Discovery of M Protease Inhibitors Encoded by SARS-CoV-2.

ABSTRACT: The coronavirus (CoV) disease 2019 (COVID-19) pandemic caused by severe acute respiratory syndrome CoV-2 (SARS-CoV-2) is a health threat worldwide. Viral main protease (M^pro, also called 3C-like protease [3CL^pro]) is a therapeutic target for drug discovery. Herein, we report that GC376, a broad-spectrum inhibitor targeting M^pro in the picornavirus-like supercluster, is a potent inhibitor for the M^pro encoded by SARS-CoV-2, with a half-maximum inhibitory concentration (IC₅₀) of 26.4 ± 1.1 nM. In this study, we also show that GC376 inhibits SARS-CoV-2 replication with a half-maximum effective concentration (EC₅₀) of 0.91 ± 0.03 μM. Only a small portion of SARS-CoV-2 M^pro was covalently modified in the excess of GC37

SUBMITTER: Hung HC 

PROVIDER: S-EPMC7449189 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature