4.4 Article

Luminescent Assay for the Screening of SARS-CoV-2 MPro Inhibitors

期刊

CHEMBIOCHEM
卷 23, 期 15, 页码 -

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbic.202200190

关键词

enzymes; inhibitors; imaging agents; luminescence

资金

  1. Dutch Research Council (NWO) [741.018.406]

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This article introduces a luminescent assay using a peptide-based probe to screen and validate M-Pro inhibitors. The method has been proven effective in screening potential inhibitors.
Since the outbreak of SARS-CoV-2 in December 2019 millions of infections have been reported globally. The viral chymotrypsin-like main protease (M-Pro) exhibits a crucial role in viral replication and represents a relevant target for antiviral drug development. In order to screen potential M-Pro inhibitors we developed a luminescent assay using a peptide based probe containing a cleavage site specific for M-Pro. This assay was validated showing IC50 values similar to those reported in the literature for known M-Pro inhibitors and can be used to screen new inhibitors.

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