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Page 1
Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode.
Fujimoto J, Kurasawa O, Takagi T, Liu X, Banno H, Kojima T, Asano Y, Nakamura A, Nambu T, Hata A, Ishii T, Sameshima T, Debori Y, Miyamoto M, Klein MG, Tjhen R, Sang BC, Levin I, Lane SW, Snell GP, Li K, Kefala G, Hoffman ID, Ding SC, Cary DR, Mizojiri R. Fujimoto J, et al. Among authors: sang bc. ACS Med Chem Lett. 2019 Sep 19;10(10):1498-1503. doi: 10.1021/acsmedchemlett.9b00400. eCollection 2019 Oct 10. ACS Med Chem Lett. 2019. PMID: 31620240 Free PMC article.
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. 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
Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure.
Okawa T, Aramaki Y, Yamamoto M, Kobayashi T, Fukumoto S, Toyoda Y, Henta T, Hata A, Ikeda S, Kaneko M, Hoffman ID, Sang BC, Zou H, Kawamoto T. Okawa T, et al. Among authors: sang bc. J Med Chem. 2017 Aug 24;60(16):6942-6990. doi: 10.1021/acs.jmedchem.7b00443. Epub 2017 Aug 3. J Med Chem. 2017. PMID: 28699740
Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist.
Kono M, Ochida A, Oda T, Imada T, Banno Y, Taya N, Masada S, Kawamoto T, Yonemori K, Nara Y, Fukase Y, Yukawa T, Tokuhara H, Skene R, Sang BC, Hoffman ID, Snell GP, Uga K, Shibata A, Igaki K, Nakamura Y, Nakagawa H, Tsuchimori N, Yamasaki M, Shirai J, Yamamoto S. Kono M, et al. Among authors: sang bc. J Med Chem. 2018 Apr 12;61(7):2973-2988. doi: 10.1021/acs.jmedchem.8b00061. Epub 2018 Mar 14. J Med Chem. 2018. PMID: 29510038
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: sang bc. J Med Chem. 2013 Aug 22;56(16):6478-94. doi: 10.1021/jm400778d. Epub 2013 Aug 1. J Med Chem. 2013. PMID: 23906342
Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors.
Kaieda A, Takahashi M, Takai T, Goto M, Miyazaki T, Hori Y, Unno S, Kawamoto T, Tanaka T, Itono S, Takagi T, Hamada T, Shirasaki M, Okada K, Snell G, Bragstad K, Sang BC, Uchikawa O, Miwatashi S. Kaieda A, et al. Among authors: sang bc. Bioorg Med Chem. 2018 Feb 1;26(3):647-660. doi: 10.1016/j.bmc.2017.12.031. Epub 2017 Dec 24. Bioorg Med Chem. 2018. PMID: 29291937
Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds.
Shirai J, Tomata Y, Kono M, Ochida A, Fukase Y, Sato A, Masada S, Kawamoto T, Yonemori K, Koyama R, Nakagawa H, Nakayama M, Uga K, Shibata A, Koga K, Okui T, Shirasaki M, Skene R, Sang B, Hoffman I, Lane W, Fujitani Y, Yamasaki M, Yamamoto S. Shirai J, et al. Bioorg Med Chem. 2018 Jan 15;26(2):483-500. doi: 10.1016/j.bmc.2017.12.006. Epub 2017 Dec 9. Bioorg Med Chem. 2018. PMID: 29262987
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors. 1. Exploration of [5,6]-fused bicyclic scaffolds.
Okaniwa M, Hirose M, Imada T, Ohashi T, Hayashi Y, Miyazaki T, Arita T, Yabuki M, Kakoi K, Kato J, Takagi T, Kawamoto T, Yao S, Sumita A, Tsutsumi S, Tottori T, Oki H, Sang BC, Yano J, Aertgeerts K, Yoshida S, Ishikawa T. Okaniwa M, et al. Among authors: sang bc. J Med Chem. 2012 Apr 12;55(7):3452-78. doi: 10.1021/jm300126x. Epub 2012 Mar 14. J Med Chem. 2012. PMID: 22376051
47 results