Advances in BET bromodomain protein inhibitors

LIU Kejun; ZHANG Zhimin; RAN Ting; CHEN Hongli; LU Tao; CHEN Yadong

doi:10.11665/j.issn.1000-5048.20150302

Journal of China Pharmaceutical University > 2015 > 46(3): 264-271. > DOI: 10.11665/j.issn.1000-5048.20150302

LIU Kejun, ZHANG Zhimin, RAN Ting, CHEN Hongli, LU Tao, CHEN Yadong. Advances in BET bromodomain protein inhibitors[J]. Journal of China Pharmaceutical University, 2015, 46(3): 264-271. DOI: 10.11665/j.issn.1000-5048.20150302

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Advances in BET bromodomain protein inhibitors

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Abstract

Abstract

Recognizing acetyl-lysine of histone is a key process of epigenetic regulation that is mediated by a protein module called bromodomain(BRD). The bromodomain inhibitors of the bromodomains and extra-terminal(BET)family have shown great potential in anti-inflammatory and antiproliferative effects. Through a review of diseases and structures about BET bromodomain, different kinds of inhibitors were analyzed and their structure-activity relationships were summarized. Herenin, the recent advances reported are reviewed for discovering more excellent small molecule inhibitors.
- BET,
- bromodomain,
- small molecular inhibitors,
- tumor,
- advances

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