BioCentury
ARTICLE | Distillery Therapeutics

A TMPRSS2 inhibitor for SARS-CoV-2

May 2, 2022 10:49 PM UTC

A peptidomimetic inhibitor of the host protease TMPRSS2, which cleaves the SARS-CoV-2 spike protein to allow fusion and cell entry, could help treat and prevent SARS-CoV-2. In an African green monkey epithelial cell line, screening of peptidomimetic compounds for their ability to inhibit TMPRSS2 without affecting cell viability, followed by structure-based analyses and SARS-CoV-2 infectivity assays in a human lung epithelial cell line, identified a ketobenzothiazole-based compound with a stabilizing N-terminal cap that inhibited infection with the original SARS-CoV-2 strain with an EC50 of 2.8 nM, and inhibited infection by the Alpha, Beta, Gamma and Delta variants with EC50s of 2.1 nM-13.9 nM...

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