Applications of covalent chemistry in targeted protein degradation,Chemical Society Reviews

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Applications of covalent chemistry in targeted protein degradation
Chemical Society Reviews ( IF 40.4 ) Pub Date : 2022-10-26 , DOI: 10.1039/d2cs00362g
Dong Lu ₁ , Xin Yu ₁ , Hanfeng Lin ₁ , Ran Cheng ₁ , Erika Y Monroy ₁ , Xiaoli Qi ₁ , Meng C Wang _{2,

3,

4} , Jin Wang _{1,

5}

Affiliation

Proteolysis-targeting chimeras (PROTACs) and targeted covalent inhibitors (TCIs) are currently two exciting strategies in the fields of chemical biology and drug discovery. Extensive research in these two fields has been conducted, and significant progress in these fields has resulted in many clinical candidates, some of which have been approved by FDA. Recently, a novel concept termed covalent PROTACs that combine these two strategies has emerged and gained an increasing interest in the past several years. Herein, we briefly review and highlight the mechanism and advantages of TCIs and PROTACs, respectively, and the recent development of covalent PROTACs using irreversible and reversible covalent chemistry.

中文翻译：

共价化学在靶向蛋白质降解中的应用

蛋白水解靶向嵌合体（PROTAC）和靶向共价抑制剂（TCIs）是目前化学生物学和药物发现领域的两种令人兴奋的策略。这两个领域已经进行了广泛的研究，这些领域的重大进展产生了许多临床候选药物，其中一些已获得 FDA 批准。最近，出现了一种称为共价 PROTAC 的新概念，它结合了这两种策略，并在过去几年中引起了越来越多的兴趣。在此，我们分别简要回顾和重点介绍了 TCI 和 PROTAC 的机制和优点，以及利用不可逆和可逆共价化学的共价 PROTAC 的最新发展。

更新日期：2022-10-26

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