BiochemistrybioRxivPreprint
Sub-stoichiometric Degradation is Dispensable for Potent PROTACs: A Case Study for Irreversible Covalent BTK Degraders
Ran Cheng, Hanfeng Lin, Xin Yu…·Jin Wang
This paper develops and characterizes PSIRC3, a covalent PROTAC for BTK, showing it achieves potent degradation with sub-nanomolar potency and high selectivity, challenging the necessity of catalytic turnover for PROTAC efficacy.
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