BET Bromodomain inhibitors and degraders based on polypharmacology:research advances
10.13220/j.cnki.jipr.2017.06.001
- VernacularTitle:基于多向药理学的BET Bromodomain抑制剂及降解剂研究进展
- Author:
Hongli CHEN
;
Haifang CHEN
;
Zhimin ZHANG
;
Tao LU
;
Yadong CHEN
- Keywords:
Bromodomain and extra-terminal domain(BET);
Bromodomain;
polypharmacology;
small-molecule inhibitors;
protein degraders
- From:
Journal of International Pharmaceutical Research
2017;44(6):471-479,486
- CountryChina
- Language:Chinese
-
Abstract:
Bromodomain and extra-terminal domain(BET)Bromodomain has become a new target for the treatment of cancers and other human disorders. Nowadays,several classes of its potent and selective small-molecule inhibitors have been identified,many of which are in clinical trials. Preclinical and clinical data have shown that BET Bromodomain inhibitors have good prospects. Howev-er,there are potential therapeutic deficiencies,such as drug resistance. At present,attempts are being made to develop BET Bromodo-main inhibitors and degraders based on polypharmacology,combining BET Bromodomain with other targets of different mechanisms. In this paper,small-molecule kinase/BET inhibitors,small-molecule histone deacetylases(HDAC)/BET inhibitors and BET protein degraders are reviewed,which may provide guidance for further research on BET protein.
