Biochemicals & reagents
1.BA Malcom et al. Antimicrob. Agents Chemother. 2006 50:1013 2.C Ma et al. bioRxiv 2020 Preprint May 8, DOI: 10.1101/2020.04.20.051581
Boceprevir directly inhibits Hepatitis C virus (HCV) NS3 protease (overall binding constant for formation of covalent adduct, Ki* = 14 nM; initial inhibition constant Ki = 7.8 µM). This blocks NS3 autoactivation, and subsequent cleavage and maturation of other viral proteins necessary for replisome assembly. This reversible, slow-binding ketoamide also restores host interferon signaling obstructed by HCV, thus reactivating the immune response (1). Recently, this compound was also found to inhibit the key SARS-CoV-2 protease, Mpro (3CLpro) in vitro (Ki = 1.18 µM) and in cells (EC50 = 1.9 µM, virus-induced cytopathic effects (CPE) assay) (2).