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蛋白酶靶向嵌合体设计的前沿策略

Advancing Strategies for Proteolysis-Targeting Chimera Design.

作者信息

Li Minglei, Zhi Ying, Liu Bo, Yao Qingqiang

机构信息

School of Pharmacy and Pharmaceutical Sciences, Shandong First Medical University & Shandong Academy of Medical Sciences, Jinan, 250117 Shandong, P. R. China.

出版信息

J Med Chem. 2023 Feb 23;66(4):2308-2329. doi: 10.1021/acs.jmedchem.2c01555. Epub 2023 Feb 14.

Abstract

Proteolysis-targeting chimeras (PROTACs) have shown great therapeutic potential by degrading various disease-causing proteins, particularly those related to tumors. Therefore, the introduction of PROTACs has ushered in a new chapter of antitumor drug development, marked by significant advances over recent years. Herein, we describe recent developments in PROTAC technology, focusing on design strategy, development workflow, and future outlooks. We also discuss potential opportunities and challenges for PROTAC research.

摘要

靶向蛋白降解嵌合体(PROTACs)通过降解各种致病蛋白,尤其是与肿瘤相关的蛋白,展现出了巨大的治疗潜力。因此,PROTACs的引入开启了抗肿瘤药物研发的新篇章,近年来取得了显著进展。在此,我们描述了PROTAC技术的最新进展,重点关注设计策略、开发流程和未来展望。我们还讨论了PROTAC研究的潜在机遇和挑战。

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