Second-order rate constants of inhibition of thrombin and APC by PCI variants
| Variant . | k2 (M−1⋅s−1) . | SR . | |
|---|---|---|---|
| Thrombin . | APC . | ||
| wt PCI | (2.82 ± 0.15) × 104 | (6.80 ± 0.32) × 102 | 0.024 |
| KRS PCI* | 1.18 × 103* | 6.0 × 102* | 0.5* |
| FRK PCI | (2.24 ± 0.24) × 101 | (8.84 ± 0.74) × 102 | 39.5 |
| KRK PCI | (2.80 ± 0.24) × 101 | (2.80 ± 0.13) × 102 | 10 |
| Variant . | k2 (M−1⋅s−1) . | SR . | |
|---|---|---|---|
| Thrombin . | APC . | ||
| wt PCI | (2.82 ± 0.15) × 104 | (6.80 ± 0.32) × 102 | 0.024 |
| KRS PCI* | 1.18 × 103* | 6.0 × 102* | 0.5* |
| FRK PCI | (2.24 ± 0.24) × 101 | (8.84 ± 0.74) × 102 | 39.5 |
| KRK PCI | (2.80 ± 0.24) × 101 | (2.80 ± 0.13) × 102 | 10 |
Values are rate constants plus or minus standard error.
The rate determination for KRS PCI is a preliminary determination from only 2 measurements (therefore, no error is shown) and was calculated by dividing kobs by the serpin concentration. SR stands for specificity ratio of rate constant for APC over thrombin.