Protein degradation through covalent inhibitor-based PROTACs
Gang Xue, Jiahui Chen, Lihong Liu, Danli Zhou, Yingying Zuo, Tiancheng Fu, Zhengying Pan
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.
Topics & Concepts
Covalent bondDegradation (telecommunications)ChemistryProtein degradationCombinatorial chemistryComputer scienceBiochemistryOrganic chemistryTelecommunicationsProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysCAR-T cell therapy research