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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. PLoS One. 2013 Dec 31;8(12):e83190. doi: 10.1371/journal.pone.0083190. eCollection 2013. PLoS One. 2013. PMID: 24391744 Free PMC article.
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: mclure kg. 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. Among authors: mclure kg. 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, a BET-inhibitor for treating atherosclerotic cardiovascular disease, raises ApoA-I/HDL and represses pathways that contribute to cardiovascular disease.
Gilham D, Wasiak S, Tsujikawa LM, Halliday C, Norek K, Patel RG, Kulikowski E, Johansson J, Sweeney M, Wong NC, Gordon A, McLure K, Young P. Gilham D, et al. Atherosclerosis. 2016 Apr;247:48-57. doi: 10.1016/j.atherosclerosis.2016.01.036. Epub 2016 Jan 22. Atherosclerosis. 2016. PMID: 26868508 Free article.
Data on gene and protein expression changes induced by apabetalone (RVX-208) in ex vivo treated human whole blood and primary hepatocytes.
Wasiak S, Gilham D, Tsujikawa LM, Halliday C, Norek K, Patel RG, McLure KG, Young PR, Gordon A, Kulikowski E, Johansson J, Sweeney M, Wong NC. Wasiak S, et al. Among authors: mclure kg. Data Brief. 2016 Jul 29;8:1280-8. doi: 10.1016/j.dib.2016.07.047. eCollection 2016 Sep. Data Brief. 2016. PMID: 27570805 Free PMC article.
20 results