Inhibitory efficacy and structural insights of Bofutrelvir against SARS-CoV-2 M^pro mutants and MERS-CoV M^pro.

ABSTRACT: The COVID-19 pandemic has caused significant global health and economic disruption. Mutations E166N, E166R, E166N, S144A and His163A in the SARS-CoV-2 main protease (M^pro) have been implicated in reducing the efficacy of certain antiviral treatments. Bofutrelvir, a promising inhibitor, has shown effectiveness against SARS-CoV-2 M^pro. This study aims to evaluate the inhibitory effects of Bofutrelvir on the E166N, E166R, His163A, E166V and S144A mutants of SARS-CoV-2 M^pro, as well as on MERS-CoV M^pro. Our findings indicate a substantial reduction in the inhibitory potency of Bofutrelvir against these mutants and MERS-CoV, with IC₅₀ values significantly higher than those for the wild-type SARS-CoV-2 M^pro. Specifically, the E166

SUBMITTER: Wang W 

PROVIDER: S-EPMC11937426 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature