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Furin-targeting activity-based probes with phosphonate and phosphinate esters as warheads
Shanping Ji1, Steven H L Verhelst1,2
1Laboratory of Chemical Biology, Department of Cellular and Molecular Medicine, KU Leuven - University of Leuven, 3000 Leuven, Belgium. steven.verhelst@kuleuven.be.
Abstract:
Activity-based probes (ABPs) are covalent chemical tools that are widely used to target proteases in chemical biology. Here, we report a series of novel ABPs for the serine protease furin with phosphonate and phosphinate esters as reactive electrophiles. We show that these probes covalently label furin and have nanomolar potencies, because of proposed interactions with the different recognition pockets around the active site of furin.

