Fig. 4: Peptidomimetic inhibitors block cellular protease activity.
From: Peptidomimetic inhibitors of TMPRSS2 block SARS-CoV-2 infection in cell culture
a Peptidomimetic compounds 2, 4, 5, and 7 as well as camostat mesylate (CM) and FOY-251 were added to Caco-2 cells. After 30 min, the fluorogenic reference substrate Boc-Gln-Ala-Arg-AMC was added, and the reaction rate of substrate degradation was assessed by recording the fluorescence intensity within 2 h. b Peptidomimetic compounds 2, 4, 5, and 7 as well as camostat mesylate (CM) were added to HEK293T cells transiently expressing TMPRSS2, followed by addition of fluorogenic reference substrate Boc-Gln-Ala-Arg-AMC. Graph shows normalized fluorescence intensities after 2 h, corrected for the signal of mock-transfected HEK293T cells. Shown are the means ± SD of n = 1 experiment performed in triplicates (a) or duplicates (b). Calculated IC50 values for each compound are presented in Supplementary Table 6.
