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Updated: Aug 9, 2025
A Fluorogenic Peptide Cleavage Assay to Screen for Proteolytic Activity: Applications for coronavirus spike protein activation
Published on: January 9, 2019
Azapeptide activity-based probes for the SARS-CoV-2 main protease enable visualization of inhibition in infected
Roeland Vanhoutte1, Marta Barniol-Xicota1, Winston Chiu2
1Department of Cellular and Molecular Medicine, Laboratory of Chemical Biology, KU Leuven Herestraat 49 box 802 3000 Leuven Belgium steven.verhelst@kuleuven.be.
Abstract:
The COVID-19 pandemic has revealed the vulnerability of the modern, global society. With expected waves of future infections by SARS-CoV-2, treatment options for infected individuals will be crucial in order to decrease mortality and hospitalizations. The SARS-CoV-2 main protease is a validated drug target, for which the first inhibitor has been approved for use in patients. To facilitate future work on this drug target, we designed a solid-phase synthesis route towards azapeptide activity-based probes that are capped with a cysteine-reactive electrophile for covalent modification of the active site of Mpro. This design led to the most potent ABP for Mpro and one of the most potent inhibitors reported thus far. We demonstrate that this ABP can be used to visualize Mpro activity and target engagement by drugs in infected cells.
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