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Page 1
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: steensma 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: steensma 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: steensma 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.
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.
Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M, Sarkisova Y, Sun F, Steffy A, Pferdekamper AC, Li AG, Joseph SB, Kim Y, Liu B, Tuntland T, Cui X, Gray NS, Steensma R, Wan Y, Jiang J, Chopiuk G, Li J, Gordon WP, Richmond W, Johnson K, Chang J, Groessl T, He YQ, Phimister A, Aycinena A, Lee CC, Bursulaya B, Karanewsky DS, Seidel HM, Harris JL, Michellys PY. Marsilje TH, et al. Among authors: steensma r. J Med Chem. 2013 Jul 25;56(14):5675-90. doi: 10.1021/jm400402q. Epub 2013 Jun 26. J Med Chem. 2013. PMID: 23742252
Fragment-based discovery of JAK-2 inhibitors.
Antonysamy S, Hirst G, Park F, Sprengeler P, Stappenbeck F, Steensma R, Wilson M, Wong M. Antonysamy S, et al. Among authors: steensma r. Bioorg Med Chem Lett. 2009 Jan 1;19(1):279-82. doi: 10.1016/j.bmcl.2008.08.064. Epub 2008 Aug 22. Bioorg Med Chem Lett. 2009. PMID: 19019674
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist.
Tagat JR, Steensma RW, McCombie SW, Nazareno DV, Lin SI, Neustadt BR, Cox K, Xu S, Wojcik L, Murray MG, Vantuno N, Baroudy BM, Strizki JM. Tagat JR, et al. Among authors: steensma rw. J Med Chem. 2001 Oct 11;44(21):3343-6. doi: 10.1021/jm0155401. J Med Chem. 2001. PMID: 11585438
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagonist.
Tagat JR, McCombie SW, Nazareno D, Labroli MA, Xiao Y, Steensma RW, Strizki JM, Baroudy BM, Cox K, Lachowicz J, Varty G, Watkins R. Tagat JR, et al. Among authors: steensma rw. J Med Chem. 2004 May 6;47(10):2405-8. doi: 10.1021/jm0304515. J Med Chem. 2004. PMID: 15115380
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.
Galkin AV, Melnick JS, Kim S, Hood TL, Li N, Li L, Xia G, Steensma R, Chopiuk G, Jiang J, Wan Y, Ding P, Liu Y, Sun F, Schultz PG, Gray NS, Warmuth M. Galkin AV, et al. Among authors: steensma r. Proc Natl Acad Sci U S A. 2007 Jan 2;104(1):270-5. doi: 10.1073/pnas.0609412103. Epub 2006 Dec 21. Proc Natl Acad Sci U S A. 2007. PMID: 17185414 Free PMC article.
11 results