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Page 1
Discovery of Second Generation RORγ Inhibitors Composed of an Azole Scaffold.
Kotoku M, Maeba T, Fujioka S, Yokota M, Seki N, Ito K, Suwa Y, Ikenogami T, Hirata K, Hase Y, Katsuda Y, Miyagawa N, Arita K, Asahina K, Noguchi M, Nomura A, Doi S, Adachi T, Crowe P, Tao H, Thacher S, Hashimoto H, Suzuki T, Shiozaki M. Kotoku M, et al. J Med Chem. 2019 Mar 14;62(5):2837-2842. doi: 10.1021/acs.jmedchem.8b01567. Epub 2019 Mar 1. J Med Chem. 2019. PMID: 30776227
Discovery of (1S,2R,3R)-2,3-dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: novel and highly selective aggrecanase inhibitors.
Shiozaki M, Maeda K, Miura T, Kotoku M, Yamasaki T, Matsuda I, Aoki K, Yasue K, Imai H, Ubukata M, Suma A, Yokota M, Hotta T, Tanaka M, Hase Y, Haas J, Fryer AM, Laird ER, Littmann NM, Andrews SW, Josey JA, Mimura T, Shinozaki Y, Yoshiuchi H, Inaba T. Shiozaki M, et al. Among authors: kotoku m. J Med Chem. 2011 Apr 28;54(8):2839-63. doi: 10.1021/jm101609j. Epub 2011 Mar 21. J Med Chem. 2011. PMID: 21417219
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: kotoku m. 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: kotoku m. 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: kotoku m. Sci Rep. 2018 Nov 26;8(1):17374. doi: 10.1038/s41598-018-35783-9. Sci Rep. 2018. PMID: 30478402 Free PMC article.
Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the "Selectivity Pocket", Substrate-Binding Site, and NAD+-Binding Site.
Mellini P, Itoh Y, Elboray EE, Tsumoto H, Li Y, Suzuki M, Takahashi Y, Tojo T, Kurohara T, Miyake Y, Miura Y, Kitao Y, Kotoku M, Iida T, Suzuki T. Mellini P, et al. Among authors: kotoku m. J Med Chem. 2019 Jun 27;62(12):5844-5862. doi: 10.1021/acs.jmedchem.9b00255. Epub 2019 Jun 12. J Med Chem. 2019. PMID: 31144814
Identification of Potent and Selective Inhibitors of Fat Mass Obesity-Associated Protein Using a Fragment-Merging Approach.
Prakash M, Itoh Y, Fujiwara Y, Takahashi Y, Takada Y, Mellini P, Elboray EE, Terao M, Yamashita Y, Yamamoto C, Yamaguchi T, Kotoku M, Kitao Y, Singh R, Roy R, Obika S, Oba M, Wang DO, Suzuki T. Prakash M, et al. Among authors: kotoku m. J Med Chem. 2021 Nov 11;64(21):15810-15824. doi: 10.1021/acs.jmedchem.1c01107. Epub 2021 Nov 3. J Med Chem. 2021. PMID: 34727689
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: kotoku m. 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
30 results