Invalidation of dieckol and 1,2,3,4,6-pentagalloylglucose (PGG) as SARS-CoV-2 main protease inhibitors and the discovery of PGG as a papain-like protease inhibitor.

ABSTRACT: The COVID-19 pandemic spurred a broad interest in antiviral drug discovery. The SARS-CoV-2 main protease (M^pro) and papain-like protease (PL^pro) are attractive antiviral drug targets given their vital roles in viral replication and modulation of host immune response. Structurally disparate compounds were reported as M^pro and PL^pro inhibitors from either drug repurposing or rational design. Two polyphenols dieckol and 1,2,3,4,6-pentagalloylglucose (PGG) were recently reported as SARS-CoV-2 M^pro inhibitors. With our continuous interest in studying the mechanism of inhibition and resistance of M^pro inhibitors, we report herein our independent validation/invalidation of these two natural products. Our FRET-based enzymatic assay

SUBMITTER: Tan H 

PROVIDER: S-EPMC9095416 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature