2. Academic Validation
  3. GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family

GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family

  • ACS Med Chem Lett. 2020 Jul 6;11(8):1581-1587. doi: 10.1021/acsmedchemlett.0c00247.
Alex Preston 1,  Stephen J Atkinson 1,  Paul Bamborough 1,  Chun-Wa Chung 1,  Laurie J Gordon 1,  Paola Grandi 2,  James R J Gray 1,  Lee A Harrison 1,  Antonia J Lewis 1,  David Lugo 1,  Cassie Messenger 1,  Anne-Marie Michon 2,  Darren J Mitchell 1,  Rab K Prinjha 1,  Inmaculada Rioja 1,  Jon Seal 1,  Simon Taylor 1,  Pierre Thesmar 1,  Ian D Wall 1,  Robert J Watson 1,  James M Woolven 1,  Emmanuel H Demont 1
Affiliations

Affiliations

  • 1 Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
  • 2 Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany.
PMID: 32832027 DOI: 10.1021/acsmedchemlett.0c00247
Abstract

Pan-BET inhibitors have shown profound efficacy in a number of in vivo preclinical models and have entered the clinic in oncology trials where adverse events have been reported. These inhibitors interact equipotently with the eight bromodomains of the BET family of proteins. To better understand the contribution of each domain to their efficacy and to improve from their safety profile, selective inhibitors are required. This Letter discloses the profile of GSK973, a highly selective inhibitor of the second bromodomains of the BET proteins that has undergone extensive preclinical in vitro and in vivo characterization.

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