学術論文


■2024年■

127. S. Yumura, D. Kitagawa, K. Moritsugu, A. Nakayama, T. Shinada, M. Sawa, T. Kinoshita, Conserved gatekeeper methionine regulates the binding and access of kinase inhibitors to ATP sites of MAP2K1, 4, and 7: Clues for developing selective inhibitors, Bioorg. Med. Chem. Lett.112, 129914 (2024).

126. K. Nishiwaki, S. Nakatani, S. Nakamura, K. Yoshioka, E. Nakagawa, M. Tsuyuguchi, T. Kinoshita, I. Nakanishi, Enhanced inhibitory activity of compounds containing purine scaffolds compared to protein kinase CK2α considering crystalline water, RSC Med. Chem.15, 1274-1282 (2024).

125. S. Hasegawa, M. Yoshida, H. Nagao, H. Sugiyama, M. Sawa, T. Kinoshita, Distinct binding modes of a benzothiazole derivative confer structural bases for increasing ERK2 or p38α MAPK selectivity, Biochem. Biophys. Res. Commun.704, 149707 (2024)



■2023年■

124. K. Nishiwaki, S. Nakamura, K. Yoshioka, E. Nakagwa, S. Nakatani, M. Tsuyuguchi, T. Kinoshita, I. Nakanishi, Design, synthesis and structure-activity relationship studies of protein kinase CK2 inhibitors containing a purine scafold, Chem. Phram. Bull. 71, 558-565 (2023).

123. H. Sugiyama, M. Yoshida, H. Nagao, M. Sawa, T. Kinoshita, Low entropic cost of binding confers high selectivity on an allosteric ERK2 inhibitor, Bioorg. Med. Chem. Lett. 93, 129431 (2023).


■2022年■

122. A. Ikeda, M. Tsuyuguchi, D. Kitagawa, M. Sawa, S. Nakamura, I. Nakanishi, T. Kinoshita, Bivalent binding mode of an amino-pyrazole inhibitor indicates the potentials for CK2a1-selective inhibitors, Biochem. Biophys. Res. Commun.630, 30-35 (2022).

121. M. Yoshida, H. Nagano, H. Sugiyama, M. Sawa, T. Kinoshita, Identification of a novel target site for ATP-independent ERK2 inhibitors, Biochem. Biophys. Res. Commun. 593, 73-78 (2022).



■2021年■

120. H. Nagao, D. Kitagawa, F. Nakajima, M. Sawa, T. Kinoshita, Identification of an allosteric and Smad3-selective inhibitor of p38aMAPK using a substrate-based approach, Bioorg. Med. Chem. Lett. 31, 128056 (2021).


■2020年■

119. Y. Murakawa, S. Valter, H. Barr, N. London, T. Kinoshita, Structural basis for producing selective MAP2K7 inhibitors, Bioorg. Med.Chem. Lett.30, 127546 (2020).

118. M. Tsuyuguchi, T. Nakaniwa, A. Hirasawa, I. Nakanishi, T. Kinoshita, Structural insights for producing CK2a1-specific inhibitors, Bioorg. Med. Chem. Lett. 30, 126837 (2020).

117. N. Furuya, T. Momose, K. Katsuno, N. Fushimi, H. Muranaka, C. Handa, M. Sawa, T. Ozawa, T. Kinoshita, An isoform-selective inhibitor of tropomyosin receptor kinase A behaves as molecular glue, Bioorg. Med. Chem. Lett.30, 126775 (2020).

116. T. Matsumoto, A. Yamano, Y. Murakawa, H. Fukada, M. Sawa, T. Kinoshita, Ensemble structural analyses depict the regulatory mechanism of non-phosphrylated human MAP2K4, Biochem. Biophys. Res. Commun.521, 106-112 (2020).

■2019年■

115. M. Tsuyuguchi, T. Nakaniwa, M. Sawa, I. Nakanishi, T. Kinoshita, A promiscuous kinase inhibitor delineates the conpicuous structural features of protein kinase CK2a1, Acta Cryst. F75, 515-519 (2019).

114. T. Oshima, Y. Niwa, K. Kuwata, A. Srivastava, T. Hyoda, T. Tsuchiya, M. Kumagai, M. Tsuyuguchi, T. Tamaru, A. Sugiyama, N. Ono, N. Zolboot, Y. Aikawa, S. Oishi, A. Nonami, F. Arai, M. Ikeda, T. Kinoshita, S.A. Kay, K. Itami, T.Hirota, Cell-based screen identifies a new potent and highly selective CK2 ihibiotor for modulation of circadian rhythms and cancer cell growth, Sci. Adv.5, eaau9060 (2019).

113. A. Sharaga, E. Olhavang, N. Davidzohn, P. Khoshkenar, N. Germain, K. Shurrush, S. Carvalho, L. Avram, S. Albeck, T. Unger, B. Lefker, C. Subramanyam, R.H. Hudkins, A. Mitchell, Z. Shulman, T. Kinoshita, N. London, Covalent docking identifies a potent and selective MKK7 inhibitor, Cell Chem. Biol. 26, 98-108 (2019).

112. T. Kinoshita, T. Hashimoto, Y. Murakawa, Y. Sogabe, T. Matsumoto, M. Sawa, A microgravity environment improves structural resolution and endows cues for specific inhibition of mitogen-activated protein kinase kinase 7, Int. J. Microgravity Sci. Appl.36, 380102 (2019).

■2018年■

111. C. Shibasaki, S. Arai, R. Shimizu, M. Saeki, T. Kinoshita, A. Ostermann, T.T. Schrader, Y. Kurosaki, T. Sunami, R. Kuroki, M. Adachi, Hydration structures of the human protein kinase CK2a clarified by joint neutron and X-ray crystallography, J, Mol. Biol.430, 5094-5104 (2018).

110. M. Tsuyuguchi, T. Nakaniwa, T. Kinoshita, Crystal structures of human CK2a2 in new crystal forms arising from a subtle difference in salt concentration, Acta Crystallogr. F74, 288-293 (2018).

109. A. Nishiyama, T. Yamada, K. Kita, R. Wang, S. Arai, K. Fukuda, A. Tanimoto, S. Takeuchi, S. Tange, A. Tajima, N. Furuya, T. Kinoshita, S. Yano, Foretinib overcomes entrectinib resistanse associated with the NTRK1 G667C mutation in NTRK1 fusion-positive tumor cells in a brain metastatis model, Clinical Cancer Res. 24, 2357-2369 (2018).

■2017年■

108. T. Kinoshita, T. Hashimoto, Y. Sogabe, H. Fukada, T. Matsumoto, M. Sawa, High-resolution structure discloses the potential for the allosteric regulation of mitogen-activated protein kinase kinase 7, Biochem. Biophys.Res. Commun.493, 313-317(2017).

107. N. Furuya, T. Momose, K. Katsuno, N. Fushimi, H. Muranaka, C. Handa, T. Ozawa, T. Kinoshita, The juxtamembrane region of TrkA kinase is critical for inhibitor selectivity, Bioorg. Med. Chem. Lett. 27, 1233-1236 (2017).

■2016年■ 

106. Y. Sogabe, T. Hashimoto, T. Matsumoto, Y. Kirii, M. Sawa, T. Kinoshita, A crucial role of Cys218 in configuring an unprecedented auto-inhibition form of MAP2K7, Biochem. Biophys. Res. Commun. 473, 476-481 (2016).

105. H. Ohno, D. Minamiguchi, S. Nakamura, K. Shu, S. Okazaki, M. Honda, R. Misu, H. Moriwaki, S. Nakanishi, S. Oishi, T. Kinoshita, I. Nakanishi, N. Fujii, Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors, Bioorg. Med. Chem.24, 1136-1141 (2016).

104. T. Kinoshita, H. Sugiyama, Y. Mori, N. Naruhide, A. Tomonaga, Identification of allosteric ERK2 inhibitors in silico biased screening and competitive binding assay, Boorg. Med. Chem. Lett. 26, 955-958 (2016).

■2015年■

103. S. Sasamura, M. Kobayashi, H. Muramatsu, S. Yoshimura, T. Kinoshita, H. Ohki, K. Okada, Y. Deai, Y. Yamagishi, M. Hashimoto, Bioconversion of FR901459, a novel derivative of cyclosporin A, by Lentzea sp. 7887, J. Antibiotics68, 511-520 (2015).

102. I. Nakanishi, K. Murata, N. Nagata, M. Kurono, T. Kinoshita, M. Yasue, T. Miyazaki, Y. Takei, S. Nakamura, A. Sakurai, N. Iwamoto, K. Nishiwaki, T. Nakaniwa, Y. Sekiguchi, A. Hirasawa, G. Tsujimoto, K. Kitaura, Identification of protein kinase CK2 inhibitors using solvent dipole ordering virtual screening, Eur. J. Med. Chem.96, 396-404 (2015).

101. Y. Sogabe, T. Matsumoto, T. Hashimoto, Y. Kirii, M. Sawa, T. Kinoshita, 5Z-7-oxozeaenol covalently binds to MAP2K7 at Cys218 in an unprecedented manner, Boorg. Med. Chem. Lett. 25, 593-596 (2015).

■2014年■

100. K. Sakai, T. Kinoshita, K. Matsumoto, Hepatocyte growth factor, Reference Module in Biomedical Science 2014, 1-10 (2014).

■2013年■

99. T. Kinoshita, T. Nakaniwa, Y. Sekiguchi, Y. Sogabe, A. Sakurai, S. Nakamura, I. Nakanishi, Crystal structure of human CK2a at 1.06 Å resolution, J. Synchrotron Rad. 20, 974-979 (2013).

■2012年■

98. T. Nakaniwa, H. Fukada, T. Inoue, M. Gouda, R. Nakai, Y. Kirii, M. Adachi, T. Tamada, S. Segawa, R. Kuroki, T. Tada, T. Kinoshita*, Seven cysteine-deficient mutants depict interplay between thermal and chemical stabilities of individual cysteine residues in MAP kinase JNK1, Biochemistry51, 8410-8421 (2012).

97. T. Matsumoto, T. Kinoshita, Y. Kirii, T. Tada, A. Yamano, Crystal and solution structures disclose a putative transient state of mitogen-activated kinase kinase 4, Biochem. Biophys. Res. Commun. 425, 195-200 (2012).

96. Z. Hou, I. Nakanishi, T. Kinoshita, Y. Takei, M. Yasu, Y. Suzuki, S. Nakamura, T. Kure, H. Ohno, K. Murata, K. Kitaura, A. Hirasawa, G. Tsujimoto, S. Oishi, N. Fujii, Structure-based design of novel potent protein kinase CK2 (CK2) inhibitors with phenyl-azole scaffolds, J. Med. Chem.55, 2899-2903 (2012).

95. T. Matsumoto, T. Kinoshita, H. Furukawa, R. Nakai, Y. Kirii, K. Yokota, T. Tada, Crystal structure of non-phosphorylated MAP2K6 in a putative auto-inhibition state, J. Biochem. 151, 541-549 (2012).

94. Y. Takashima, E. Mizohata, S.R. Krungkrai, Y. Fukunishi, T. Kinoshita, T. Sakata, H. Matsumura, J. Krungkrai, T. Horii, T. Inoue, The in silico screening and X-ray analysis of the inhibitor complex of Plasmodium falciparum orotidine-5’-monophosphate decarboxylase, J. Biochem. 152, 133-138 (2012).

■2011年■

93. T. Kinoshita, Y. Sekiguchi, H. Fukada, T. Nakaniwa, T. Tada, S. Nakamura, K. Kitaura, H. Ohno, Y. Suzuki, A. Hirasawa, I. Nakanishi, G. Tsujimoto, A detailed thermodynamic profile of cyclopentyl and isopropyl derivatives binding to CK2 kinase, Mol. Cell. Biochem. 356, 97-105 (2011).

92. T. Kinoshita, K. Doi, H. Sugiyama, S. Kinoshita, M. Wada, S. Naruto, A. Tomonaga, Knowledge-based identification of the ERK2/STAT3 signal pathway as a therapeutic target of type 2 diabetes and drug discovery, Chem. Biol. Drug Des. 78, 471-476 (2011).

91. K. Sakai, T. Nakamura, T. Kinoshita, T. Nakamura, K. Matsumoto, HGF-antagonists: structure, activities, and anti-cancer approach, Current Signal Transduction Therapy6, 191-199 (2011).

90. Y. Sogabe, T. Kitatani, A. Yamaguchi, T. Kinoshita, H. Adachi, K. Takano, T. Inoue, Y. Mori, H. Matsumura, T. Sakamoto, T. Tada, High-resolution structure of exo-arabinanase from Penicillium Chrysogenum, Acta Crystallogr.D67, 415-422 (2011).

■2010年以前■

89. T. Matsumoto, T. Kinoshita, Y. Kirii, K. Yokota, K. Hamada, T. Tada, Crystal structures of MKK4 kinase domain reveal that substrate peptide binds to an allosteric site and induces an auto-inhibition state, Biochem. Biophys. Res. Commun. 400, 369-373 (2010).

88. X. Yang, T. Kinoshita, M. Gouda, K. Yokota, T. Tada, A silent mutation allows efficient production of active human Frk tyrosine kinase in Escherichia coli, Biosci. Biotechnol. Biochem. 74, 125-128 (2010).

87. N. Miyano, T. Kinoshita, R. Nakai, Y. Kirii, K. Yokota, T. Tada, Structure Basis for the inhibitor recognition of human Lyn kinase domain, Bioorg. Med. Chem. Lett. 19, 6557-6560 (2009).

86. T. Tamada, T. Kinoshita, K. Kurihara, M. Adachi, T. Ohhara, K. Imai, R. Kuroki, T. Tada, Combined high-resolution neutron and x-ray analysis of inhibited elastase confirms the active-site oxyanion hole but rules against a low-barrier hydrogen bond, J. Am. Chem. Soc. 131, 11033-11040 (2009).

85. Y. Sekiguchi, T. Nakaniwa, T. Kinoshita, I. Nakanishi, K. Kitaura, A. Hirasawa, G. Tsujimoto, T. Tada, Structural insight into human CK2a in complex with the potent inhibitor ellagic acid, Bioorg. Med. Chem. Lett. 19, 2920-2923 (2009).

84. T. Nakaniwa, T. Kinoshita, Y. Sekiguchi, T. Tada, I. Nakanishi, K. Kitaura, Y. Suzuki, H. Ohno, A. Hirasawa, G. Tsujimoto, Structure of human protein kinase CK2a2 with a potent indazole-derivative inhibitor, Acta Crystallogr. F65, 75-79 (2009).

83. T. Kinoshita, I. Yoshida, S. Nakae, K. Okita, M. Gouda, M. Matsubara, K. Yokota, H. Ishiguro, T. Tada, Crystal structure of human mono-phosphorylated ERK1 at Tyr204, Biochem. Biopys. Res. Commun. 377, 1123-1127 (2008).

82. T. Kinoshita, T. Tada, I. Nakanishi, Conformational change of adenosine deaminase during ligand-exchange in a crystal, Biochem. Biopys. Res. Commun. 373, 53-57 (2008).

81. T. Kinoshita, N. Miyano, R. Nakai, K. Yokota, H. Ishiguro, T. Tada, Protein purification and preliminary crystallographic analysis of human Lyn tyrosine kinase, Protein Expr. Purif. 58, 318-324 (2008).

80. T. Kinoshita, T. Tamada, K. Imai, K. Kurihara, T. Ohhara, T. Tada, R. Kuroki, Crystallization of porcine pancreatic elastase and preliminary neutron diffraction experiment, Acta Cryst. F63, 315-317 (2007).

79. M. Ohori, T. Kinoshita, S. Yoshimura, M. Warizaya, H. Nakajima, H. Miyake, Role of a cysteine residue in the active site of ERK and the MAPKK family, Biochem. Biophys. Res. Commun. 353, 633-637 (2007).

78. T. Kitatani, Y. Nakamura, K. Wada, T. Kinoshita, M. Tamoi, S. Shigeoka, T. Tada, Structure of apo-glyceraldehyde-3-phosphate dehydrogenase from Synechococcus PCC7942, Acta Cryst. F62, 727-730 (2006).

77. T. Kinoshita, A. Yamaguchi, T. Tada, Tris(hydroxymethyl)aminomethane induces conformational change and crystal-packing contraction of porcine pancreatic elastase, Acta Cryst. F62, 623-626 (2006).

76. T. Kinoshita, M. Matsubara, H. Ishiguro, K. Okita, T. Tada, Structure of human Fyn kinase domain complexed with staurosporine, Biochem. Biophys. Res. Commun. 346, 840-844 (2006).

75. T. Kitatani, Y. Nakamura, K. Wada, T. Kinoshita, S. Shigeoka, T. Tada, Structure of NADP-dependent glyceraldehyde-3-phosphate dehydrogenase from Synechococcus PCC7942 complexed with NADP, Acta Cryst. F62, 315-319 (2006).

74. M. Kuno, N. Seki, S. Tsujimoto, I. Nakanishi, T. Kinoshita, K. Nakamura, T. Terasaka, N. Nishio, A. Sato, T. Fujii, Anti-inflammatory activity of non-nucleoside adenosine deaminase inhibitor FR234938, Eur. J. Pharmacol. 534, 241-249 (2006).

73. H. Adachi, A. Niino, T. Kinoshita, M. Warizaya, R. Maruki, K. Takano, H. Matsumura, T. Inoue, S. Murakami, Y. Mori, T. Sasaki, Solution-stirring method improves crystal quality of human triosephosphate isomerase, J. Biosci. Bioeng. 101, 83-86 (2006).

72. J. Ishida, H. Yamamoto, Y. Kido, K. Kamijo, K. Murano, H. Miyake, M. Okubo, T. Kinoshita, M. Warizaya, A. Iwashita, K. Mihara, N. Matsuoka, K. Hattori, Discovery of potent and selective PARP-1 and PARP-2 inhibitors: SBDD analysis via a combination of X-ray structural study and homology modeling, Bioorg. Med. Chem.14, 1378-1390 (2006).

71. T. Kinoshita, M. Warizaya, M. Ohori, K. Sato, M. Neya, T. Fujii, Crystal structure of human ERK2 complexed with a pyrazolo[3,4c]pyridazine derivative, Bioorg. Med. Chem. Lett. 16, 55-58 (2006).

70. A. Iwashita, K. Hattori, H. Yamamoto, J. Ishida, Y. Kido, K. Kamijo, K. Murano, H. Miyake, T. Kinoshita, M. Warizaya, M. Ohkubo, N. Matsuoka, S. Mutoh, Discovery of quinazolinone and quinoxaline derivatives as potent and selective poly(ADP-ribose) polymerase-1/2 inhibitors, FEBS Lett. 579, 1389-1393, (2005).

69. H. Adachi, A. Niino, S. Murakami, K. Takano, H. Matsumura, T. Kinoshita, M. Warizaya, T. Inoue, Y. Mori and T. Sasaki, Protein crystallization by combining laser irradiation and solution-stirring techniques, Jpn. J. Appl. Phys. 44, 1365-1366, (2005).

68. T. Kinoshita, R. Maruki, M. Warizaya, H. Nakajima and S. Nishimura, Structure of a high-resolution crystal form of human triosephosphate isomerase: improvement of crystals using the gel-tube method, Acta Cryst. F61, 346-349, (2005).

67. H. Adachi, K. Takano, A. Niino, H. Matsumura, T. Kinoshita, M. Warizaya, Y. Mori, T. Sasaki, Solution stirring initiates nucleation and improves the quality of adenosine deaminase crystals, Acta Cryst. D61, 759-762, (2005).

66. T. Terasaka, K. Tsuji, T. Kato, I. Nakanishi, T. Kinoshita, Y. Kato, M. Kuno, T. Inoue, K. Tanaka and K. Nakamura, Rational design of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors: predicting enzyme conformational change and metabolism, J. Med. Chem. 48, 4750-4753, (2005).

65. T. Kinoshita, I. Nakanishi, T. Terasaka, M. Kuno, N. Seki, M. Warizaya, H. Matsumura, T. Inoue, K. Takano, H. Adachi, Y. Mori, T. Fujii, Structural basis of compound recognition by adenosine deaminase, Biochemistry. 44, 10562-10569, (2005).

64. T. Kinoshita, T. Kitatani, M. Warizaya, T. Tada, Structure of the complex of porcine pancreatic elastase with a trimacrocyclic peptide inhibitor FR901451, Acta Cryst. F61, 808-811, (2005).

63. M. Ohori, T. Kinoshita, M. Okubo, K. Sato, A. Yamazaki, H. Arakawa, S. Nishimura, N. Inamura, H. Nakajima, M. Neya, T. Fujii, Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex, Biochem. Biophys. Res. Commun. 336, 357-363, (2005).

62. M. Kobayashi, S. Yoshimura, T. Kinoshita, M. Hashimoto, S. Hashimoto, S. Takase, A. Fujie, M. Hino, Y. Hori, FR207944, an Antifungal Antibiotic from Chaetomium sp. No.217. II. Isolation and Structure Elucidation, Biosci. Biotechnol. Biochem. 69, 1029-1032 (2005).

61. Y. Ohtsu, S. Yoshimura, T. Kinoshita, S. Takase, H. Nakajima, The novel gluconeogenesis inhibitor FR225654 that originates from Phoma sp. No. 00144 II. Structure determination, J. Antibiot. 58, 479-482 (2005).

60. B. Sato, H. Nakajima, T. Fujita, S. Takase, S. Yoshimura, T. Kinoshita, H. Terano, FR177391, a new anti-hyperlipidemic agent from Serratia, J. Antibiot. 58, 634-639 (2005).

59. A. Otaka, J. Watanabe, A. Yukimasa, Y. Sasaki, H. Watanabe, T. Kinoshita, S. Oishi, H. Tamamura, N. Fujii, SmI2-mediated reduction of ,-difluoro-,-enoates with application to the synthesis of functionalized (Z)-fluoroalkene-type dipetide isosteres, J. Org. Chem. 69, 1634-1645 (2004).

58. T. Kinoshita, T. Tsutsumi, R. Maruki, M. Warizaya, Y. Ishii, T. Fujii, Cloning, expression, purification, crystallization and preliminary diffraction analysis of the C-terminal catalytic domain of human poly(ADP-ribose) polymerase, Acta Cryst. D60, 109-111 (2004).

57. T. Terasaka, T. Kinoshita, M. Kuno, I. Nakanishi, A highly potent non-nucleotide adenosine deaminase inhibitor: efficient drug discovery by intentional lead hybridization, J. Am. Chem. Soc. 126, 34-35 (2004).

56. T. Kinoshita, I. Nakanishi, M. Warizaya, A. Iwashita, Y. Kido, K. Hattori, T. Fujii, Inhibitor-induced structural change of the active site of human poly(ADP-ribose) polymerase, FEBS Lett. 556, 43-46 (2004).

55. M. Warizaya, T. Kinoshita, A. Kato, H. Nakajima, T. Fujii, Cloning, expression, purification, crystallization and preliminary diffraction analysis of human liver glyceraldehyde-3-phophate dehydrogenase, Acta Cryst. D60, 567-568 (2004).

54. H. Adachi, H. Matsumura, A. Niino, K. Takano, T. Kinoshita, M. Warizaya, T. Inoue, Y. Mori, T. Sasaki, Improving the quality of protein crystals using stirring crystallization, Jpn. J. Appl. Phys. 43, L522-L525 (2004).

53. T. Terasaka, H. Okumura, K. Tsuji, T. Kato, I. Nakanishi, T. Kinoshita, Y. Kato, M. Kuno, N. Seki, Y. Naoe, T. Inoue, K. Tanaka, K. Nakamura, Structure-based design and synthesis of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors, J. Med. Chem. 47, 2728-2731 (2004).

52. H. Adachi, H. Matsumura, A. Niino, K. Takano, T. Kinoshita, M. Warizaya, T. Inoue, Y. Mori, T. Sasaki, Generation of protein crystals using a solution-stirring technique, Jpn. J. Appl. Phys. 43, L762-L764 (2004).

51. T. Terasaka, T. Kinoshita, M. Kuno, N. Seki, K. Tanaka, I. Nakanishi, Structure-based design, synthesis, and structure-activity relationship studies of novel non-nucleoside adenosine deaminase inhibitors, J. Med. Chem. 47, 3730-3743 (2004).

50. K. Hattori, Y. Kido, H. Yamamoto, J. Ishida, K. Kamijo, K. Murano, M. Ohkubo, T. Kinoshita, A. Iwashita, K. Mihara, S. Yamazaki, N. Matsuoka, Y. Teramura, H. Miyake, Rational approaches to discovery of orally active and brain penetrable PARP inhibitors, J. Med. Chem. 47, 4151-4154, (2004).

49. M. Warizaya, T. Kinoshita, M. Yamaoka, T. Shibata, N. Saito, H. Nakajima and T. Fujii, Expression, purification, crystallization and preliminary X-ray diffraction studies of human liver regucalcin, Acta Cryst. D60, 2019-2021, (2004).

48. A. Niino, H. Adachi, K. Takano, H. Matsumura, T. Kinoshita, M. Warizaya, T. Inoue, Y. Mori and T. Sasaki, Control of protein crystal nucleation and growth using stirring solution, Jpn. J. Appl. Phys. 43, L1442-L1444, (2004).

47. T. Kinoshita, I. Nakanishi, A. Sato, T. Tada, True interaction mode of porcine pancreatic elastase with FR136706, a potent peptidyl inhibitor, Bioorg. Med. Chem. Lett. 13, 21-24 (2003).

46. T. Kinoshita, N. Nishio, I. Nakanishi, A. Sato, T. Fujii, Structure of bovine adenosine deaminase complexed with 6-hydroxyl-1,6-dihydropurine riboside, Acta Cryst. D59, 299-303 (2003).

45. T. Terasaka, I. Nakanishi, K. Nakamura, Y. Eikyu, T. Kinoshita, N. Nishio, A. Sato, M. Kuno, N. Seki, K. Sakane, Structure-based de novo design of non-nucleoside adenosine deaminase inhibitors, Bioorg. Med. Chem. Lett. 13, 1115-1118 (2003).

44. T. Kinoshita, M. Ataka, M. Warizaya, M. Neya, T. Fujii, Improving quality and harvest period of protein crystals for structure based drug design: effects of a gel and a magnetic field on bovine adenosine deaminase crystals, Acta Cryst. D59, 1333-1335 (2003).

43. H. Mori, Y. Urano, T. Kinoshita, S. Yoshimura, S. Takase, M. Hino, FR235222, a fungal metabolite, is a novel immunosuppressant that inhibits mammalian histone deacetylase III. Structure determination, J. Antibiotics56, 181-185 (2003).

42. K. Wada, T. Tada, Y. Nakamura, T. Kinoshita, M. Tamoi, S. Shigeoka, K. Nishimura, Crystallization and preliminary X-ray diffraction studies of catalase-peroxidase from Synechococcus PCC 7942, Acta Cryst. D58, 157-159 (2002).

41. T. Kinoshita, H. Miyake, T. Fujii, S. Takakura, T. Goto, The structure of human recombinant aldose reductase complexed with the potent inhibitor zenarestat, Acta Cryst. D58, 622-626 (2002).

40. K. Tsubaki, H. Tanaka, T. Kinoshita, K. Fuji, Synthesis of the proton-ionizable lariat crown ether and chiral recognition of primary amines, Tetrahedron58, 1679-1684 (2002).

39. K. Tsubaki, H. Tanaka, T. Furuta, K. Tanaka, T. Kinoshita, K. Fuji, Use of meso-ternaphthalene derivatives: linear recognition of the ,-diamines by homoditopic receptors. Synthesis of the proton-ionizable lariat crown ether and chiral recognition of primary amines, Tetrahedron58, 5611-5617 (2002).

38. A. Otaka, F. Katagiri, T. Kinoshita, Y. Odagaki, O. Shinya, H. Tamamura, N. Hamanaka, N. Fujii, Regio- and stereoselective synthesis of (E)-alkene trans-Xaa-Pro dipeptide mimetics utilizing organocopper-mediated anti-Sn2' reactions, J. Org. Chem. 67, 6152-6161 (2002).

37. K. Tsubaki, K. Mukoyoshi, H. Morikawa, T. Kinoshita, K. Fuji, Enantiometric recognition of amino acids using a chiral spiropyran derivative, Chirality14, 713-715 (2002).

36. Y. Nakamura, T. Tada, K. Wada, T. Kinoshita, M. Tamoi, S. Shigeoka, K. Nishimura, Purification, crystallization and preliminary X-ray diffraction analysis of the fructose-1,6/sedoheptulose- 1,7-bisphosphatase of Synechococcus PCC 7942, Acta Cryst. D57, 454-456 (2001).

35. Y. Nakamura, T. Tada, K. Wada, T. Kinoshita, M. Tamoi, S. Shigeoka, K. Nishimura, Crystallization and preliminary X-ray diffraction analysis of NADP-dependent glyceraldehide-3-dehydrogenase of Synechococcus PCC 7942, Acta Cryst. D57, 879-881 (2001).

34. K. Tsubaki, T. Otsubo, T. Kinoshita, M. Kawada, K. Fuji, The first example for cycloenatiomeric hexahomooxacalix[3]arenes, Chem. Pharm. Bull. 49, 507-509 (2001).

33. K. Tsubaki, T. Morimoto, T. Otsubo, T. Kinoshita, K. Fuji, Synthesis, structure, and ion-binding properties of new tetraoxacalix[3]arenes, J. Org. Chem. 66, 4083-4086 (2001).

32. T. Kinoshita, T. Tada, Y. Saito, Y. Ishii, A. Sato, M. Murata, Crystallization and preliminary X-ray analysis of cephalosporin C acylase from Pseudomonas sp. strain N176, Acta Cryst. D56, 458-459 (2000).

31. I. Nakanishi, T. Kinoshita, A. Sato, T. Tada, Structure of porcine pancreatic elastase complexed with FR901277, a novel macrocyclic inhibitor of elastases, at 1.6 Å resolution, Biopolymers53, 434-445 (2000).

30. S. Tabuchi, H. Ito, H. Sogabe, M. Kuno, T. Kinoshita, I. Katumi, N. Yamamoto, H. Mitsui, Y. Satoh, Dual CCK-A and CCK-B receptor antagonists (II). Preparation and structure activity relationships of 5-alkyl-9-methyl-1,4-benzodiazepines and discovery of FR208419, Chem. Pharm. Bull.(Tokyo). 48, 1-15, (2000).

29. S. Yoshimura, B. Sato, T. Kinoshita, S. Takase, H. Terano, A new antimitotic substance, FR182877, J. Antibiotics53, 615-622 (2000).

28. A. Otaka, E. Mitsuyama, T. Kinoshita, H. Tamamura, N. Fujii, Stereoselective synthesis of CF2-substituted phosphothreonine mimetics and their incorporation into peptides using newly developed deprotection procedures, J. Org. Chem. 65, 4888-4899 (2000).

27. K. Tsubaki, H. Tanaka, T. Furuta, T. Kinoshita, K. Fuji, Recognition of the chain length of ,-diamines by a meso-ternaphthalene derivative with two crown ethers, Tetrahedron Lett. 41, 6089-6093 (2000).

26. T. Kawabata, J. Chen, H. Suzuki, Y. Nagae, T. Kinoshita, S.Chancharunee, K. Fuji, Memory of chirality in diastereoselective α-alkylation of isoleucine and allo-isoleucine derivatives, Org. Lett. 2, 3883-3885 (2000).

25. T. Kinoshita, N. Nishio, A. Sato, M. Murata, Crystallization and preliminary analysis of bovine adenosine deaminase, Acta Cryst.D55, 2031-2032 (1999).

24. I. Nakanishi, T. Kinoshita, T. Tada, T. Fujita, H. Hatanaka, A. Sato, Molecular structure of FR901277, a novel inhibitor of human leukocyte elastase, and its binding mode simulation, Bioorg. Med. Chem. Lett. 9, 2397-2402 (1999).

23. A. Akahane, H. Katayama, T. Mitsunaga, T. Kato, T. Kinoshita, Y. Kita, T. Kusunoki T. Terai, K. Yoshida, Y. Shiokawa, Discovery of 6-oxo-3-(2-phenylpyrazolo[1,5alfa]pyridin-3-yl)-1(6H)-pyridazine-butanoic acid (FK838) : A novel non-xanthine adenosine A1 receptor antagonist with potent diruretic activity, J. Med. Chem. 42, 779-783 (1999).

22. S. Kuroda, A. Akahane, H. Itani, S. Nishimura, K. Durkin, T. Kinoshita, Y. Tenda, K. Sakane, Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist, Bioorg. Med. Chem. Lett. 9, 1979-1984 (1999).

21. S. Kuroda, A. Akahane, H. Itani, S. Nishimura, K. Durkin, T. Kinoshita, K. Sakane, Synthesis of the water-soluble adenosine A1 receptor antagonist FR166124 through a novel sequential Horner-Emmons/isomerization reaction, Tetrahedron55, 10351-10364 (1999).

20. K. Fuji, K. Tsubaki, K. Tanaka, N. Hayashi, T. Otsubo, T. Kinoshita, Visualization of molecular length of ,-diamines and temperature by a receptor based on phenolphthalein and crown ether, J. Am. Chem. Soc. 121, 3807-3808 (1999).

19. K. Tsubaki, Y. Murata, K. Komatsu, T. Kinoshita, K. Fuji, The supramolecular structure of 1,4-bis(9-fluorenyl)-1,4-dihydro[60] fullerene with hexahomotrioxacalix[3]arene in the solid state, Heterocycles51, 2553-2556 (1999).

18. A. Tanaka, T. Terasawa, H. Hagihara, T. Kinoshita, Y. Sakuma, N. Ishibe, M. Sawada, H. Takasugi, H. Tanaka, Synthesis, X-ray crystal structure, and biological activity of FR186054, a novel, potent, orally active inhibitor of acyl-CoA: cholesterol O-acyltransferase (ACAT) bearing a pyrazol ring, Bioorg. Med. Chem. Lett.8, 81-86 (1998).

17. K. Fuji, T. Oka, T. Kawabata, T. Kinoshita, The first synthesis of an optically active molecular bevel gear with only two cogs on each wheel, Tetrahedron Lett. 39, 1373-1376 (1998).

16. K. Tsubaki, T. Otsubo, K. Tanaka, K. Fuji, T. Kinoshita, Stepwise construction of some hexahomooxacalix[3]arenes and their conformations in solid state, J. Org. Chem. 63, 3260-3265 (1998).

15. K. Tsubaki, K. Tanaka, T. Kinoshita, K. Fuji, Complexation of C60 with hexahomooxacalix[3]arenes and supramolecular structures of complexes in the solid state, Chem. Commun, 895-896 (1998).

14. K. Fuji, M. Sakurai, T. Kinoshita, T. Kawabata, Palladium-catalyzed asymmetric reduction of allylic esters with a new chiral monodentate ligand, 8-diphenylphosphino-8'-mothoxy-1,1'-binaphthyl, Tetrahedron Lett. 39, 6323-6326 (1998).

13. G. Kurisu, T. Kinoshita, A. Sugimoto, A. Nagara, Y. Kai, N. Kasai, S. Harada, Structure of the zinc endoprotease from Streptomyces caespitosus, J. Biochem. 121, 304-308 (1997).

12. K. Fuji, M. Sakurai, T. Kinoshita, T. Tada, A. Kuroda, T. Kawabata, Assessment of the activity of 8-diphenylphoosphosphino-8'-mothoxy-1,1'-binaphthyl as a ligand for palladium-catalyzed reactions, Chem. Pharm. Bull. 45, 1524-1526 (1997).

11. D. Barrett, H. Sasaki, H. Tsutsumi, T. Kinoshita, K. Sakane, Alkylation of 1-[N-(hydroxymethyl)-N-methylamino]-4-quinolones. An improved preparation of intermediates for novel potent tricyclic quinolone antibacterial agents, Bull. Chem. Soc. Jpn. 69, 1371-1376 (1996).

10. D. Barrett, H. Sasaki, T. Kinoshita, A. Fujikawa, K. Sakane, A novel synthesis of the pyrazolo[1,5-a]quinoline ring system. New N1-C2 bridged DNA gyrase inhibitors via a novel tandem 1,4-conjugate addition-Michael [3+2] annulation process, Tetrahedron 52, 8471-8488 (1996), citation: 12.

9. D. Barrett, H. Sasaki, T. Kinoshita, K. Sakane, A novel [3+2] annulation: synthesis and X-ray crystallographic structure of a novel tetrahydropyrazolo[1,5-a]quinoline, an intermediate towards new tricyclic quinolone antibacterials, Chem. Commun., 61-62 (1996).

8. M. Ohkubo, A. Kuno, K. Katsuta, Y. Ueda, K. Shirakawa, H. Nakanishi, I. Nakanishi, T. Kinoshita, H. Takasugi, Studies on cerebral protective agents. IX. Synthesis of novel 1,2,3,4-tetrahydroisoquinolines as N-Methyl-D-aspartate antagonists, Chem. Pharm. Bull. 44, 95-102 (1996).

7. M. Ohkubo, A. Kuno, K. Katsuta, Y. Ueda, K. Shirakawa, H. Nakanishi, T. Kinoshita, H. Takasugi, Studies on Cerebral Protective Agents. X. Synthesis and evaluation of anticonvulsant activities for novel 4,5,6,7-tetrahydrothieno[3,3-c]pyridines and related compounds, Chem. Pharm. Bull. 44, 778-784 (1996).

6. K. Fuji, M. Sakurai, N. Tohkai, A. Kuroda, T. Kawabata, Y. Fukazawa, T. Kinoshita, T. Tada, Unexpectically facile racemization of 8-diphenylphosphinoyl-8'-methoxy-1.1'-binaphthyl, Chem. Commun., 1609-1610 (1996).

5. S. Harada, T. Kinoshita, N. Kasai, S., Tsunasawa, F. Sakiyama, Complete amino acid sequence of a zinc matalloendoprotease from Streptomyces caespitosus, Eur. J. Biochem. 233, 683-686 (1995).

4. D. Barrett, H. Tsutsumi, T. Kinoshita, M. Murata, K. Sakane, Synthesis of new 1,8-bridged tricyclic quinolones by a novel intramolecular arylation of N-1 tethered malonamides, Tetrahedron51, 11125-11140 (1995).

3. K. Hattori, M. Nagano, T. Kato, I. Nakanishi, K. Imai, T. Kinoshita, K. Sakane, Asymmetric synthesis of FR165914: a novel 3-adrenergic agonist with a benzocycloheptane structure, Bioorg. Med. Chem. Lett. 5, 2821-282 (1995).

2. Y. Sato, T. Matsuo, H. Sogabe, H. Itoh, T. Tada, T. Kinoshita, K. Yoshida, T. Takaya, Studies on a novel, potent and orally effective cheolecytokinin. An antagonist, FK-480. Synthesis and structure-activity relationships of FK-480 and related compounds, Chem. Pharm. Bull.42, 2071-2083 (1994).

1. S. Harada, K. Kitadokoro, T. Kinoshita, Y. Kai, N. Kasai, Crystallization and main-chain structure of neutral protease from Streptomyces caespitosus, J. Biochem.110, 46-49 (1991).