Drug-Repurposing Screening Identified Tropifexor as a SARS-CoV-2 Papain-like Protease Inhibitor.

ABSTRACT: The global COVID-19 pandemic underscores the dire need for effective antivirals. Encouraging progress has been made in developing small-molecule inhibitors targeting the SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) and main protease (M^pro). However, the development of papain-like protease (PL^pro) inhibitors faces several obstacles. Nevertheless, PL^pro represents a high-profile drug target given its multifaceted roles in viral replication. PL^pro is involved in not only the cleavage of viral polyprotein but also the modulation of host immune response. In this study, we conducted a drug-repurposing screening of PL^pro against the MedChemExpress bioactive compound library and identified three hits, EACC, KY-226, and tropifexor, as potent

SUBMITTER: Ma C 

PROVIDER: S-EPMC9017246 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature