BET Bromodomain inhibitors and degraders based on polypharmacology:research advances / 国际药学研究杂志
Journal of International Pharmaceutical Research
;
(6): 471-479,486, 2017.
Article
in Chinese
| WPRIM
| ID: wpr-617470
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Type of study:
Practice guideline
Language:
Chinese
Journal:
Journal of International Pharmaceutical Research
Year:
2017
Type:
Article
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