Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry

Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry

PROTACs have emerged as promising therapeutic agents but their cellular uptake is often inefficient. Here, the authors show that reversible covalent warhead chemistry improves PROTAC intracellular accumulation and target engagement, and develop a dual inhibitor/degrader of Bruton’s tyrosine kinase

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Bibliographic Details
Main Authors: Wen-Hao Guo, Xiaoli Qi, Xin Yu, Yang Liu, Chan-I Chung, Fang Bai, Xingcheng Lin, Dong Lu, Lingfei Wang, Jianwei Chen, Lynn Hsiao Su, Krystle J. Nomie, Feng Li, Meng C. Wang, Xiaokun Shu, José N. Onuchic, Jennifer A. Woyach, Michael L. Wang, Jin Wang
Format: article
Language:EN
Published: Nature Portfolio 2020
Subjects:
Science
Q
Online Access:https://doaj.org/article/4979b2c9fe654e15a019e2b5da2998c8
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Summary:PROTACs have emerged as promising therapeutic agents but their cellular uptake is often inefficient. Here, the authors show that reversible covalent warhead chemistry improves PROTAC intracellular accumulation and target engagement, and develop a dual inhibitor/degrader of Bruton’s tyrosine kinase

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