Bromodomain and extraterminal proteins-a novel class of therapeutic targets in epigenetics
10.16438/j.0513-4870.2017-0143
- VernacularTitle:含溴结构域和额外终端域家族蛋白——表观遗传领域的新型治疗靶点
- Author:
Jin-jing CHEN
1
;
Xiao-li ZHAO
2
;
Zhen WANG
2
;
Lin-feng CHEN
1
Author Information
1. University of Illinois at Urbana-Champaign, Department of Biochemistry, Urbana 61801, USA
2. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
- Publication Type:REVIEWS
- Keywords:
bromodomain and extraterminal;
bromodomain containing 4;
epigenetics;
therapeutic target;
chromatin regulation
- From:
Acta Pharmaceutica Sinica
2017;52(8):1209-1215
- CountryChina
- Language:Chinese
-
Abstract:
Bromodomain and extraterminal (BET) proteins are a class of proteins that can interpret epigenetic codes and play an important role in regulating gene transcription through identifying and binding acetylated histones or non-histones proteins. The BET inhibitors have emerged with good therapeutic effects in preclinical disease models such as cancer and inflammation. Some of them have entered clinical studies, demonstrating that there is considerable prospect for drug development with BET as a potential therapeutic target. This review briefly describes the structures and functions of the BET proteins, the BET inhibitors in various diseases, as well as molecular mechanisms involved.