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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: thacher s. Sci Rep. 2018 Nov 26;8(1):17374. doi: 10.1038/s41598-018-35783-9. Sci Rep. 2018. PMID: 30478402 Free PMC article.
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: thacher 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: thacher 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.
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. Among authors: thacher s. 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 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: thacher 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
New dermatological agents for the treatment of psoriasis.
Thacher SM, Vasudevan J, Tsang KY, Nagpal S, Chandraratna RA. Thacher SM, et al. J Med Chem. 2001 Feb 1;44(3):281-97. doi: 10.1021/jm0000214. J Med Chem. 2001. PMID: 11462969 Review. No abstract available.
Retinoic acid (RA) receptor transcriptional activation correlates with inhibition of 12-O-tetradecanoylphorbol-13-acetate-induced ornithine decarboxylase (ODC) activity by retinoids: a potential role for trans-RA-induced ZBP-89 in ODC inhibition.
Dawson MI, Park JH, Chen G, Chao W, Dousman L, Waleh N, Hobbs PD, Jong L, Toll L, Zhang X, Gu J, Agadir A, Merchant JL, Bai L, Verma AK, Thacher SM, Chandraratna RA, Shroot B, Hill DL. Dawson MI, et al. Among authors: thacher sm. Int J Cancer. 2001 Jan 1;91(1):8-21. doi: 10.1002/1097-0215(20010101)91:1<8::aid-ijc1007>3.0.co;2-h. Int J Cancer. 2001. PMID: 11149424 Free article.
35 results