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Page 1
Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent.
Kurasawa O, Miyazaki T, Homma M, Oguro Y, Imada T, Uchiyama N, Iwai K, Yamamoto Y, Ohori M, Hara H, Sugimoto H, Iwata K, Skene R, Hoffman I, Ohashi A, Nomura T, Cho N. Kurasawa O, et al. Among authors: uchiyama n. J Med Chem. 2020 Feb 13;63(3):1084-1104. doi: 10.1021/acs.jmedchem.9b01427. Epub 2020 Jan 14. J Med Chem. 2020. PMID: 31895562
Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
Nie Z, Feher V, Natala S, McBride C, Kiryanov A, Jones B, Lam B, Liu Y, Kaldor S, Stafford J, Hikami K, Uchiyama N, Kawamoto T, Hikichi Y, Matsumoto S, Amano N, Zhang L, Hosfield D, Skene R, Zou H, Cao X, Ichikawa T. Nie Z, et al. Among authors: uchiyama n. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3662-6. doi: 10.1016/j.bmcl.2013.02.083. Epub 2013 Feb 27. Bioorg Med Chem Lett. 2013. PMID: 23664874 Clinical Trial.
Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist.
Yukawa T, Nara Y, Kono M, Sato A, Oda T, Takagi T, Sato T, Banno Y, Taya N, Imada T, Shiokawa Z, Negoro N, Kawamoto T, Koyama R, Uchiyama N, Skene R, Hoffman I, Chen CH, Sang B, Snell G, Katsuyama R, Yamamoto S, Shirai J. Yukawa T, et al. Among authors: uchiyama n. J Med Chem. 2019 Feb 14;62(3):1167-1179. doi: 10.1021/acs.jmedchem.8b01181. Epub 2019 Feb 4. J Med Chem. 2019. PMID: 30652849
Molecular mechanism and potential target indication of TAK-931, a novel CDC7-selective inhibitor.
Iwai K, Nambu T, Dairiki R, Ohori M, Yu J, Burke K, Gotou M, Yamamoto Y, Ebara S, Shibata S, Hibino R, Nishizawa S, Miyazaki T, Homma M, Oguro Y, Imada T, Cho N, Uchiyama N, Kogame A, Takeuchi T, Kurasawa O, Yamanaka K, Niu H, Ohashi A. Iwai K, et al. Among authors: uchiyama n. Sci Adv. 2019 May 22;5(5):eaav3660. doi: 10.1126/sciadv.aav3660. eCollection 2019 May. Sci Adv. 2019. PMID: 31131319 Free PMC article.
Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase.
Tanaka Y, Kurasawa O, Yokota A, Klein MG, Ono K, Saito B, Matsumoto S, Okaniwa M, Ambrus-Aikelin G, Morishita D, Kitazawa S, Uchiyama N, Ogawa K, Kimura H, Imamura S. Tanaka Y, et al. Among authors: uchiyama n. J Med Chem. 2020 Mar 26;63(6):3215-3226. doi: 10.1021/acs.jmedchem.9b01979. Epub 2020 Mar 16. J Med Chem. 2020. PMID: 32142284
Structure-based design and SAR development of 5,6-dihydroimidazolo[1,5-f]pteridine derivatives as novel Polo-like kinase-1 inhibitors.
Kiryanov A, Natala S, Jones B, McBride C, Feher V, Lam B, Liu Y, Honda K, Uchiyama N, Kawamoto T, Hikichi Y, Zhang L, Hosfield D, Skene R, Zou H, Stafford J, Cao X, Ichikawa T. Kiryanov A, et al. Among authors: uchiyama n. Bioorg Med Chem Lett. 2017 Mar 1;27(5):1311-1315. doi: 10.1016/j.bmcl.2016.10.009. Epub 2016 Oct 15. Bioorg Med Chem Lett. 2017. PMID: 28169164
Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders.
Mikami S, Nakamura S, Ashizawa T, Nomura I, Kawasaki M, Sasaki S, Oki H, Kokubo H, Hoffman ID, Zou H, Uchiyama N, Nakashima K, Kamiguchi N, Imada H, Suzuki N, Iwashita H, Taniguchi T. Mikami S, et al. Among authors: uchiyama n. J Med Chem. 2017 Sep 28;60(18):7677-7702. doi: 10.1021/acs.jmedchem.7b00807. Epub 2017 Sep 5. J Med Chem. 2017. PMID: 28796496
New Series of Potent Allosteric Inhibitors of Deoxyhypusine Synthase.
Tanaka Y, Kurasawa O, Yokota A, Klein MG, Saito B, Matsumoto S, Okaniwa M, Ambrus-Aikelin G, Uchiyama N, Morishita D, Kimura H, Imamura S. Tanaka Y, et al. Among authors: uchiyama n. ACS Med Chem Lett. 2020 Jul 30;11(8):1645-1652. doi: 10.1021/acsmedchemlett.0c00331. eCollection 2020 Aug 13. ACS Med Chem Lett. 2020. PMID: 34345355 Free PMC article.
Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.
Okaniwa M, Hirose M, Arita T, Yabuki M, Nakamura A, Takagi T, Kawamoto T, Uchiyama N, Sumita A, Tsutsumi S, Tottori T, Inui Y, Sang BC, Yano J, Aertgeerts K, Yoshida S, Ishikawa T. Okaniwa M, et al. Among authors: uchiyama n. J Med Chem. 2013 Aug 22;56(16):6478-94. doi: 10.1021/jm400778d. Epub 2013 Aug 1. J Med Chem. 2013. PMID: 23906342
365 results