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Issue 12, 2016
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Chemical probes and inhibitors of bromodomains outside the BET family

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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

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Publication details

The article was received on 06 Jul 2016, accepted on 06 Sep 2016 and first published on 07 Sep 2016


Article type: Review Article
DOI: 10.1039/C6MD00373G
Citation: Med. Chem. Commun., 2016,7, 2246-2264
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    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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