| Literature DB >> 32691589 |
Robert J Watson, Paul Bamborough, Heather Barnett, Chun-Wa Chung, Rob Davis, Laurie Gordon, Paola Grandi1, Massimo Petretich1, Alex Phillipou, Rab K Prinjha, Inmaculada Rioja, Peter Soden, Thilo Werner1, Emmanuel H Demont.
Abstract
Pan-bromodomain and extra terminal (BET) inhibitors interact equipotently with all eight bromodomains of the BET family of proteins. They have shown profound efficacy in vitro and in vivo in oncology and immunomodulatory models, and a number of them are currently in clinical trials where significant safety signals have been reported. It is therefore important to understand the functional contribution of each bromodomain to assess the opportunity to tease apart efficacy and toxicity. This article discloses the in vitro and cellular activity profiles of GSK789, a potent, cell-permeable, and highly selective inhibitor of the first bromodomains of the BET family.Entities:
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Year: 2020 PMID： 32691589 DOI： 10.1021/acs.jmedchem.0c00614
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446