当前位置: X-MOL 学术ChemBioChem › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Recent Developments in PROTAC-Mediated Protein Degradation: From Bench to Clinic
ChemBioChem ( IF 3.2 ) Pub Date : 2021-09-08 , DOI: 10.1002/cbic.202100270
Zhenyi Hu 1 , Craig M Crews 1, 2, 3
Affiliation  

Over the past two decades, Proteolysis-targeting chimeras (PROTACs) have been developed as a new approach for targeted protein degradation by hijacking the ubiquitin-proteasome system. In this review, we describe recent PROTAC developments, focusing on mechanistic and kinetic studies, pharmacokinetic study, spatiotemporal control of PROTACs, covalent PROTACs, resistance to PROTACs, and new E3 ligands.
image


中文翻译:

PROTAC 介导的蛋白质降解的最新进展:从实验室到临床

在过去的二十年中,蛋白水解靶向嵌合体 (PROTAC) 已被开发为一种通过劫持泛素-蛋白酶体系统来靶向蛋白质降解的新方法。在这篇综述中,我们描述了 PROTAC 的最新进展,重点是机制和动力学研究、药代动力学研究、PROTAC 的时空控制、共价 PROTAC、对 PROTAC 的耐药性和新的 E3 配体。
图片
更新日期:2021-09-08
down
wechat
bug