Protein degradation through covalent inhibitor-based PROTACs.


State Key Laboratory of Chemical Oncogenomics, Key Laboratory of Chemical Genomics, Engineering Laboratory for Chiral Drug Synthesis, School of Chemical Biology and Biotechnology Shenzhen Graduate School, Peking University, Xili University Town, PKU Campus, F-311, Shenzhen, 518055, China. [Email]


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.

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