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

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

ACS medicinal chemistry letters（2014）

引用 77|浏览34

暂无评分

摘要

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-activity relationship (SAR) of the first potent, selective series of inhibitors of the BRPF1 bromodomain.

查看译文

关键词

brd1,brpf1,brpf2,brpf3,bromodomain,chemical probe,epigenetics,fragment,inhibitor,transcription

AI 理解论文

溯源树

样例

生成溯源树，研究论文发展脉络

Chat Paper

正在生成论文摘要