Advances in BET bromodomain protein inhibitors
10.11665/j.issn.1000-5048.20150302
- VernacularTitle:BET bromodomain蛋白小分子抑制剂研究进展
- Author:
Kejun LIU
1
;
Zhimin ZHANG
;
Ting RAN
;
Hongli CHEN
;
Tao LU
;
Yadong CHEN
Author Information
1. 中国药科大学理学院
- Publication Type:Journal Article
- Keywords:
BET;
bromodomain;
small molecular inhibitors;
tumor;
advances
- From:
Journal of China Pharmaceutical University
2015;46(3):264-271
- CountryChina
- Language:Chinese
-
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.
