GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins

Journal of Medicinal Chemistry
Robert J WatsonEmmanuel 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.

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Citations

Sep 15, 2020·Medicinal Research Reviews·Ewelina KulikowskiNorman C W Wong
Feb 19, 2021·Journal of Medicinal Chemistry·Yi ZhangYuanxiang Wang
Apr 15, 2021·Current Opinion in Chemical Biology·Isabelle A EngelbergStephen V Frye
Jun 10, 2021·Organic & Biomolecular Chemistry·Ellen E GuestJonathan D Hirst
May 14, 2021·The FEBS Journal·Marton Siklos, Stefan Kubicek
Jul 13, 2021·Journal of Medicinal Chemistry·Francesco RianjongdeeEmmanuel H Demont
Aug 21, 2021·ACS Medicinal Chemistry Letters·Michael A CleggPhilip G Humphreys
Aug 26, 2021·Biological Chemistry·Anna-Theresa BlaslMichael Lammers
Oct 23, 2020·Journal of Medicinal Chemistry·Stuart J ConwayShaomeng Wang
Aug 28, 2021·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Qianqian WangXiaojun Yao

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