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Discovery of a Potent Fluorescence Polarization Probe for Identifying USP1 Allosteric Inhibitors

open access: yesAdvanced Science, EarlyView.
This study presents the first ubiquitin‐specific protease 1 (USP1) allosteric fluoroprobe and fluorescence polarization assay, enabling the differentiation of allosteric and catalytic site inhibitors. Further, a novel class of tetrahydroisoquinoline‐based USP1 inhibitors is designed, with compound 14a (USP1 IC50 = 29.9 nM) showing strong selectivity ...
Jiawei Cheng   +12 more
wiley   +1 more source

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