TABLE 3.
Km determinations for wild-type uPA and variants and Ki for inhibition of Nb4 mutants and uPA mutants
The data represent the mean ± S.D. of three independent experiments.
| Km | Ki | Ki (mut)/Ki (WT) | |
|---|---|---|---|
| mm | nm | ||
| uPA variant | |||
| Wild type | 0.12 ± 0.02 | 1.20 ± 0.08 | 1 |
| R35A | 0.11 ± 0.01 | 20.7 ± 0.4 | 17 |
| H37A | 0.12 ± 0.01 | 19.0 ± 3.0 | 16 |
| S37dA | 0.09 ± 0.01 | 0.34 ± 0.06 | 0.3 |
| D60aA | 0.09 ± 0.01 | 10.0 ± 1.0 | 8 |
| Y60bA | 0.09 ± 0.01 | 1.0 ± 0.2 | 0.75 |
| H99A | 0.46 ± 0.13 | 168 ± 6.0 | 140 |
| K143A | 0.12 ± 0.01 | 82 ± 6.0 | 68 |
| Y151A | 0.36 ± 0.02 | 5.8 ± 0.4 | 5 |
| Q192A | 0.21 ± 0.03 | 10.3 ± 0.3 | 8.5 |
| Nb4 variant | |||
| Wild type | 1.80 ± 0.15 | 1 | |
| S31A | 2.1 ± 0.1 | 1.1 | |
| D99A | >4000 | >4000 | |
| S106A | 61 ± 4.0 | 33 | |
| E107A | 3.6 ± 0.1 | 1.5 | |
| S108A | 11 ± 1.0 | 6 | |
| R110A | >4000 | >4000 | |
| R111A | >4000 | >4000 | |
| R112A | 2.6 ± 0.1 | 1.4 | |
| Y113A | 61 ± 4.0 | 33 | |