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Discovery and SAR of JTE-151: A Novel RORγ Inhibitor for Clinical Development.
Maeba T, Hirata K, Kotoku M, Seki N, Maeda K, Hirashima S, Yamanaka H, Sakai T, Obika S, Hori A, Hara Y, Noji S, Suwa Y, Yokota M, Fujioka S, Yamaguchi T, Katsuda Y, Hata T, Miyagawa N, Arita K, Nomura Y, Taniguchi T, Asahina K, Aratsu Y, Naka Y, Adachi T, Nomura A, Akai S, Oshida SI, Pai S, Crowe P, Bradley E, Steensma R, Tao H, Fenn M, Babine R, Li X, Thacher S, Soeta T, Ukaji Y, Shiozaki M. Maeba T, et al. Among authors: hirashima s. J Med Chem. 2024 Jan 25;67(2):952-970. doi: 10.1021/acs.jmedchem.3c01933. Epub 2024 Jan 3. J Med Chem. 2024. PMID: 38170624
SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious RORγ Inhibitor.
Hirata K, Kotoku M, Seki N, Maeba T, Maeda K, Hirashima S, Sakai T, Obika S, Hori A, Hase Y, Yamaguchi T, Katsuda Y, Hata T, Miyagawa N, Arita K, Nomura Y, Asahina K, Aratsu Y, Kamada M, Adachi T, Noguchi M, Doi S, Crowe P, Bradley E, Steensma R, Tao H, Fenn M, Babine R, Li X, Thacher S, Hashimoto H, Shiozaki M. Hirata K, et al. Among authors: hirashima s. ACS Med Chem Lett. 2015 Nov 4;7(1):23-7. doi: 10.1021/acsmedchemlett.5b00253. eCollection 2016 Jan 14. ACS Med Chem Lett. 2015. PMID: 26819660 Free PMC article.
Ternary complex of human RORγ ligand-binding domain, inverse agonist and SMRT peptide shows a unique mechanism of corepressor recruitment.
Noguchi M, Nomura A, Murase K, Doi S, Yamaguchi K, Hirata K, Shiozaki M, Hirashima S, Kotoku M, Yamaguchi T, Katsuda Y, Steensma R, Li X, Tao H, Tse B, Fenn M, Babine R, Bradley E, Crowe P, Thacher S, Adachi T, Kamada M. Noguchi M, et al. Among authors: hirashima s. Genes Cells. 2017 Jun;22(6):535-551. doi: 10.1111/gtc.12494. Epub 2017 May 11. Genes Cells. 2017. PMID: 28493531 Free article.
Ternary crystal structure of human RORγ ligand-binding-domain, an inhibitor and corepressor peptide provides a new insight into corepressor interaction.
Noguchi M, Nomura A, Doi S, Yamaguchi K, Hirata K, Shiozaki M, Maeda K, Hirashima S, Kotoku M, Yamaguchi T, Katsuda Y, Crowe P, Tao H, Thacher S, Adachi T. Noguchi M, et al. Among authors: hirashima s. Sci Rep. 2018 Nov 26;8(1):17374. doi: 10.1038/s41598-018-35783-9. Sci Rep. 2018. PMID: 30478402 Free PMC article.
Further studies on hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitors toward improved replicon cell activities: benzimidazole and structurally related compounds bearing the 2-morpholinophenyl moiety.
Hirashima S, Oka T, Ikegashira K, Noji S, Yamanaka H, Hara Y, Goto H, Mizojiri R, Niwa Y, Noguchi T, Ando I, Ikeda S, Hashimoto H. Hirashima S, et al. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3181-6. doi: 10.1016/j.bmcl.2007.03.027. Epub 2007 Mar 14. Bioorg Med Chem Lett. 2007. PMID: 17383878
Following the discovery of JTK-109 (1) as a potent inhibitor of hepatitis C virus NS5B RNA-dependent RNA polymerase, [(a) Hirashima, S.; Suzuki, T.; Ishida, T.; Noji, S.; Yata, S.; Ando, I.; Komatsu, M.; Ikeda, S.; Hashimoto, H. ...
Following the discovery of JTK-109 (1) as a potent inhibitor of hepatitis C virus NS5B RNA-dependent RNA polymerase, [(a) Hirashima, …
107 results