Enhancing Intracellular Accumulation and Target Engagement of PROTACs with Reversible Covalent Chemistry
W.-H. Guo, X. Qi, X. Yu, Y. Liu, C.-I. Chung, F. Bai, X. Lin, D. Lu, L. Wang, J. Chen, L. Su, K. J. Nomie, F. Li, M. C. Wang, X. Shu, , J. Wang
This study discovers that reversible covalent chemistry enhances PROTAC intracellular accumulation and target engagement, leading to improved efficacy.
bioRxiv · Dec 30, 2019Pharmacology & Toxicology