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Development of methyl isoxazoleazepines as inhibitors of BET.
Hewitt MC, Leblanc Y, Gehling VS, Vaswani RG, Côté A, Nasveschuk CG, Taylor AM, Harmange JC, Audia JE, Pardo E, Cummings R, Joshi S, Sandy P, Mertz JA, Sims RJ 3rd, Bergeron L, Bryant BM, Bellon S, Poy F, Jayaram H, Tang Y, Albrecht BK. Hewitt MC, et al. Among authors: tang y. Bioorg Med Chem Lett. 2015 May 1;25(9):1842-8. doi: 10.1016/j.bmcl.2015.03.045. Epub 2015 Mar 24. Bioorg Med Chem Lett. 2015. PMID: 25851940
Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.
Crawford TD, Tsui V, Flynn EM, Wang S, Taylor AM, Côté A, Audia JE, Beresini MH, Burdick DJ, Cummings R, Dakin LA, Duplessis M, Good AC, Hewitt MC, Huang HR, Jayaram H, Kiefer JR, Jiang Y, Murray J, Nasveschuk CG, Pardo E, Poy F, Romero FA, Tang Y, Wang J, Xu Z, Zawadzke LE, Zhu X, Albrecht BK, Magnuson SR, Bellon S, Cochran AG. Crawford TD, et al. Among authors: tang y. J Med Chem. 2016 Jun 9;59(11):5391-402. doi: 10.1021/acs.jmedchem.6b00264. Epub 2016 May 31. J Med Chem. 2016. PMID: 27219867
GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.
Wang S, Tsui V, Crawford TD, Audia JE, Burdick DJ, Beresini MH, Côté A, Cummings R, Duplessis M, Flynn EM, Hewitt MC, Huang HR, Jayaram H, Jiang Y, Joshi S, Murray J, Nasveschuk CG, Pardo E, Poy F, Romero FA, Tang Y, Taylor AM, Wang J, Xu Z, Zawadzke LE, Zhu X, Albrecht BK, Magnuson SR, Bellon S, Cochran AG. Wang S, et al. Among authors: tang y. J Med Chem. 2018 Oct 25;61(20):9301-9315. doi: 10.1021/acs.jmedchem.8b01225. Epub 2018 Oct 5. J Med Chem. 2018. PMID: 30289257
GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.
Taylor AM, Bailey C, Belmont LD, Campbell R, Cantone N, Côté A, Crawford TD, Cummings R, DeMent K, Duplessis M, Flynn M, Good AC, Huang HR, Joshi S, Leblanc Y, Murray J, Nasveschuk CG, Neiss A, Poy F, Romero FA, Sandy P, Tang Y, Tsui V, Zawadzke L, Sims RJ 3rd, Audia JE, Bellon SF, Magnuson SR, Albrecht BK, Cochran AG. Taylor AM, et al. Among authors: tang y. J Med Chem. 2022 Aug 25;65(16):11177-11186. doi: 10.1021/acs.jmedchem.2c00662. Epub 2022 Aug 5. J Med Chem. 2022. PMID: 35930799
Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains.
Taylor AM, Vaswani RG, Gehling VS, Hewitt MC, Leblanc Y, Audia JE, Bellon S, Cummings RT, Côté A, Harmange JC, Jayaram H, Joshi S, Lora JM, Mertz JA, Neiss A, Pardo E, Nasveschuk CG, Poy F, Sandy P, Setser JW, Sims RJ 3rd, Tang Y, Albrecht BK. Taylor AM, et al. Among authors: tang y. ACS Med Chem Lett. 2015 Mar 25;7(2):145-50. doi: 10.1021/ml500411h. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985289 Free PMC article.
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