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RVX-297- a novel BD2 selective inhibitor of BET bromodomains.
Kharenko OA, Gesner EM, Patel RG, Norek K, White A, Fontano E, Suto RK, Young PR, McLure KG, Hansen HC. Kharenko OA, et al. Among authors: gesner em. Biochem Biophys Res Commun. 2016 Aug 12;477(1):62-67. doi: 10.1016/j.bbrc.2016.06.021. Epub 2016 Jun 6. Biochem Biophys Res Commun. 2016. PMID: 27282480
Discovery of a new chemical series of BRD4(1) inhibitors using protein-ligand docking and structure-guided design.
Duffy BC, Liu S, Martin GS, Wang R, Hsia MM, Zhao H, Guo C, Ellis M, Quinn JF, Kharenko OA, Norek K, Gesner EM, Young PR, McLure KG, Wagner GS, Lakshminarasimhan D, White A, Suto RK, Hansen HC, Kitchen DB. Duffy BC, et al. Bioorg Med Chem Lett. 2015 Jul 15;25(14):2818-23. doi: 10.1016/j.bmcl.2015.04.107. Epub 2015 May 11. Bioorg Med Chem Lett. 2015. PMID: 26022843
RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.
McLure KG, Gesner EM, Tsujikawa L, Kharenko OA, Attwell S, Campeau E, Wasiak S, Stein A, White A, Fontano E, Suto RK, Wong NC, Wagner GS, Hansen HC, Young PR. McLure KG, et al. Among authors: gesner em. PLoS One. 2013 Dec 31;8(12):e83190. doi: 10.1371/journal.pone.0083190. eCollection 2013. PLoS One. 2013. PMID: 24391744 Free PMC article.
BET Bromodomain Inhibition Blocks an AR-Repressed, E2F1-Activated Treatment-Emergent Neuroendocrine Prostate Cancer Lineage Plasticity Program.
Kim DH, Sun D, Storck WK, Welker Leng K, Jenkins C, Coleman DJ, Sampson D, Guan X, Kumaraswamy A, Rodansky ES, Urrutia JA, Schwartzman JA, Zhang C, Beltran H, Labrecque MP, Morrissey C, Lucas JM, Coleman IM, Nelson PS, Corey E, Handelman SK, Sexton JZ, Aggarwal R, Abida W, Feng FY, Small EJ, Spratt DE, Bankhead A 3rd, Rao A, Gesner EM, Attwell S, Lakhotia S, Campeau E, Yates JA, Xia Z, Alumkal JJ. Kim DH, et al. Among authors: gesner em. Clin Cancer Res. 2021 Sep 1;27(17):4923-4936. doi: 10.1158/1078-0432.CCR-20-4968. Epub 2021 Jun 18. Clin Cancer Res. 2021. PMID: 34145028 Free PMC article.
Role of pri-miRNA tertiary structure in miR-17~92 miRNA biogenesis.
Chaulk SG, Thede GL, Kent OA, Xu Z, Gesner EM, Veldhoen RA, Khanna SK, Goping IS, MacMillan AM, Mendell JT, Young HS, Fahlman RP, Glover JN. Chaulk SG, et al. RNA Biol. 2011 Nov-Dec;8(6):1105-14. doi: 10.4161/rna.8.6.17410. Epub 2011 Nov 1. RNA Biol. 2011. PMID: 21955497
19 results