Applications of covalent chemistry in targeted protein degradation.
Applications of covalent chemistry in targeted protein degradation.
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DOI：
10.1039/d2cs00362g
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发表时间：
2022-11-14
影响因子：
46.2
通讯作者：
Wang, Jin
中科院分区：
文献类型：
--
作者：
Lu, Dong;Yu, Xin;Lin, Hanfeng;Cheng, Ran;Monroy, Erika Y.;Qi, Xiaoli;Wang, Meng C.;Wang, Jin
涉及蛋白水解靶向嵌合体（Protac）和靶向共价抑制剂（TCI）目前是化学生物学和药物发现领域的两种令人兴奋的策略。已经在这两个领域进行了广泛的研究，这些领域的重大进展导致了许多临床候选者，其中一些候选者已获得FDA批准。最近，一个新颖的概念称为共价protac，结合了这两种策略，并且在过去几年中越来越兴趣。本文中，我们分别简要审查和强调了TCI和Protacs的机制和优势，以及使用不可逆和可逆的共价化学化学的最新共价protac的发展。
这篇综述总结了靶向蛋白质降解中共价化学的最新工作，并描述了共价protac的概念，利弊，发展和前景。
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 have 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. This review summarizes the recent work of covalent chemistry in targeted protein degradation, and describes the concept, pros and cons, development, and the outlook of covalent PROTACs.
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影响因子：
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作者：
Caine EA;Mahan SD;Johnson RL;Nieman AN;Lam N;Warren CR;Riching KM;Urh M;Daniels DL
通讯作者：
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影响因子：
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Crews, Craig M.
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