GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

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• 作者：Paul Bamborough ; Heather A. Barnett ; Isabelle Becher ; Mark J. Bird ; Chun-wa Chung ; Peter D. Craggs ; Emmanuel H. Demont ; Hawa Diallo ; David J. Fallon ; Laurie J. Gordon ; Paola Grandi ; Clare I. Hobbs ; Edward Hooper-Greenhill ; Emma J. Jones ; Robert P. Law ; Armelle Le Gall ; David Lugo ; Anne-Marie Michon ; Darren J. Mitchell ; Rab K. Prinjha ; Robert J. Sheppard ; Allan J. B. Watson ; Robert J. Watson
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：June 9, 2016
• 年：2016
• 卷：7
• 期：6
• 页码：552-557
• 全文大小：442K
• 年卷期：0
• ISSN：1948-5875

文摘

The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engagement assay was recently described. Herein, we report the optimization of this series leading to the identification of a superior BRPF1 inhibitor suitable for in vivo studies.