Table 3.
Ki constants of human serine proteases inhibited by various APPI-3M variants
| Mutant | aKi [pM] | |||
|---|---|---|---|---|
| Mesotrypsin | Anionic trypsin | Cationic trypsin | KLK6 | |
| Unmodified APPI-3M | 98.0 ± 1.0 | 2.26 ± 0.08 | 22.5 ± 0.6 | 362 ± 10 |
| T11V/G17R | 494 ± 28 | 0.92 ± 0.07 | 2.37 ± 0.17 | 16.4 ± 0.9 |
| T11S/G17R | 1060 ± 30 | 2.98 ± 0.19 | 7.25 ± 0.5 | 124 ± 13 |
| T11S | 581 ± 7 | 1.16 ± 0.09 | 7.63 ± 0.55 | 1000 ± 60 |
| T11V | 65.0 ± 1.0 | 3.72 ± 0.21 | 14.1± 0.5 | 378 ± 9 |
| G17R | 676 ± 8 | 3.58 ± 0.16 | 8.12 ± 0.08 | 77.4 ± 2.6 |
aResults (means ± SD) were obtained from three independent experiments