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Page 1
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: bryant bm. 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
Targeting MYC dependence in cancer by inhibiting BET bromodomains.
Mertz JA, Conery AR, Bryant BM, Sandy P, Balasubramanian S, Mele DA, Bergeron L, Sims RJ 3rd. Mertz JA, et al. Among authors: bryant bm. Proc Natl Acad Sci U S A. 2011 Oct 4;108(40):16669-74. doi: 10.1073/pnas.1108190108. Epub 2011 Sep 26. Proc Natl Acad Sci U S A. 2011. PMID: 21949397 Free PMC article.
Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.
Gehling VS, Hewitt MC, Vaswani RG, Leblanc Y, Côté A, Nasveschuk CG, Taylor AM, Harmange JC, Audia JE, Pardo E, Joshi S, Sandy P, Mertz JA, Sims RJ 3rd, Bergeron L, Bryant BM, Bellon S, Poy F, Jayaram H, Sankaranarayanan R, Yellapantula S, Bangalore Srinivasamurthy N, Birudukota S, Albrecht BK. Gehling VS, et al. Among authors: bryant bm. ACS Med Chem Lett. 2013 Jul 16;4(9):835-40. doi: 10.1021/ml4001485. eCollection 2013 Sep 12. ACS Med Chem Lett. 2013. PMID: 24900758 Free PMC article.
Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition.
Ghosh S, Taylor A, Chin M, Huang HR, Conery AR, Mertz JA, Salmeron A, Dakle PJ, Mele D, Cote A, Jayaram H, Setser JW, Poy F, Hatzivassiliou G, DeAlmeida-Nagata D, Sandy P, Hatton C, Romero FA, Chiang E, Reimer T, Crawford T, Pardo E, Watson VG, Tsui V, Cochran AG, Zawadzke L, Harmange JC, Audia JE, Bryant BM, Cummings RT, Magnuson SR, Grogan JL, Bellon SF, Albrecht BK, Sims RJ 3rd, Lora JM. Ghosh S, et al. Among authors: bryant bm. J Biol Chem. 2016 Jun 17;291(25):13014-27. doi: 10.1074/jbc.M115.708560. Epub 2016 Apr 7. J Biol Chem. 2016. PMID: 27056325 Free PMC article.
Regulation of GLI Underlies a Role for BET Bromodomains in Pancreatic Cancer Growth and the Tumor Microenvironment.
Huang Y, Nahar S, Nakagawa A, Fernandez-Barrena MG, Mertz JA, Bryant BM, Adams CE, Mino-Kenudson M, Von Alt KN, Chang K, Conery AR, Hatton C, Sims RJ 3rd, Fernandez-Zapico ME, Wang X, Lillemoe KD, Fernández-Del Castillo C, Warshaw AL, Thayer SP, Liss AS. Huang Y, et al. Among authors: bryant bm. Clin Cancer Res. 2016 Aug 15;22(16):4259-70. doi: 10.1158/1078-0432.CCR-15-2068. Epub 2016 May 11. Clin Cancer Res. 2016. PMID: 27169995 Free PMC article.
EZH2 inhibitor efficacy in non-Hodgkin's lymphoma does not require suppression of H3K27 monomethylation.
Bradley WD, Arora S, Busby J, Balasubramanian S, Gehling VS, Nasveschuk CG, Vaswani RG, Yuan CC, Hatton C, Zhao F, Williamson KE, Iyer P, Méndez J, Campbell R, Cantone N, Garapaty-Rao S, Audia JE, Cook AS, Dakin LA, Albrecht BK, Harmange JC, Daniels DL, Cummings RT, Bryant BM, Normant E, Trojer P. Bradley WD, et al. Among authors: bryant bm. Chem Biol. 2014 Nov 20;21(11):1463-75. doi: 10.1016/j.chembiol.2014.09.017. Chem Biol. 2014. PMID: 25457180
BET bromodomain inhibition suppresses TH17-mediated pathology.
Mele DA, Salmeron A, Ghosh S, Huang HR, Bryant BM, Lora JM. Mele DA, et al. Among authors: bryant bm. J Exp Med. 2013 Oct 21;210(11):2181-90. doi: 10.1084/jem.20130376. Epub 2013 Oct 7. J Exp Med. 2013. PMID: 24101376 Free PMC article.
Correction: Bromodomain inhibition of the transcriptional coactivators CBP/EP300 as a therapeutic strategy to target the IRF4 network in multiple myeloma.
Conery AR, Centore RC, Neiss A, Keller PJ, Joshi S, Spillane KL, Sandy P, Hatton C, Pardo E, Zawadzke L, Bommi-Reddy A, Gascoigne KE, Bryant BM, Mertz JA, Sims RJ. Conery AR, et al. Among authors: bryant bm. Elife. 2016 Jul 14;5:e19432. doi: 10.7554/eLife.19432. Elife. 2016. PMID: 27411486 Free PMC article. No abstract available.
36 results