Protein degradation through covalent inhibitor-based PROTACs. Issue 10 (10th January 2020)

• Record Type: Journal Article
• Authors: Xue, Gang; Chen, Jiahui; Liu, Lihong; Zhou, Danli; Zuo, Yingying; Fu, Tiancheng; Pan, Zhengying
• Is Part Of: Chemical communications. Volume 56:Issue 10(2020)
• Page Start: 1521
• Page End: 1524
• Publication Date: 2020-01-10
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/c9cc08238g
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : Covalent inhibitor-based PROTACs were successfully developed for the degradation of target proteins in live cells to further extend the application scope of PROTACs. Abstract : Tremendous advancements in proteolysis targeting chimera (PROTAC) technology have been made in recent years. However, whether a covalent inhibitor-based PROTAC can be developed remains controversial. Here, we successfully developed chimeric degraders based on covalent inhibitors to degrade BTK and BLK kinases, demonstrating that covalent inhibitor-based PROTACs are viable and useful tools.