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.
G. Xue, J. Chen, L. Liu, D. Zhou, Y. Zuo, T. Fu and Z. Pan, Chem. Commun., 2020, 56, 1521 DOI: 10.1039/C9CC08238G
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