TMPRSS2 Inhibitor Discovery Facilitated through an In Silico and Biochemical Screening Platform.

ABSTRACT: The COVID-19 pandemic has highlighted the need for new antiviral approaches because many of the currently approved drugs have proven ineffective against mitigating SARS-CoV-2 infections. The host transmembrane serine protease TMPRSS2 is a promising antiviral target because it plays a role in priming the spike protein before viral entry occurs for the most virulent variants. Further, TMPRSS2 has no established physiological role, thereby increasing its attractiveness as a target for antiviral agents. Here, we utilize virtual screening to curate large libraries into a focused collection of potential inhibitors. Optimization of a recombinant expression and purification protocol for the TMPRSS2 peptidase domain facilitates subsequent biochemical screening and characterization of selected compo

SUBMITTER: Peiffer AL 

PROVIDER: S-EPMC10237299 | biostudies-literature | 2023 Jun

REPOSITORIES: biostudies-literature