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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

Recent Developments in Targeting Bromodomain and Extra Terminal Domain Proteins for Cancer Therapeutics

Author(s): Maohua Cai, Jinyun Dong*, Haobin Li and Jiang-Jiang Qin*

Volume 29, Issue 25, 2022

Published on: 28 March, 2022

Page: [4391 - 4409] Pages: 19

DOI: 10.2174/0929867329666220211091806

Price: $65


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.

Keywords: Cancer, BET, BRD4, inhibitor, PROTAC, drug design.

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