TABLE 2.
Effect of NS3 mutations on inhibitory potency of peptide CP5-46–4D5E
A, NS3-4A A156V mutant. Fold change in the IC50 for the mutant NS3-4A protease compared with that for the wild-type (WT) protease. Measurements were carried out in duplicate, the curves were fitted using GraphPad Prism with a nonlinear regression model, and the S.D. is shown. B, effect of mutants R155K and A156V on peptide CP5-46A-4D5E in the cell culture replicon assay. Fold change in the IC50 for the mutant NS3-4A protease compared with that for the WT protease. Measurements were carried out in triplicate and mean values are shown.
| A. Protease | IC50 | Change |
|---|---|---|
| nm | -Fold | |
| NS3-4A WT | 1.14 ± 0.047 | |
| NS3-4A A156V | 1.65 ± 0.248 | 1.5 |
| B. Peptide | IC50 |
Change |
||||
|---|---|---|---|---|---|---|
| WT | R155K | A156V | WT | R155K | A156V | |
| μm | -Fold | |||||
| CP5-46A-4D5E-Ant | 36.4 | 49.3 | 72.5 | 1.0 | 1.4 | 2.0 |
| Ant-CP5-46A-4D5E | 48.4 | 56.7 | 51.4 | 1.0 | 1.2 | 1.1 |