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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.

SUBMITTER: Moustakim M

PROVIDER: S-EPMC5644722 | biostudies-literature | 2016 Dec

REPOSITORIES: biostudies-literature

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Chemical probes and inhibitors of bromodomains outside the BET family.

Moustakim Moses M Clark Peter G K PGK Hay Duncan A DA Dixon Darren J DJ Brennan Paul E PE

MedChemComm 20160907 12

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 ce ...[more]

PMID: 29170712

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