Issue 12, 2016

Chemical probes and inhibitors of bromodomains outside the BET family

Abstract

In the last five years, the development of inhibitors of bromodomains has emerged as an area of intensive worldwide research. Emerging evidence has implicated a number of non-BET bromodomains in the onset and progression of diseases such as cancer, HIV infection and inflammation. The development and use of small molecule chemical probes has been fundamental to pre-clinical evaluation of bromodomains as targets. Recent efforts are described highlighting the development of potent, selective and cell active non-BET bromodomain inhibitors and their therapeutic potential. Over half of typical bromodomains now have reported ligands, but those with atypical binding site residues remain resistant to chemical probe discovery efforts.

Graphical abstract: Chemical probes and inhibitors of bromodomains outside the BET family

Article information

Article type
Review Article
Submitted
06 Jul 2016
Accepted
06 Sep 2016
First published
07 Sep 2016
This article is Open Access
Creative Commons BY license

Med. Chem. Commun., 2016,7, 2246-2264

Chemical probes and inhibitors of bromodomains outside the BET family

M. Moustakim, P. G. K. Clark, D. A. Hay, D. J. Dixon and P. E. Brennan, Med. Chem. Commun., 2016, 7, 2246 DOI: 10.1039/C6MD00373G

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