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Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).
Taylor AM, Côté A, Hewitt MC, Pastor R, Leblanc Y, Nasveschuk CG, Romero FA, Crawford TD, Cantone N, Jayaram H, Setser J, Murray J, Beresini MH, de Leon Boenig G, Chen Z, Conery AR, Cummings RT, Dakin LA, Flynn EM, Huang OW, Kaufman S, Keller PJ, Kiefer JR, Lai T, Li Y, Liao J, Liu W, Lu H, Pardo E, Tsui V, Wang J, Wang Y, Xu Z, Yan F, Yu D, Zawadzke L, Zhu X, Zhu X, Sims RJ 3rd, Cochran AG, Bellon S, Audia JE, Magnuson S, Albrecht BK. Taylor AM, et al. Among authors: conery ar. ACS Med Chem Lett. 2016 Mar 15;7(5):531-6. doi: 10.1021/acsmedchemlett.6b00075. eCollection 2016 May 12. ACS Med Chem Lett. 2016. PMID: 27190605 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: conery ar. 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.
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
Crawford TD, Romero FA, Lai KW, Tsui V, Taylor AM, de Leon Boenig G, Noland CL, Murray J, Ly J, Choo EF, Hunsaker TL, Chan EW, Merchant M, Kharbanda S, Gascoigne KE, Kaufman S, Beresini MH, Liao J, Liu W, Chen KX, Chen Z, Conery AR, Côté A, Jayaram H, Jiang Y, Kiefer JR, Kleinheinz T, Li Y, Maher J, Pardo E, Poy F, Spillane KL, Wang F, Wang J, Wei X, Xu Z, Xu Z, Yen I, Zawadzke L, Zhu X, Bellon S, Cummings R, Cochran AG, Albrecht BK, Magnuson S. Crawford TD, et al. Among authors: conery ar. J Med Chem. 2016 Dec 8;59(23):10549-10563. doi: 10.1021/acs.jmedchem.6b01022. Epub 2016 Sep 28. J Med Chem. 2016. PMID: 27682507
Bromodomains: a new target class for drug development.
Cochran AG, Conery AR, Sims RJ 3rd. Cochran AG, et al. Among authors: conery ar. Nat Rev Drug Discov. 2019 Aug;18(8):609-628. doi: 10.1038/s41573-019-0030-7. Epub 2019 Jul 4. Nat Rev Drug Discov. 2019. PMID: 31273347 Review.
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: conery ar. 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.
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. Elife. 2016 Jul 14;5:e19432. doi: 10.7554/eLife.19432. Elife. 2016. PMID: 27411486 Free PMC article. No abstract available.
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: conery ar. 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.
17 results