Table 4.
Inhibtion of α-thrombin hydrolysis of Sar-Pro-Arg-pNA by PAR exodomain.
| Ki (μM)a | Inhibition typeb | R2c | |
|---|---|---|---|
| PAR1-wt | 26 ± 7.7 | NC | 0.97 |
| PAR1-L38A | 38 ± 9.9 | NC | 0.98 |
| PAR1-D39A | 7.1 ± 1.0d | NC | 0.99 |
| PAR1-P40A | 26 ± 12
α = 3.8 ± 2.8 |
M | 0.99 |
| PAR4-wt | 64 ± 23 | C | 0.99 |
| PAR4-L43A | 56 ± 16 | C | 0.98 |
| PAR4-P44A | 41 ± 15 | C | 0.98 |
| PAR4-P46A | 68 ± 25 | C | 0.99 |
| PAR1-wte | (100)f | NI | - |
| PAR4-wte | 110 ± 15 | C | 0.98 |
10 mM Tris·HCl, 150 mM NaCl, pH 8.0, 25°C
a
± 95% confidence interval
b
NC (Noncompetitive), C (Competitive), (M) Mixed, (NI) No Inhibition
c
goodness of fit to inhibition model
d
p < 0.05 compared to wild type sequence
e
In the presence of 10 μM hirugen
f
No inhibition at the concentration in parentheses