Table 1. Kinetic Parameters of Dipeptide Nitriles 1a and 1b and Dipeptide Alkynes 2a and 2b with Respect to Cathepsins B, S, L, and Ka.
compound | R | CatB | CatS | CatL | CatK |
---|---|---|---|---|---|
Ki (μM) | |||||
1a | F | 0.109 ± 0.023 | 0.406 ± 0.040 | 0.661 ± 0.011 | 25.94 ± 0.58 |
1b | H | 0.042 ± 0.003 | 0.046 ± 0.004 | 0.220 ± 0.004 | 8.81 ± 0.17 |
kinact/KI (M–1 s–1) | |||||
2a | F | 22 ± 2 | 58 ± 1 | 30 ± 3 | 3 ± 0,1 |
2b | H | 85 ± 3 | 682 ± 85 | 281 ± 30 | 48 ± 5 |
Data shown are mean values ± SEM of three experiments, each performed in duplicate.