Ebselen, Disulfiram, Carmofur, PX-12, Tideglusib, and Shikonin Are Nonspecific Promiscuous SARS-CoV-2 Main Protease Inhibitors.

ABSTRACT: Among the drug targets being investigated for SARS-CoV-2, the viral main protease (M^pro) is one of the most extensively studied. M^pro is a cysteine protease that hydrolyzes the viral polyprotein at more than 11 sites. It is highly conserved and has a unique substrate preference for glutamine in the P1 position. Therefore, M^pro inhibitors are expected to have broad-spectrum antiviral activity and a high selectivity index. Structurally diverse compounds have been reported as M^pro inhibitors. In this study, we investigated the mechanism of action of six previously reported M^pro inhibitors, ebselen, disulfiram, tideglusib, carmofur, shikonin, and PX-12, using a consortium of techniques including FRET-based enzymatic assay, thermal shift as

SUBMITTER: Ma C 

PROVIDER: S-EPMC7571300 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature