Recent Advances in Small Molecule PROTACs for the Treatment of Cancer

doi:10.2174/0929867327666201117141611

摘要

PROTAC (靶向嵌合体蛋白水解)技术是一种基于泛素-蛋白酶体系统的靶向蛋白降解策略，近年来逐渐发展成为一种潜在的靶向肿瘤治疗手段。该策略在药效学、选择性和耐药方面已经显示出比传统小分子抑制剂的显著优势。一些小分子PROTACs已进入I期临床试验。本文介绍了PROTACs策略的原理、特点和优势。并对小分子PROTACs在肿瘤治疗中的研究进展进行了综述。我们希望这篇综述将有助于优化理想的小分子PROTACs的设计，推进靶向抗癌研究。

关键词: 抗癌，E3连接酶，PROTAC，蛋白降解，泛素化，配体，转导。

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Current Medicinal Chemistry

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

Volume: 28 Issue: 24

关键词: 抗癌，E3连接酶，PROTAC，蛋白降解，泛素化，配体，转导。

摘要: 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.

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Recent Advances in Small Molecule PROTACs for the Treatment of Cancer, Current Medicinal Chemistry 2021; 28 (24) . https://dx.doi.org/10.2174/0929867327666201117141611

DOI https://dx.doi.org/10.2174/0929867327666201117141611	Print ISSN 0929-8673
Publisher Name Bentham Science Publisher	Online ISSN 1875-533X