Figure 3
From: PK/PD investigation of antiviral host matriptase/TMPRSS2 inhibitors in cell models
Effect of protease inhibitors at various concentrations (10, 25, and 50 µM) on CYP3A4 enzyme activity. The reference inhibitor (INH) ketoconazole (30 µM) significantly suppressed the activity of CYP3A4 (***p < 0.01). MI-463 (***p < 0.01), MI-472 (***p < 0.01), MI-485 (***p < 0.01), MI-1903 (***p < 0.01), and MI-1904 (10 and 25 µM, ***p < 0.01; 50 µM, **p < 0.01) all had a significant inhibitory effect on CYP3A4. MI-21 at 10, 25 and 50 µM did not significantly suppress CYP3A4 activity (p > 0.05). Relative fluorescence units (RFUs) of each compound (λex/em = 535/587 nm) are depicted as mean values ± S.E.M. (n = 3; MI-21, n = 4).
