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RORγt inhibitors suppress T(H)17 responses in inflammatory arthritis and inflammatory bowel disease.
de Wit J, Al-Mossawi MH, Hühn MH, Arancibia-Cárcamo CV, Doig K, Kendrick B, Gundle R, Taylor P, Mcclanahan T, Murphy E, Zhang H, Barr K, Miller JR, Hu X, Aicher TD, Morgan RW, Glick GD, Zaller D, Correll C, Powrie F, Bowness P. de Wit J, et al. Among authors: barr k. J Allergy Clin Immunol. 2016 Mar;137(3):960-3. doi: 10.1016/j.jaci.2015.09.048. Epub 2015 Nov 21. J Allergy Clin Immunol. 2016. PMID: 26611672 No abstract available.
Inhibition of RORγT Skews TCRα Gene Rearrangement and Limits T Cell Repertoire Diversity.
Guo Y, MacIsaac KD, Chen Y, Miller RJ, Jain R, Joyce-Shaikh B, Ferguson H, Wang IM, Cristescu R, Mudgett J, Engstrom L, Piers KJ, Baltus GA, Barr K, Zhang H, Mehmet H, Hegde LG, Hu X, Carter LL, Aicher TD, Glick G, Zaller D, Hawwari A, Correll CC, Jones DC, Cua DJ. Guo Y, et al. Among authors: barr k. Cell Rep. 2016 Dec 20;17(12):3206-3218. doi: 10.1016/j.celrep.2016.11.073. Cell Rep. 2016. PMID: 28009290 Free article.
Identification of an allosteric binding site for RORγt inhibition.
Scheepstra M, Leysen S, van Almen GC, Miller JR, Piesvaux J, Kutilek V, van Eenennaam H, Zhang H, Barr K, Nagpal S, Soisson SM, Kornienko M, Wiley K, Elsen N, Sharma S, Correll CC, Trotter BW, van der Stelt M, Oubrie A, Ottmann C, Parthasarathy G, Brunsveld L. Scheepstra M, et al. Among authors: barr k. Nat Commun. 2015 Dec 7;6:8833. doi: 10.1038/ncomms9833. Nat Commun. 2015. PMID: 26640126 Free PMC article.
Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as RORγt Allosteric Inhibitors for Autoimmune Diseases.
Zhang H, Lapointe BT, Anthony N, Azevedo R, Cals J, Correll CC, Daniels M, Deshmukh S, van Eenenaam H, Ferguson H, Hegde LG, Karstens WJ, Maclean J, Miller JR, Moy LY, Simov V, Nagpal S, Oubrie A, Palte RL, Parthasarathy G, Sciammetta N, van der Stelt M, Woodhouse JD, Trotter BW, Barr K. Zhang H, et al. Among authors: barr k. ACS Med Chem Lett. 2020 Jan 9;11(2):114-119. doi: 10.1021/acsmedchemlett.9b00431. eCollection 2020 Feb 13. ACS Med Chem Lett. 2020. PMID: 32071676 Free PMC article.
Allosteric inhibition of protein tyrosine phosphatase 1B.
Wiesmann C, Barr KJ, Kung J, Zhu J, Erlanson DA, Shen W, Fahr BJ, Zhong M, Taylor L, Randal M, McDowell RS, Hansen SK. Wiesmann C, et al. Among authors: barr kj. Nat Struct Mol Biol. 2004 Aug;11(8):730-7. doi: 10.1038/nsmb803. Epub 2004 Jul 18. Nat Struct Mol Biol. 2004. PMID: 15258570
Discovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors.
Lin J, Lu W, Caravella JA, Campbell AM, Diebold RB, Ericsson A, Fritzen E, Gustafson GR, Lancia DR Jr, Shelekhin T, Wang Z, Castro J, Clarke A, Gotur D, Josephine HR, Katz M, Diep H, Kershaw M, Yao L, Kauffman G, Hubbs SE, Luke GP, Toms AV, Wang L, Bair KW, Barr KJ, Dinsmore C, Walker D, Ashwell S. Lin J, et al. J Med Chem. 2019 Jul 25;62(14):6575-6596. doi: 10.1021/acs.jmedchem.9b00362. Epub 2019 Jul 8. J Med Chem. 2019. PMID: 31199148
Structure-Based Design and Identification of FT-2102 (Olutasidenib), a Potent Mutant-Selective IDH1 Inhibitor.
Caravella JA, Lin J, Diebold RB, Campbell AM, Ericsson A, Gustafson G, Wang Z, Castro J, Clarke A, Gotur D, Josephine HR, Katz M, Kershaw M, Yao L, Toms AV, Barr KJ, Dinsmore CJ, Walker D, Ashwell S, Lu W. Caravella JA, et al. J Med Chem. 2020 Feb 27;63(4):1612-1623. doi: 10.1021/acs.jmedchem.9b01423. Epub 2020 Feb 12. J Med Chem. 2020. PMID: 31971798
Second-generation peptidomimetic inhibitors of protein farnesyltransferase demonstrating improved cellular potency and significant in vivo efficacy.
O'Connor SJ, Barr KJ, Wang L, Sorensen BK, Tasker AS, Sham H, Ng SC, Cohen J, Devine E, Cherian S, Saeed B, Zhang H, Lee JY, Warner R, Tahir S, Kovar P, Ewing P, Alder J, Mitten M, Leal J, Marsh K, Bauch J, Hoffman DJ, Sebti SM, Rosenberg SH. O'Connor SJ, et al. Among authors: barr kj. J Med Chem. 1999 Sep 9;42(18):3701-10. doi: 10.1021/jm9901935. J Med Chem. 1999. PMID: 10479301
Structure of the Brachydanio rerio Polo-like kinase 1 (Plk1) catalytic domain in complex with an extended inhibitor targeting the adaptive pocket of the enzyme.
Elling RA, Fucini RV, Hanan EJ, Barr KJ, Zhu J, Paulvannan K, Yang W, Romanowski MJ. Elling RA, et al. Among authors: barr kj. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2008 Aug 1;64(Pt 8):686-91. doi: 10.1107/S1744309108019623. Epub 2008 Jul 26. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2008. PMID: 18678933 Free PMC article.
301 results