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Current Medicinal Chemistry


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

Review Article

Recent Advances in Small Molecule PROTACs for the Treatment of Cancer

Author(s): Wen Li, Reham M. Elhassan, Xuben Hou* and Hao Fang*

Volume 28, Issue 24, 2021

Published on: 17 November, 2020

Page: [4893 - 4909] Pages: 17

DOI: 10.2174/0929867327666201117141611

Price: $65


The PROTAC (PROteolysis TArgeting Chimera) technology is a target protein degradation strategy, based on the ubiquitin-proteasome system, which has been gradually developed into a potential means of targeted cancer therapy in recent years. This strategy has already shown significant advantages over traditional small-molecule inhibitors in terms of pharmacodynamics, selectivity, and drug resistance. Several small molecule PROTACs have been in Phase I clinical trial. Herein, we have introduced the mechanism, characteristics, and advantages of PROTAC strategy. And we have summarized the recent advances in the development of small-molecule PROTACs for cancer treatment. We hope this review will be helpful in optimizing the design of the ideal small- molecule PROTACs and advancing targeted anticancer research.

Keywords: Anticancer, E3 ligase, PROTAC, protein degradation, ubiquitination, ligand, transduction.

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