In:
Current Medicinal Chemistry, Bentham Science Publishers Ltd., Vol. 29, No. 25 ( 2022-08), p. 4391-4409
Kurzfassung:
Bromodomain and extra-terminal domain (BET) proteins are a well-studied
family of proteins associated with a variety of diseases, including malignancy and chronic inflammation. Currently, numerous pan BET inhibitors have exhibited potent efficacy
in several in vivo preclinical models and entered clinical trials but have largely stalled due to their adverse events. Therefore, the development of new selective inhibitors and
PROTACs (Proteolysis Targeting Chimeras) targeting BET is urgently needed. In the present review, we summarize the BET protein structure and the recent development in BET
inhibitors, focusing mainly on BRD4-selective inhibitors and PROTAC degraders.
Materialart:
Online-Ressource
ISSN:
0929-8673
DOI:
10.2174/0929867329666220211091806
Sprache:
Englisch
Verlag:
Bentham Science Publishers Ltd.
Publikationsdatum:
2022
SSG:
15,3