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Structure-based lead optimization to improve potency and selectivity of a novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid series of heparanase-1 inhibitor.
Imai Y, Suzuki R, Wakasugi D, Matsuda D, Tanaka-Yamamoto N, Ohki Y, Mima M, Endo M, Tabata R, Matsuzawa H, Hasegawa Y, Kato S, Sugisaki M, Miyagawa H, Fujimoto N, Fukunaga T, Kato S, Takahashi T, Kakinuma H. Imai Y, et al. Among authors: kakinuma h. Bioorg Med Chem. 2023 Oct 1;93:117460. doi: 10.1016/j.bmc.2023.117460. Epub 2023 Aug 26. Bioorg Med Chem. 2023. PMID: 37660465
The preparation and crystallization of Fab fragments of a family of mouse esterolytic catalytic antibodies and their complexes with a transition-state analogue.
Muranova TA, Ruzheinikov SN, Sedelnikova SE, Moir A, Partridge LJ, Kakinuma H, Takahashi N, Shimazaki K, Sun J, Nishi Y, Rice DW. Muranova TA, et al. Among authors: kakinuma h. Acta Crystallogr D Biol Crystallogr. 2001 Aug;57(Pt 8):1192-5. doi: 10.1107/s0907444901010149. Epub 2001 Jul 23. Acta Crystallogr D Biol Crystallogr. 2001. PMID: 11468416
(1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol (TS-071) is a potent, selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for type 2 diabetes treatment.
Kakinuma H, Oi T, Hashimoto-Tsuchiya Y, Arai M, Kawakita Y, Fukasawa Y, Iida I, Hagima N, Takeuchi H, Chino Y, Asami J, Okumura-Kitajima L, Io F, Yamamoto D, Miyata N, Takahashi T, Uchida S, Yamamoto K. Kakinuma H, et al. J Med Chem. 2010 Apr 22;53(8):3247-61. doi: 10.1021/jm901893x. J Med Chem. 2010. PMID: 20302302
173 results