Recent Advances in Small Molecule PROTACs for the Treatment of Cancer

Title:Recent Advances in Small Molecule PROTACs for the Treatment of Cancer

Volume: 28 Issue: 24

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

Affiliation:

• Department of Medicinal Chemistry and Key Laboratory of Chemical Biology of Natural Products (MOE), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012,China

• Department of Medicinal Chemistry and Key Laboratory of Chemical Biology of Natural Products (MOE), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012,China

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

Abstract: 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.

Cite this article as:

Li Wen , Elhassan M. Reham , Hou Xuben *, Fang Hao *, Recent Advances in Small Molecule PROTACs for the Treatment of Cancer, Current Medicinal Chemistry 2021; 28 (24) . https://dx.doi.org/10.2174/0929867327666201117141611