., 341 (9), 523-535 (2008). 543 H. Mukai, Y. Suzuki, Y. Kiso, E. Munekata: Elucidation of structural requirements of mastoparan for mast cell activation – Toward the comprehensive prediction of cryptides acting on mast cells. Protein & Peptide Letters, 15 (9), 931-937 (2008). 544 Hidehito Mukai, Yoshinori Hokari, Tetsuo Seki, Toshifumi Takao, Makoto Kubota, Yuko Matsuo, Hiroyuki Tsukagoshi, Masahiko Kato, Hirokazu Kimura, Yasutsugu Shimonishi, Yoshiaki Kiso, Yoshisuke Nishi, Kaori Wakamatsu, Eisuke Munekata: Discovery of mitocryptide-1, a neutrophil-activating cryptide from healthy porcine heart. J. Biol. Chem. 283 (45), 30596-30605 (2008). 545 Taku Yoshiya, Nui Ito, Tooru Kimura, Yoshiaki Kiso: Isopeptide method: Development of S-acyl isopeptide method for the synthesis of difficult sequence-containing peptides. J. Peptide Science, 14 (11), 1203-1208 (2008). 546 Sebastian D. Kiewitz, Taeko Kakizawa, Yoshiaki Kiso, Chiara Cabrele: Switching from the unfolded to the folded state of the helix-loop-helix domain of the Id proteins based on the O-acyl isopeptide method. J. Peptide Sci., 14 (11), 1209-1215 (2008). 547 Kentaro Takayama, Yuka Suehisa, Takuya Fujita, Jeffrey-Tri Nguyen, Shiroh Futaki, Akira Yamamoto, Yoshiaki Kiso, Yoshio Hayashi: Oligoarginine-based prodrugs with self-cleavable spacers for Caco-2 cell permeation. Chem. Pharm. Bull., 56(11), 1515-1520 (2008). 548 Koushi Hidaka, Tooru Kimura, Adam J. Ruben, Tsuyoshi Uemura, Mami Kamiya, Aiko Kiso, Tetsuya Okamoto, Yumi Tsuchiya, Yoshio Hayashi, Ernesto Freire, Yoshiaki Kiso: Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. Bioorg. Med. Chem., 16(23), 10049-10060 (2008). 549 Atsuhiko Taniguchi, Mariusz Skwarczynski, Youhei Sohma, Takami Nagano, Takuma Okada, Keisuke Ikeda, Halan Prakash, Hidehito Mukai, Yoshio Hayashi, Tooru Kimura, Shun Hirota, Katsumi Matsuzaki, Yoshiaki Kiso: Controlled production of Alzheimer’s amyloid ß peptide from a photo-triggered, water-soluble precursor “click peptide”. ChemBioChem. 9(18), 3055-3065 (2008). 550 Yuri Yamazaki, Kyoko Kohno, Hiroyuki Yasui, Yoshiaki Kiso, Miki Akamatsu, Benjamin Nicholson, Gordafaried Deyanat-Yazdi, Saskia Neuteboom, Barbara Potts, G. Kenneth Lloyd, Yoshio Hayashi: Tubulin photoaffinity labeling by biotin-tagged derivatives of potent diketopiperazine anti-microtubule agents. ChemBioChem, 9(18), 3074-3081 (2008). 551 Hiroyoshi Matsumura, Motoyasu Adachi, Shigeru Sugiyama, Shino Okada, Megumi Yamakami, Taro Tamada, Koushi Hidaka, Yoshio Hayashi, Tooru Kimura, Yoshiaki Kiso, Tomoya Kitatani, Sho Maki, Hiroshi Y. Yoshikawa, Hiroaki Adachi, Kazufumi Takano, Satoshi Murakami, Tsuyoshi Inoue, Ryota Kuroki and Yusuke Mori: Crystallization and preliminary neutron diffraction studies of HIV-1 protease cocrystallized with inhibitor KNI-272. Acta Crystallographica, F64 (11), 1003-1006 (2008). 552 Atsuhiko Taniguchi, Youhei Sohma, Mariusz Skwarczynski, Takami Nagano, Takuma Okada, Keisuke Ikeda, Halan Prakash, Hidehito Mukai, Yoshio Hayashi, Tooru Kimura, Shun Hirota, Katsumi Matsuzaki, Yoshiaki Kiso: Development of water-soluble click peptides by use of the O-acyl isopeptide method: In situ production of Alzheimer's amyloid ß peptide. Proc. 30th Eur. Peptide Symp., (ed. Hilkka Lankinen) pp.32-33 (2008) 553 Taku Yoshiya, Atsuhiko Taniguchi, Naoko Abe, Nui Ito, Youhei Sohma, Mariusz Skwarczynski, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Isopeptide method: an efficient preparation of difficult peptides on solid support. Proc. 30th Eur. Peptide Symp., (ed. Hilkka Lankinen) pp.80-81 (2008) 554 Yuri Yamazaki, Kyoko Kohno, Hiroyuki Yasui, Yoshiaki Kiso, Saskia Neuteboom, Ana M. Barral, Barbara Potts, Kenneth Lloyd, Yoshio Hayashi: Development of biotin-tagged diketopiperazine based anti-microtubule agents and tubulin photoaffinity labeling. Proc. 30th Eur. Peptide Symp., (ed. Hilkka Lankinen) pp.528-529 (2008) 555 Hidehito Mukai, Nobuhiko Ueki, Kaori Wakamatsu, Yoshiaki Kiso: Cryptic signal: a novel signaling mechanism involving cryptides. Proc. 30th Eur. Peptide Symp., (ed. Hilkka Lankinen) pp.570-571 (2008) 556 Maiko Ebina, Eugene Futai, Chiaki Tanabe, Noboru Sasagawa, Yoshiaki Kiso, and Shoichi Ishiura: Inhibition by KMI-574 leads to dislocalization of BACE1 from lipid rafts. J. Neurosci. Res.,87 (2),360-368 (2009). 557 Yoshiaki Kiso, Atsuhiko Taniguchi, Youhei Sohma: Click peptides: design and applications. Wiley Encyclopedia of Chemical Biology, (ed. Tadhg P. Begley), Vol. 1, 379-383 (2009). 558 Atsuhiko Taniguchi, Youhei Sohma, Yuta Hirayama, Hidehito Mukai, Tooru Kimura, Yoshio Hayashi, Katsumi Matsuzaki, Yoshiaki Kiso: “Click peptide”: pH-triggered in situ production and aggregation of monomer Aß1-42. ChemBioChem, 10(4), 710-715 (2009). 559 Yoshiaki Kiso: Defying difficult diseases: peptide chemistry in medicinal science. Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp1-4 (2009). 560 Yuki Mori, Yuri Yamazaki, Akiko Oda, Reiko Okamoto, Masaru Nagahara, Yoshiaki Kiso, Yoshio Hayashi: A synthetic method for monodehydro-cyclic-dipeptides toward natural product synthesis. Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp15-16 (2009). 561 Kazuki Saito, Mamiko Nakato, Takaaki Mizuguchi, Hiromasa Uchimura, Shigeyuki Yokoyama, Hiroshi Hirota, Yoshiaki Kiso: High-throughput screening method for ligand peptides using capillary electrophoresis-mass spectrometry (CE-MS). Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp119-120 (2009). 562 Yoshio Hayashi, Yuri Yamazaki, Shigenobu Nishiguchi, Thomas Regnier, Yuki Mori, Akihiro Taguchi, Yoshiaki Kiso: Small peptide-based medicinal chemistry for intractable disease. Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp139-140 (2009). 563 Taeko Kakizawa, Shizuyo Koide-Yoshida, Tooru Kimura, Takaaki Mizuguchi, Hiromasa Uchimura, Yoshio Hayashi, Kazuki Saito, Yoshiaki Kiso: Chemical synthesis of 71-meric neuregulin 1-ß1. Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp169-170 (2009). 564 Taku Yoshiya, Youhei Sohma, Tooru Kimura, Yoshiaki Kiso: Isopeptide method: a racemization-free peptide synthesis by segment condensation. Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp189-190 (2009). 565 Nui Ito, Taku Yoshiya, Tooru Kimura, Yoshiaki Kiso: A novel S-acyl Isopeptide method for the synthesis of difficult sequence-containing peptide. Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp191-194 (2009). 566 Hidehito Mukai, Nobuhiko Ueki, Kazuya Someya, Masanori Kawanami, Yuko Matsuo, Mayumi Kiyama, Rie Kamijo, Miharu Kikuchi, Shigetomo Fukuhara, Eisuke Munekata, Yoshiaki Kiso: Cryptic signaling and the exocytotic mechanisms induced by amphiphilic peptides. Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp 307-310 (2009). 567 Yoshio Hamada, Hiroko Ohta, Naoko Miyamoto, Takashi Hamada, Tomoya Nakanishi, Moe Yamasaki, Abdellah Yamani, Kazuki Saito, Yoshiaki Kiso: Significance of interaction of BACE1-Arg235 with its ligands and design of BACE1 inhibitors. Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp317-320 (2009). 568 Hiroko Ohta, Yoshio Hamada, Naoko Miyamoto, Ryoji Yamaguchi, Abdellah Yamani, Koushi Hidaka, Tooru Kimura, Kazuki Saito, Shoichi Ishiura, Yoshiaki Kiso; SAR study of BACE1 inhibitors containing pyridine derivatives. Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp321-324 (2009). 569 Koushi Hidaka, Tooru Kimura, Tsuyoshi Uemura, Adam J. Ruben, Ernesto Freire, Yoshiaki Kiso: Effect of dipeptidomimetics on malaria parasite proliferation inhibition targeting plasmepsin. Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp325-326 (2009). 570 Akihiro Taguchi, Shigenobu Nishiguchi, Thomas Regnier, Minoru Ozeki, Manabu Node, Yoshiaki Kiso, Yoshio Hayashi: Efficient total synthesis of (+)-negamycin and its derivatives. Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp375-376 (2009). 571 Takaaki Mizuguchi, Hiromasa Uchimura, Taeko Kakizawa, Tooru Kimura, Shigeyuki Yokoyama, Yoshiaki Kiso, Kazuki Saito: Design and synthesis of inhibitory peptides against EGF receptor dimerization. Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp383-384 (2009). 572 Atsuhiko Taniguchi, Youhei Sohma, Mariusz Skwarczynski, Takuma Okada, Keisuke Ikeda, Halan Prakash, Hidehito Mukai, Tooru Kimura, Yoshio Hayashi, Shun Hirota, Katsumi Matsuzaki, Yoshiaki Kiso: Click peptide by use of the O-acyl isopeptide method: production of amyloid ß peptide from water-soluble analogue. Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp397-400 (2009). 573 Yuri Yamazaki, Kyoko Kohno, Hiroyuki Yasui, Yoshiaki Kiso, Miki Akamatsu, Benjamin Nicholson, Gordafaried Deyanat-Yazdi, Saski Neuteboom, Barbara Potts, G. Kenneth Lloyd, Yoshio Hayashi: Development of biotin-tagged tubulin photoaffinity probes derivatized from diketopiperazine based anti-microtubule agents. Peptide Science 2008 (M. Nomizu, ed.) The Japanese Peptide Society, pp423-424 (2009). 574 Motoyasu Adachi, Takashi Ohhara, Kazuo Kurihara, Taro Tamada, Eijiro Honjo, Nobuo Okazaki, Shigeki Arai, Yoshinari Shoyama, Kaname Kimura, Hiroyoshi Matsumura, Shigeru Sugiyama, Hiroaki Adachi, Kazufumi Takano, Yusuke Mori, Koushi Hidaka, Tooru Kimura, Yoshio Hayashi Yoshiaki Kiso, Ryota Kuroki: Structure of HIV-1 protease in complex with potent inhibitor KNI-272 determined by high resolution X-ray and neutron crystallography, Proc. Natl. Acad. Sci. USA, 106 (12), 4641-4646 (2009). 2009/3/24 575 Yuri Yamazaki, Yuki Mori, Akiko Oda, Yuka Okuno, Yoshiaki Kiso, Yoshio Hayashi: Acid catalyzed monodehydro-2, 5-diketopiperazine formation from N-a-ketoacyl amino acid amides. Submitted to Tetrahedron, 65 (18), 3688-3694 (2009). 2009/5/2 576 Hidehito Mukai, Tetsuo Seki, Hiroko Nakano, Yoshinori Hokari, Toshifumi Takao, Masanori Kawanami, Hiroyuki Tsukagoshi, Hirokazu Kimura, Yoshiaki Kiso, Yasutsugu Shimonishi, Yoshisuke Nishi, Eisuke Munekata: Mitocryptide-2: purification, identification, and characterization of a novel cryptide that activates neutrophils. J. Immunology, 182(8) 5072-5080 (2009). 2009/4/15 577 Yoshio Hamada, Yoshiaki Kiso: Recent progress in the drug discovery of non-peptidic BACE1 inhibitors. Expert Opinion on Drug Discovery, 4 (4), 391-416 (2009). 2009/4 578 Yoshio Hamada, Hiroko Ohta, Naoko Miyamoto, Diganta Sarma, Takashi Hamada, Tomoya Nakanishi, Moe Yamasaki, Abdellah Yamani, Shoichi Ishiura, Yoshiaki Kiso: Significance of interactions of BACE1-Arg235 with its ligands and design of BACE1 inhibitors with P2 pyridine scaffold. Bioorg. Med. Chem. Lett., 19 (9), 2435-2439 (2009). 579 Prasenjit Bhaumik, Huogen Xiao, Charity L. Parr, Yoshiaki Kiso, Alla Gustchina, Rickey Y. Yada, Alexander Wlodawer: Crystal structure of the histo-aspartic protease (HAP) from Plasmodium falciparum. J. Mol. Biol., 388 (3), 520-540 (2009). 580 Thomas Regnier, Diganta Sarma, Koushi Hidaka, Usman Bacha, Ernesto Freire, Yoshio Hayashi, Yoshiaki Kiso: New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3Clpro inhibitors. Bioorg. Med. Chem. Lett., 19(10), 2722-2727 (2009). 581 Takaaki Mizuguchi, Hiromasa Uchimura, Taeko Kakizawa, Tooru Kimura, Shigeyuki Yokoyama, Yoshiaki Kiso, Kazuki Saito: Inhibitory effect of a dimerization-arm-mimetic peptide on EGF receptor activation. Bioorg. Med. Chem. Lett., 19 (12), 3279-3282 (2009). 582 Taku Yoshiya, Hiroyuki Kawashima, Youhei Sohma, Tooru Kimura, Yoshiaki Kiso: O-Acyl isopeptide method: efficient synthesis of isopeptide segment and application to racemization-free segment condensation. Org. Biomol. Chem., 7 (14), 2894-2904 (2009). Cover photo used. 583 Jeffrey-Tri Nguyen, Yoshiaki Kiso: Rational drug design of HTLV-I protease inhibitors. Proteases in Biology and Disease. Vol.8. Viral proteases and antiviral protease inhibitor therapy. (U. Lendeckel, N. M. Hooper, Eds.) Springer pp. 83-100 (2009). 584 Hui Wang, Taeko Kakizawa, Atsuhiko Taniguchi, Takaaki Mizuguchi, Tooru Kimura, Yoshiaki Kiso: Synthesis of amyloid b peptide 1-42 (E22D) click peptide: pH-triggered in situ production of its native form. Bioorg. Med. Chem., 17 (14), 4881-4887 (2009). 585 Yoshio Hayashi, Shigenobu Nishiguchi, Magne O. Sydnes, Thomas Regnier, Jun-ya Hasegawa, Takahiro Katoh, Tetsuya Kajimoto, Manabu Node, Yoshiaki Kiso: A new synthesis of (+)-negamycin and its derivatives as a potential therapeutic agent for Duchenne muscular dystrophy treatment. Peptides for Youth: Proc. 20th Amer. Peptide Symp. (Eds. S. Del Valle, E. Escher, W. D. Lubell), pp.137-138 (2009). 586 Taku Yoshiya, Youhei Sohma, Yoshio Hamada, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso: Racemization-free segment condensation based on the O-acyl isopeptide method: Toward a chemical protein synthesis on solid support. Peptides for Youth: Proc. 20th Amer. Peptide Symp. (Eds. S. Del Valle, E. Escher, W. D. Lubell), pp.161-162 (2009). 587 Hiromi Kodera, Naoki Nishishita, Yoshiaki Hirano, Yoshiaki Kiso, Yoshio Hayashi: Synthesis of polylactides with side chain functionality: ring-opening polymerization of a homobislactone prepared from lysine. Peptides for Youth: Proc. 20th Amer. Peptide Symp. (Eds. S. Del Valle, E. Escher, W. D. Lubell), pp.243-244 (2009). 588 Yoshio Hayashi, Yuri Yamazaki, Mariusz Skwarczynski, Youhei Sohma, Atsuhiko Taniguchi, Mayo Noguchi, Tooru Kimura, Saskia Neuteboom, Barbara Potts, G. Kenneth Lloyd, Yoshiaki Kiso: Application of intramolelcular migration reaction in peptide chemistry to chemical biology, chemical pharmaceutics and medicinal chemistry. Peptides for Youth: Proc. 20th Amer. Peptide Symp. (Eds. S. Del Valle, E. Escher, W. D. Lubell), pp.513-514 (2009). 589 Yuri Yamazaki, Kyoko Kohno, Hiroyuki Yasui, Yoshiaki Kiso, Saskia Neuteboom, Ana M. Barral, Barbara Potts, G. Kenneth Lloyd, Yoshio Hayashi: Synthesis of biotin-tagged diketopiperazine-based anti-microtubule agents and tubulin photoaffinity labeling. Peptides for Youth: Proc. 20th Amer. Peptide Symp. (Eds. S. Del Valle, E. Escher, W. D. Lubell), pp.527-528 (2009). 590 Taku Yoshiya, Hiroyuki Kawashima, Youhei Sohma, Tooru Kimura, Yoshiaki Kiso: O-Acyl isopeptide method: Toward an efficient chemical preparation of peptides/proteins using racemization-free segment condensation method. Peptides Breaking Away: Proc. 21st Amer. Peptide Symp. (Ed. Michal Lebl) pp.13-14 (2009). 591 Yuri Yamazaki, Yuki Mori, Akiko Oda, Yoshiaki Kiso, Yoshio Hayashi: Acid catalyzed monodehydro-2,5-diketopiperazine formation toward natural product synthesis. Peptides Breaking Away: Proc. 21st Amer. Peptide Symp. (Ed. Michal Lebl) pp.54-55 (2009). 592 Atsuhiko Taniguchi, Youhei Sohma, Mariusz Skwarczynski, Yuta Hirayama, Takuma Okada, Keisuke Ikeda, Halan Prakash, Hidehito Mukai, Tooru Kimura, Yoshio Hayashi, Shun Hirota, Katsumi Matsuzaki, Yoshiaki Kiso: "Click peptide" based on "O-acyl isopeptide method": In situ production of monomer amyloid ß peptide from water-soluble precursor analogues. Peptides Breaking Away: Proc. 21st Amer. Peptide Symp. (Ed. Michal Lebl) pp.195-196 (2009). 593 Hidehito Mukai, Tetsuo Seki, Eisuke Munekata, Yoshiaki Kiso: Cryptides: discovery of functional cryptic peptides hidden in protein structures and identification of their signaling mechanisms. Peptides Breaking Away: Proc. 21st Amer. Peptide Symp. (Ed. Michal Lebl) pp.203-204 (2009). 594 Yoshio Hayashi, Akihiko Taguchi, Thomas Regnier, Shigenobu Nishiguchi, Yoshiaki Kiso: Efficient total synthesis of dipeptidic antibiotics (+)-negamycin and its derivatives. Peptides Breaking Away: Proc. 21st Amer. Peptide Symp. (Ed. Michal Lebl) pp.278-279 (2009). 595 Sebastian D. Kiewitz, Yoshiaki Kiso, Chiara Cabrele: Conformation and stability of the helix-loop-helix domain of the Id protein family. Peptides Breaking Away: Proc. 21st Amer. Peptide Symp. (Ed. Michal Lebl) pp.343-344 (2009). 596 Koushi Hidaka, Tooru Kimura, Hamdy M. Abdel-Rahman, Jeffrey-Tri Nguyen, Keith F. McDaniel, William E. Kohlbrenner, Akhteruzzaman Molla, Motoyasu Adachi, Taro Tamada, Ryota Kuroki, Noriko Katsuki, Yoshiaki Tanaka, Hikaru Matsumoto, Jun Wang, Yoshio Hayashi, Dale J. Kempf, Yoshiaki Kiso: Small-sized HIV-1 protease inhibitors containing allophenylnorstatine to explore S2' pocket. J. Med. Chem. 52 (23), 7604-7617 (2009). 597 Shigenobu Nishiguchi, Magne O. Sydnes, Akihiro Taguchi, Thomas Regnier, Tetsuya Kajimoto, Manabu Node, Yuri Yamazaki, Fumika Yakushiji, Yoshiaki Kiso, Yoshio Hayashi: Total synthesis of (+)-negamycin and its 5-epi-derivative. Tetrahedron, 66(1), 314-320 (2010). 598 木曽良明、林良雄、相馬洋平、日高興士：生物分子システムを基盤とする統合創薬科学。MEDCHEM NEWS, 20(1), 2-8 (2010). 599 Yuko Kawasaki, Eduardo E. Chufan, Virginie Lafont, Koushi Hidaka, Yoshiaki Kiso, L. Mario Amzel, Ernesto Freire: How much binding affinity can be gained by filling a cavity? Chem. Biol. Drug Design, 75(2), 143-151 (2010). 600 谷口敦彦、相馬洋平、木曽良明：ペプチド・タンパク質の機能解明のツールとしてのクリックペプチド：アミロイドβペプチド水溶性プレカーサーに見るその合成と応用への展望。化学と生物48(4), 232-234 (2010). 601 Keisuke Kashimoto, Koushi Hidaka, Tsuyoshi Uemura, Takuya Miura, Enesto Freire, Tooru Kimura, Yoshiaki Kiso: Attachment of basic amino group to plasmepsin inhibitors exhibiting potent antimalarial activity. Peptide Science 2009 (K. Okamoto, Ed.), 33-36 (2010). 602 Hidehito Mukai, Tetsuo Seki, Yoshinori Hokari, Akiyoshi Fukamizu, Yoshiaki Kiso: Characterization of receptors and signaling mechanisms for mitocryptides-2, a novel cryptide that activates neutrophils. Peptide Science 2009 (K. Okamoto, Ed.), 97-98 (2010). 603 Yuka Hasegawa, Taku Yoshiya, Tooru Kimura, Yoshiaki Kiso: S-Acyl isopeptide method: an effective preparation of Cys-containing difficult peptide. Peptide Science 2009 (K. Okamoto, Ed.), 161-162 (2010). 604 Hiroyuki Kawashima, Taku Yoshiya, Youhei Sohma, Tooru Kimura, Yoshiaki Kiso: Isopeptide method: a racemization-free peptide synthesis by sequential segment condensation. Peptide Science 2009 (K. Okamoto, Ed.), 163-166 (2010). 605 Ayano Higa, Taku Yoshiya, Atsuhiko Taniguchi, Naoko Abe, Nui Ito, Youhei Sohma, Tooru Kimura, Yoshiaki Kiso: O-Acyl isopeptide method: application of isodipeptide units for Ser-, Thr- and Cys-containing difficult peptide synthesis. Peptide Science 2009 (K. Okamoto, Ed.), 167-170 (2010). Youhei Sohma, Stephen B. H. Kent: Design and synthesis of a mini-proinsulin convertible to human insulin. Peptide Science 2009 (K. Okamoto, Ed.), 179-180 (2010). 606 Yoshio Hamada, Daisuke Shuto, Ping Liu, Takashi Hamada, Koushi Hidaka, Tooru Kimura, Yoshiaki Kiso: Significance of wild-type APP sequence in developing the BACE1 inhibitors. Peptide Science 2009 (K. Okamoto, Ed.), 255-258 (2010). 607 Diganta Sarma, Thomas Regnier, Koushi Hidaka, Sho Konno, Usman Bacha, Ernesto Freire, Yoshiaki Kiso, Yoshio Hayashi: Synthesis of tripeptide-type SARS-CoV 3Clpro inhibitors with a highly electrophilic carbonyl group. Peptide Science 2009 (K. Okamoto, Ed.), 311-314 (2010). 608 Makiko Sumikura, Yuri Yamazaki, Tomoko Yoshida, Yuki Mori, Hiroyuki Yasui, Yoshiaki Kiso, Saskia Neuteboom, Barbara Potts, G. Kenneth Lloyd, Yoshio Hayashi: Synthesis and structure-activity relationship study of cyclic dipeptide-based microtubule depolymerization agents with a benzopheneone structure. Peptide Science 2009 (K. Okamoto, Ed.), 315-316 (2010). 609 Akihiro Taguchi, Mayuko Ina, Yuri Yamazaki, Fumika Yakushiji, Yoshikazu Takahashi, Yoshiaki Kiso, Yoshio Hayashi: Synthesis and antimicrobial activity of (+)-negamycin derivatives focused on the hydrazine amide moiety. Peptide Science 2009 (K. Okamoto, Ed.), 317-318 (2010). 610 Hui Wang, Taeko Kakizawa, Atsuhiko Taniguchi, Takaaki Mizuguchi, Youhei Sohma, Hidehito Mukai, Tooru Kimura, Yoshiaki Kiso: Investigation of Ab1-42 mutants based on O-acyl isopeptide method; synthesis of O-acyl isopeptides and in situ production of their native form. Peptide Science 2009 (K. Okamoto, Ed.), 367-368 (2010). 611 Yuta Hirayama, Atsuhiko Taniguchi, Youhei Sohma, Hidehito Mukai, Tooru Kimura, Yoshio Hayashi, Katsumi Matsuzaki, Yoshiaki Kiso: Click peptide: water -soluble precursor producing monomer amyloid b peptide in situ. Peptide Science 2009 (K. Okamoto, Ed.), 371-372 (2010). 612 Kazuki Saito, Itsuki Yasuo, Hiromasa Uchimura, Shizuyo Koide-Yoshida, Takaaki Mizuguchi, Yoshiaki Kiso: Quantitative porteolytic 18O-labeling analysis of protein disulfide bond rearrangement. Peptide Science 2009 (K. Okamoto, Ed.), 393-394 (2010). 613 Kazuki Saito, Itsuki Yasuo, Hiromasa Uchimura, Shizuyo Koide-Yoshida, Takaaki Mizuguchi, Yoshiaki Kiso: Verification of protein disulfide bond arrangement by in-gel tryptic digestion under entirely neutral pH conditions. PROTEOMICS, 10 (7), 1505-1509 (2010). 614 Taku Yoshiya, Yuka Hasegawa, Wakana Kawamura, Hiroyuki Kawashima, Youhei Sohma, Tooru Kimura, Yoshiaki Kiso: S-Acyl isopeptide method: use of allyl-type protective group for improved preparation of thioester-containing S-acyl isopeptides by Fmoc-based SPPS. Biopolymers Peptide Science, in press. 615 Yuri Yamazaki, Makiko Sumikura, Koushi Hidaka, Hiroyuki Yasui, Yoshiaki Kiso, Fumika Yakushiji, Yoshio Hayashi: Anti-microtubule "plinabulin" chemical probe KPU-244-B3 labeled both a- and b-tubulin. Bioorg. Med. Chem., 18 (9), 3169-3174 (2010). 616 Harichandra D. Tagad, Yoshio Hamada, Jeffrey-Tri Nguyen, Takashi Hamada, Hamdy Abdel-Rahman, Abdellah Yamani, Ayaka Nagamine, Hayato Ikari, Naoto Igawa, Koushi Hidaka, Youhei Sohma, Tooru Kimura, Yoshiaki Kiso: Design of pentapeptidic BACE1 inhibitors with carboxylic acid bioisosteres at P1’ and P4 positions. Bioorg. Med. Chem., 18 (9), 3175-3186 (2010). 617 Taeko Kakizawa, Koushi Hidaka, Daisuke Hamada, Ryoji Yamaguchi, Tsuyoshi Uemura, Hitomi Kitamura, Harichandra D. Tagad, Takashi Hamada, Zyta Ziora, Yoshio Hamada, Tooru Kimura, Yoshiaki Kiso: Tetrapeptides, as small-sized peptidic inhibitors; synthesis and their inhibitory activity against BACE1. J. Peptide Science, 16 (6), 257-262 (2010). 618 Michael Beißwenger, Taku Yoshiya, Yoshiaki Kiso, Chiara Cabrele: Reversible modification of peptides containing the O-acyl iso-prolyl-seryl motif. J. Peptide Science, 16 (6), 303-308 (2010). 619 向井秀仁、木曽良明、若松馨：クリプタイドの発見と新しい生体情報伝達機構。生化学、82 (6), 524-532 (2010). 620 Noriko Shimizu, Shigeru Sugiyama, Mihoko Maruyama, Yoshinori Takahashi, Motoyasu Adachi, Taro Tamada, Koushi Hidaka, Yoshio Hayashi, Tooru Kimura, Yoshiaki Kiso, Hiroaki Adachi, Kazufumi Takano, Satoshi Murakami, Tsuyoshi Inoue, Ryota Kuroki, Yusuke, Mori, Hiroyoshi Matsumura: Crystal growth procedure of HIV-1 protease-inhibitor KNI-272 complex for neutron structural analysis at 1.9A resolution. Crystal Growth & Design, 10 (7), 2990-2994 (2010). 621 Taku Yoshiya, Hiroyuki Kawashima, Yuka Hasegawa, Kazuhiro Okamoto, Tooru Kimura, Youhei Sohma, Yoshiaki Kiso: Racemization-free synthesis of cyclic peptide by use of the O-acyl isopeptide method. J. Peptide Science. 16 (8), 437-442 (2010). 622 Takuya Miura, Koushi Hidaka, Tsuyoshi Uemura, Keisuke Kashimoto, Yuto Hori, Yuko Kawasaki, Adam J. Ruben, Ernesto Freire, Tooru Kimura, Yoshiaki Kiso: Improvement of both plasmepsin inhibitory activity and Antimalarial activity by 2-aminoethylamino substitution. Bioorg. Med. Chem. Lett., 20 (16), 4836-4839 (2010). 623 Tadashi Satoh, Mi Li, Jeffrey-Tri Nguyen, Yoshiaki Kiso, Alla Gustchina, Alexander Wlodawer: Crystal structures of the inhibitor complexes of human T cell leukemia virus (HTLV-1) protease. J. Mol. Biol., 401, 626-641 (2010). 624 Adam J. Ruben, Yoshiaki Kiso and Ernesto Freire: The Plasmepsin Family as Antimalarial Drug Targets. In Methods and Principles in Medicinal Chemistry, 45(Aspartic Acid Proteases as Therapeutic Targets) (Ed. By Arun K. Ghosh) Wiley, pp513-547 (October 2010). 625 Yuri Yamazaki, Yui Kido, Koushi Hidaka, Hiroyuki Yasui, Yoshiaki Kiso, Fumika Yakushiji, Yoshio Hayashi: Tubulin photoaffinity labeling study with a plinabulin chemical probe possessing a biotin tag at the oxazole. Bioorg. Med. Chem, 19, 595-602 (2011). 626 Hironobu Hojo, Hidekazu Katayama, Chiharu Tano, Yuko Nakahara, Azusa Yoneshige, Junko Matsuda, Youhei Sohma, Yoshiaki Kiso, and Yoshiaki Nakahara: Synthesis of the sphingo¬lipid activator protein, saposin C, using an azido-protected O-acyl isopeptide as an aggrega-tion-disrupting element. Tetrahedron Letters, 52, 635-639 (2011). 627 Youhei Sohma, Yuta Hirayama, Atsuhiko Taniguchi, Hidehito Mukai, Yoshiaki Kiso：‘Click peptide’ using production of monomer Ab from the O-acyl isopeptide: Application to assay system of aggregation inhibitors and cellular cytotoxicity. Bioorg. Med. Chem., 19, 1729–1733 (2011). 628 Jeffrey-Tri Nguyen , Keiko Kato, Henri-Obadja Kumada, Koushi Hidaka, Tooru Kimura and Yoshiaki Kiso: Maintaining potent HTLV-I protease inhibition without the P3-cap moiety in small tetrapeptidic inhibitors. Bioorg. Med. Chem. Lett. 21, 1832–1837 (2011). 629 Tesuo Seki, Akiyoshi Fukamizu, Yoshiaki Kiso, Hidehito Mukai: Mitocryptide-2, a neutrophil-activating cryptide, is a specific endogenous agonist for formyl-peptide receptor-like 1. Biochem. Biophys. Res. Commun. 404(1), 482-487 (2011). 630 Taku Yoshiya, Ayano Higa, Naoko Abe, Fukue Fukao, Tomomi Kuruma, Youhei Sohma and Yoshiaki Kiso: “Click Peptide” Concept: O-Acyl Isopeptide of Islet Amyloid Polypeptide As a non-aggregative precursor molecule. Submitted to ChemBioChem. 12 (8), 1216-1222 (2011). 631 Jeffrey-Tri Nguyen, Keiko Kato, Koushi Hidaka, Henri-Obadja Kumada, Tooru Kimura, Yoshiaki Kiso: Design and synthesis of several small-size HTLV-I protease inhibitors with different hydrophilicity profiles. Bioorg. Med. Chem. Lett. 21, 2425–2429 (2011). 632 Youhei Sohma, Hui Wang, Atsuhiko Taniguchi, Yuta Hirayama, Taeko Kakizawa, Hidehito Mukai, Yoshiaki Kiso: The E22-type mutant of amyloid peptide (A) adopts distinct self-assembly mechanisms from wild-type A. Bioorg. Med. Chem. 19, 3837-3792 (2011). 633 Hidehito Mukai, Tetsuo Seki, Yoshinori Hokari, Akiyoshi Fukamizu, Yoshiaki Kiso: Cryptides: Non-Classical Bioactive Peptides Hidden in Protein Structures. Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 29 (2011). 634 Youhei Sohma*, Atsuhiko Taniguchi, Yuta Hirayama, Hui Wang, Moe Yamasaki, Hidehito Mukai, and Yoshiaki Kiso: Use of O-Acyl Isopeptides to Identify New Functions of Amyloid Peptides. Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 54 (2011). 635 Yuri Yamazaki, Yui Kido, Koushi Hidaka, Hiroyuki Yasui, Yoshiaki Kiso, Fumika Yakushiji, Yoshio Hayashi: Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 56 (2011). 636 Takaaki Mizuguchi, Hiromasa Uchimura, Yoshiaki Kiso, Kazuki Saito: Intact Cell-based SPR Analyses of Interactions between EGF and its Receptor. Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 98 (2011). 637 Hiromasa Uchimura, Yusam Kim, Takaaki Mizuguchi, Yoshiaki Kiso, Kazuki Saito: Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 148 (2011). 638 Moe Yamasaki, Youhei Sohma, Atsuhiko Taniguchi, Yuta Hirayama, Miki Furuya, Hidehito Mukai, Yoshiaki Kiso: Click Peptide: In Situ Production of pyroGlu-Abeta from the O-Acyl Isopeptide. Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 210 (2011). 639 Mayuko Ina, Takao Nomoto, Masataka Shiozuka, Akihiro Taguchi, Yuri Yamazaki, Fumika Yakushiji, Yoshiaki Kiso, Yoshiaki Nonomura, Ryoichi Matsuda, Yoshio Hayashi: Synthesis and Biological Evaluation of Dipeptidic Antibiotics (+)-Negamycin and Its Derivatives for Development of Duchenne Muscular Dystrophy Chemotherapy Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 211 (2011). 640 Hui Wang, Youhei Sohma, Atsuhiko Taniguchi, Yuta Hirayama, Taeko Kakizawa, Hidehito Mukai, Yoshiaki Kiso: Click Peptide: Application to E22-type Mutant of Amyloid Peptide Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 221 (2011). 641 Sho Konno, Kiyohiko Nakada, Rie Kakiuchi, Yuri Yamazaki, Fumika Yakushiji, Koushi Hidaka, Yoshiaki Kiso, Kenichi Akaji, Yoshio Hayashi: Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 251 (2011). 642 Taeko Kakizawa, Koushi Hidaka, Daisuke Hamada, Ryoji Yamaguchi, Tsuyoshi Uemura, Hitomi Kitamura, Harichandra D. Tagad, Takashi Hamada, Zyta Ziora, Yoshio Hamada, Tooru Kimura, Yoshiaki Kiso: Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 252 (2011). 643 Yoshio Hamada, Harichandra D. Tagad, Takashi Hamada, Tooru Kimura, Yoshiaki Kiso: Tripeptidic BACE1 Inhibitors by Conformational Structure-based Design. Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 253 (2011). 644 Harichandra D. Tagad, Yoshio Hamada, Koushi Hidaka, Youhei Sohma, Tooru Kimura, Yoshiaki Kiso: Phenyl(cyclo)alkylamines: Second generation P1' position analogs for pentapeptidic BACE1 inhibitors. Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 254 (2011). 645 Yoshio Hamada, Harichandra D. Tagad, Takashi Hamada, Tooru Kimura, Yoshiaki Kiso: Can the substrate of an enzyme turn into its inhibitor by vastly-reduced kcat value? Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 255 (2011). 646 Tomoya Nakanishi, Yoshio Hamada, Ryoji Yamaguchi, Makoto Yamaguchi, Takashi Hamada, Koushi Hidaka, Tooru Kimura, Yoshiaki Kiso: Design of BACE1 Inhibitors Containing 5-Nitro-Isophthalamide. Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 256 (2011). 647 Kenji Suzuki, Yoshio Hamada, Megumi Ogata, Takashi Hamada, Satoshi Nojima, Naoya Kinomura, Tsutomu Mimoto, Yoshiaki Kiso: Novel BACE1 inhibitors containing P1-P1’ non-natural amino acid-guanidinyl analogues. Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp.258 (2011). 648 Takuya Miura, Koushi Hidaka, Keisuke Kashimoto, Yuto Hori, Yukiko Azai, Yuko Kawasaki, Adam J. Ruben, Ernesto Freire, Tooru Kimura, Yoshiaki Kiso: Optimization of Peptidomimetic Plasmepsin Inhibitor Containing Allophenylnorstatine Using Basic Substituent for Malaria Treatment. Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 261 (2011). 649 Kazuki Saito, Mamiko Nakato, Takaaki Mizuguchi, Shinji Wada, Hiromasa Uchimura, Shigeyuki Yokoyama, Hiroshi Hirota, Yoshiaki Kiso: Screening Methodology for Discovery of Inhibitory Peptides against Pathogenic Proteins using a Plug-plug Affinity Capillary Electrophoresis Technique. Peptide Science 2010: Proceedings of the Fifth International Peptide Symposium. Nobutaka Fujii and Yoshiaki Kiso (Editors), The Japanese Peptide Society, pp. 287 (2011). 650 Zyta Ziora, Mariusz Skwarczynski, Yoshiaki Kiso: Medicinal Chemistry of -hydroxy-- amino acids. In Amino Acids, Peptides and Proteins in Organic Chemistry, Vol. 4 - Building blocks, catalysis and coupling chemistry (ed. By Andrew B. Hughes) Wiley-VCH. Pp189-245 (2011). 651 Prasenjit Bhaumik, Yasumi Horimoto, Huogen Xiao, Alexander Wlodawer, Yoshiaki Kiso, Rickey Y. Yada and Alla Gustchina: Crystal structure of the free and inhibited plasmepsin I from Plasmodium falciparum. J. Structural Biol., 175(1),73-84 (2011). 652 Hiromasa Uchimura, Yusam Kim, Takaaki Mizuguchi, Yoshiaki Kiso, Kazuki Saito: Quantitative evaluation of refolding conditions for a disulfide-bond-containing protein using a concise 18O-labeling technique. Protein Science 20(6), 1090-1096 (2011). 653 Henri-Obadja Kumada, Jeffrey-Tri Nguyen, Keiji Nishiyama, Taeko Kakizawa, Yasuhiro Arii, Koushi Hidaka, Tooru Kimura, Yoshio Hayashi and Yoshiaki Kiso: Development of L40I HTLV-I protease inhibition assay using novel fluorogenic and chromogenic substrate. J. Peptide Science, 17 (8), 569-575 (2011) 654 Harichandra D. Tagad, Yoshio Hamada, Jeffrey-Tri Nguyen, Koushi Hidaka, Takashi Hamada, Youhei Sohma, Tooru Kimura, Yoshiaki Kiso: Structure-guided design and synthesis of P1' position 1-phenylcycloalkylamine-derived pentapeptidic BACE1 inhibitors. Bioorg. Med. Chem. 19, 5238–5246 (2011). 655 Prasenjit Bhaumik, Huogen Xiao, Koushi Hidaka, Alla Gustchin, Yoshiaki Kiso, Rickey Y. Yada, Alexander Wlodawer: Structural insights into activation and inhibition of histo-as¬partic protease (HAP) from Plasmodium falciparum. Biochemistry. 50 (41), 8862–8879 (2011). 656 Youhei Sohma, Hitomi Kitamura, Hiroyuki Kawashima, Hironobu Hojo, Masayuki Yamashita, Kenichi Akaji, Yoshiaki Kiso: Synthesis of an O-acyl isopeptide by using native chemical ligation to efficiently construct a hydrophobic polypeptide. Tetrahedron Letters, 52(52), 7146-7148 (2011). 657 濵田芳男、木曽良明：アルツハイマー病とＢＡＣＥ１阻害剤の設計。和光純薬時報 79(1),5-7 (2011). 658 Takaaki Mizuguchi, Hiromasa Uchimura, Hiroshi Kataoka, Kenichi Akaji, Yoshiaki Kiso, Kazuki Saito, Intact-cell-based surface plasmon resonance measurements for ligand affinity evaluation of a membrane receptor. Anal. Biochem. 420(2), 185-187 (2012). 659 Akihiro Taguchi, Shigenobu Nishiguchi, Masataka Shiozuka, Takao Nomoto, Mayuko Ina, Shouta Nojima, Ryoichi Matsuda, Yoshiaki Nonomura, Yoshiaki Kiso, Yuri Yamazaki, Fumika Yakushiji, and Yoshio Hayashi: Negamycin Analogue with Readthrough-Promoting Activity as a Potential Drug Candidate for Duchenne Muscular Dystrophy. ACS Med Chem Lett., 3(2), 118-122 (2012). 660 Yoshio Hamada, Harichandra D. Tagad, Yoshinori Nishimura, Shoichi Ishiura and Yoshiaki Kiso: Tripeptidic BACE1 inhibitors devised by in-silico conformational structure-based design. Bioorg. Med. Chem. Lett., 22, 1130–1135 (2012) 661 Yoshio Hamada, Shoichi Ishiura, Yoshiaki Kiso: BACE1 inhibitor peptides: Can an infinitely small kcat value turn the substrate of an enzyme into its inhibitor?, ACS Med Chem Lett., 3(3), 193-197 (2012). 662 Yuri Yamazaki, Koji Tanaka, Benjamin Nicholson, Gordafaried Deyanat-Yazdi, Barbara Potts, Tomoko Yoshida, Akiko Oda, Takayoshi Kitagawa, Sumie Orikasa, Yoshiaki Kiso, Hiroyuki Yasui, Miki Akamatsu, Takumi Chinen, Takeo Usui, Yuki Shinozaki, Fumika Yakushiji, Brian R. Miller, Saskia Neuteboom, Michael Palladino, Kaneo Kanoh, George Kenneth Lloyd, and Yoshio Hayashi: Synthesis and Structure-Activity Relationship Study of 2 Antimicrotubule Agents Phenylahistin Derivatives with a 3 Didehydropiperazine-2,5-dione Structure. J. Med.Chem. 55 (3), 1056–1071 (2012). 663 Yoshinori Hokari, Tetsuo Sekoi, Hiroko Nakano, Akiyoshi Fukamizu, Eisuke Munekata, Yoshiaki Kiso, Hidehito Mukai: Novel neutrophil-activating cryptides hidden in mitochondrial cytochrome c: identification and structure-activity studies. Peptide Science 2011 (K. Sakaguchi, ed.) The Japanese Peptide Society, pp61-62 (2012). 664 Kazuki Saito, Hiromasa Uchimura, Yusam Kim, Itsuki Yasuo, Shizuyo Koide-Yoshida, Takaaki Mizuguchi, Hiroshi Kataoka, Yoshiaki Kiso: Quantitative analyses of disulfide bond formation in proteins using 18O-labeled peptide standards. Peptide Science 2011 (K. Sakaguchi, ed.) The Japanese Peptide Society, pp77-78 (2012). 665 Youhei Sohma, Hitomi Kitamura, Hiroyuki Kawashima, Hironobu Hojo, Kenichi Akaji, Yoshiaki Kiso: Synthesis of O-acyl isopeptide by use of native chemical ligation to efficiently construct hydrophobic polypeptide. Peptide Science 2011 (K. Sakaguchi, ed.) The Japanese Peptide Society, pp137-138 (2012). 666 Sho Konnno, Kiyoko Nakada, Pillaivar Thanigaimalai, RIe Kakiuchi, Takehito Yamamoto, Yuri Yamazaki, Fumika Yakushiji, Kenichi Akaji, Yoshiaki Kiso, Yuko Kawasaki, Ernesto Freire, Yoshio Hayashi: Design, synthesis and evaluation of tripeptidemimetics with aryl ketone as inhibitors of SARS-COV 3CL protease. Peptide Science 2011 (K. Sakaguchi, ed.) The Japanese Peptide Society, pp151-154 (2012). 667 Yoshio Hamada, Harichandra D. Tagad, Yoshiaki Kiso: Design and SAR study of tripeptide BACE1 inhibitors. Peptide Science 2011 (K. Sakaguchi, ed.) The Japanese Peptide Society, pp247-250 (2012). 668 木曽良明、日高興士：ペプチド化学を基盤とした統合創薬科学。化学工業63(4), 258-263 (2012). 669 木曽良明：ペプチド合成と創薬のマイルストーン．遺伝子医学MOOK 21号最新ペプチド合成技術とその創薬研究への応用（木曽良明 編集）メディカル・ドゥ、pp31-33 (2012). 670 相馬洋平・木曽良明: O-アシルイソペプチドの合成. 遺伝子医学MOOK 21号最新ペプチド合成技術とその創薬研究への応用（木曽良明 編集）メディカル・ドゥ、pp43-47 (2012). 671 濵田芳男・木曽良明: アルツハイマー病治療薬をめざしたBACE1阻害剤の設計と合成. 遺伝子医学MOOK 21号最新ペプチド合成技術とその創薬研究への応用（木曽良明 編集）メディカル・ドゥ、pp151- 160(2012). 672 向井秀仁・木曽良明: クリプタイド：タンパク質に隠された新しい生理活性ペプチド - その発見と存在意義および効率的スクリーニング -.遺伝子医学MOOK 21号最新ペプチド合成技術とその創薬研究への応用（木曽良明 編集）メディカル・ドゥ、pp298-304 (2012). 673 Yoshinori Hokari, Tetsuo Seki, Hiroko Nakano,Yuko Matsuo, Akiyoshi Fukarnizu, Eisukc Munekata, Yoshiaki Kiso, Hidchito Mukai: Isolation and Identification of Novel Neutrophil-Activating Cryptides Hidden in Mitochondrial Cytochrome c. Protein Peptide Letters, 19, 680‐687 (2012). 674 Yuri Yamazaki, Makiko Sumikura, Yurika Masuda, Yoshiki Hayashi, Hiroyuki Yasui, Yoshiaki Kiso, Takumi Chinen, Takeo Usui, Fumika Yakushiji, Barbara Potts, Saskia Neuteboom, Michael Palladino, George Kenneth Lloyd, Yoshio Hayashi: Synthesis and structure–activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents. Bioorganic & Medicinal Chemistry 20 (2012) 4279–4289. 675 Yoshio Hamada, Yoshiaki Kiso: The application of bioisosteres in drug design for novel drug discovery: focusing on acid protease inhibitors. Expert Opinion on Drug Discovery,7(10), 903-922 (2012). 676 木曽良明：オピニオン：創薬を牽引するペプチド科学。ファルマシア48(7),623(2012). 677 濵田芳男、木曽良明：分子認識を基盤とする創薬科学研究。ペプチド医薬の最前線（木曽良明、向井秀仁監修）シーエムシー出版、1-8 (2012). 678 相馬洋平、木曽良明：クリックペプチドの合成。ペプチド医薬の最前線（木曽良明、向井秀仁監修）シーエムシー出版、20-24 (2012). 679 向井秀仁、木曽良明：クリプタイド：タンパク質に隠された一群の新しい生理活性ペプチド、クリプタイドの発見。ペプチド医薬の最前線（木曽良明、向井秀仁監修）シーエムシー出版、52-59(2012). 680 濱田芳男、木曽良明：アルツハイマー病治療薬開発の現状。PET Journal, 20, 27-29 (2012). 681 Jeffrey-Tri Nguyen, Yoshiaki Kiso: Human T-cell leukemia virus type I (HTLV-I) retropepsin. Handbook of Proteolytic Enzymes 3rd Edition. 213-217 (2013) 682 Sho Konno, Pillaiyar Thanigaimalai, Takehito Yamamoto, Kiyohiko Nakada, Rie Kakiuchi, Kentaro Takayama, Yuri Yamazaki, Fumika Yakushiji, Kenichi Akaji, Yoshiaki Kiso, Yuko Kawasaki, Shen-En Chen, Ernesto Freire, Yoshio Hayashi: Design and synthesis of new tripeptide-type SARS-CoV 3CL protease inhibitors containing an electrophilic arylketone moiety. Bioorg. Med. Chem. 21(2), 412-424 (2013). 683 Youhei Sohma, Moe Yamasaki, Hiroyuki Kawashima, Atsuhiko Taniguchi, Masayuki Yamashita, Kenichi Akaji, Hidehito Mukai, Yoshiaki Kiso, Comparative Properties of A1–42, A11–42, and [Pyr11]A11–42 Generated from O-Acyl Isopeptides. Bioorg. Med. Chem. Lett., 23 (5), 1326-1329 (2013). 684 Takaaki Mizuguchi, Naho Ohara, Mika Iida, Ryunosuke Ninomiya, Shinji Wada, Yoshiaki Kiso, Kazuki Saito, Kenichi Akaji: Ring size and side-chain orientation of inhibitory cyclic peptides against EGF receptor dimerization. Peptide Science 2012, K. Sugimura (Ed.), The Japanese Peptide Society, pp19-20 (2013). 685 Koushi Hidaka, Yuki Toda, Yuko Tsuda, Yoshiaki Kiso: Oxamide replacement in pseudo-symmetric HIV protease inhibitor involving multiple bridging wate molecules. Peptide Science 2012, K. Sugimura (Ed.), The Japanese Peptide Society, pp271-272 (2013). 686 Tatsuya Hattori, Shunsuke Shirota, Takayuki Marutani, Yoshiaki Kiso, Yoshisuke Nishi, Hidehito Mukai: Functional analysis of mitocryptides with their monoclonal antibodies. Peptide Science 2012, K. Sugimura (Ed.), The Japanese Peptide Society, pp277-278 (2013). 687 Yoshio Hamada, Yoshiaki Kiso: Advances in the identification of -secretase inhibitors. Expert Opinion on Drug Discovery 8 (6), 709-731 (2013). 688 Youhei Sohma, Yoshiaki Kiso: Synthesis of O-Acyl Isopeptides. Chemical Record, 13(2), 218-223 (2013). 689 Pillaiyar Thanigaimalai, Sho Konno, Takehito Yamamoto, Yuji Koiwai, Akihiro Taguchi, Kentaro Takayama, Fumika Yakushiji, Kenichi Akaji, Yoshiaki Kiso, Yuko Kawasaki, Shen-En Chen, Aurash Naser-Tavakolian, Arne Schön, Ernesto Freire, Yoshio Hayashi: Design, synthesis, and biological evaluation of novel dipeptide-type SARS-CoV 3CL protease inhibitors: Structure-activity relationship study. Eur. J. Med. Chem., 65, 436-447 (2013). 690 Hiroyuki Kawashima, Youhei Sohma, Tomoya Nakanishi, Hitomi Kitamura, Hidehito Mukai, Masayuki Yamashita, Kenichi Akaji, Yoshiaki Kiso, A new class of aggregation inhibitor of amyloid- peptide based on an O-acyl isopeptide. Bioorg. Med. Chem. 21 (2013) 6323–6327. 691 Kenji Suzuki, Yoshio Hamada, Jeffrey-Tri Nguyen, Yoshiaki Kiso, Novel BACE1 inhibitors with a non-acidic heterocycle at the P1’ position. Bioorg. Med. Chem. 21 (2013) 6665–6673. 692 Taku Yoshiya, Shugo Tsuda, Masayoshi Mochizuki, Koushi Hidaka, Yuko Tsuda, Yoshiaki Kiso, Susumu Kageyama, Hiromi Ii, Tatsuhiro Yoshiki, Yuji Nishiuchi: A Fluorogenic Probe for γ-Glutamyl Cyclotransferase: Application of an Enzyme-Triggered O-to-N Acyl Migration-Type Reaction. ChemBioChem, 14 (16), 2110–2113 (2013). 693 向井秀仁、木曽良明：クリプタイド：タンパク質に隠された新しい機能ペプチド．バイオサイエンスとインダストリー, 71, 18-22(2013). 694 Takuya Miura, Koushi Hidaka, Yukiko Azai, Keisuke Kashimoto, Yuko Kawasaki, Shen-En Chen, Renato Ferreira de Freitas, Ernesto Freire, Yoshiaki Kiso: Optimization of plasmepsin inhibitor by focusing on similar structural feature with chloroquine to avoid drug-resistant mechanism of Plasmodium falciparum. Bioorg. Med. Chem. Lett., 24, 1698-1701 (2014). 695 Kazuki Saito, Mamiko Nakato, Takaaki Mizuguchi, Shinji Wada, Hiromasa Uchimura, Hiroshi Kataoka, Shigeyuki Yokoyama, Hiroshi Hirota and Yoshiaki Kiso: Application of plug-plug technique to ACE experiments for discovery of peptides binding to a larger target protein: A model study of calmodulin-binding fragments selected from a digested mixture of reduced BSA. Electrophoresis, 35 (6), 846-854 (2014). 696 濱田芳男、木曽良明：アルツハイマー病治療薬開発の現状。PET Journal, (25) 31-34 (2014). END |
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