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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: babine r. 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: babine r. 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: babine r. Genes Cells. 2017 Jun;22(6):535-551. doi: 10.1111/gtc.12494. Epub 2017 May 11. Genes Cells. 2017. PMID: 28493531 Free article.
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 1. Michael acceptor structure-activity studies.
Dragovich PS, Webber SE, Babine RE, Fuhrman SA, Patick AK, Matthews DA, Lee CA, Reich SH, Prins TJ, Marakovits JT, Littlefield ES, Zhou R, Tikhe J, Ford CE, Wallace MB, Meador JW 3rd, Ferre RA, Brown EL, Binford SL, Harr JE, DeLisle DM, Worland ST. Dragovich PS, et al. Among authors: babine re. J Med Chem. 1998 Jul 16;41(15):2806-18. doi: 10.1021/jm980068d. J Med Chem. 1998. PMID: 9667970
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 2. Peptide structure-activity studies.
Dragovich PS, Webber SE, Babine RE, Fuhrman SA, Patick AK, Matthews DA, Reich SH, Marakovits JT, Prins TJ, Zhou R, Tikhe J, Littlefield ES, Bleckman TM, Wallace MB, Little TL, Ford CE, Meador JW 3rd, Ferre RA, Brown EL, Binford SL, DeLisle DM, Worland ST. Dragovich PS, et al. Among authors: babine re. J Med Chem. 1998 Jul 16;41(15):2819-34. doi: 10.1021/jm9800696. J Med Chem. 1998. PMID: 9667971
Synthesis, SAR exploration, and X-ray crystal structures of factor XIa inhibitors containing an alpha-ketothiazole arginine.
Deng H, Bannister TD, Jin L, Babine RE, Quinn J, Nagafuji P, Celatka CA, Lin J, Lazarova TI, Rynkiewicz MJ, Bibbins F, Pandey P, Gorga J, Meyers HV, Abdel-Meguid SS, Strickler JE. Deng H, et al. Bioorg Med Chem Lett. 2006 Jun 1;16(11):3049-54. doi: 10.1016/j.bmcl.2006.02.052. Epub 2006 Mar 9. Bioorg Med Chem Lett. 2006. PMID: 16524727
Conversion of human-selective PPARalpha agonists to human/mouse dual agonists: a molecular modeling analysis.
Wang M, Winneroski LL, Ardecky RJ, Babine RE, Brooks DA, Etgen GJ, Hutchison DR, Kauffman RF, Kunkel A, Mais DE, Montrose-Rafizadeh C, Ogilvie KM, Oldham BA, Peters MK, Rito CJ, Rungta DK, Tripp AE, Wilson SB, Xu Y, Zink RW, McCarthy JR. Wang M, et al. Among authors: babine re. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6113-6. doi: 10.1016/j.bmcl.2004.09.031. Bioorg Med Chem Lett. 2004. PMID: 15546740
23 results