1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain

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• 作者：Emmanuel H. Demont ; Paul Bamborough ; Chun-wa Chung ; Peter D. Craggs ; David Fallon ; Laurie J. Gordon ; Paola Grandi ; Clare I. Hobbs ; Jameed Hussain ; Emma J. Jones ; Armelle Le Gall ; Anne-Marie Michon ; Darren J. Mitchell ; Rab K. Prinjha ; Andy D. Roberts ; Robert J. Sheppard ; Robert J. Watson
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2014
• 出版时间：November 13, 2014
• 年：2014
• 卷：5
• 期：11
• 页码：1190-1195
• 全文大小：408K
• 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. Here, we report the discovery, binding mode, and structure鈥揳ctivity relationship (SAR) of the first potent, selective series of inhibitors of the BRPF1 bromodomain.

Keywords:

BRPF1; BRPF2; BRD1; BRPF3; bromodomain; chemical probe; epigenetics; fragment; inhibitor