Table 5. Inhibitory Activity of Dipeptide Alkynes Containing a Glycine-Derived P1 Moiety with Respect to Cathepsins B, L, S, and Ka.
|
kinact/KI (M–1 s–1) |
||||||
|---|---|---|---|---|---|---|
| 2b | 56c | 56d | 56e | 56f | 62 | |
| CatB | 85(3) | n.i. | n.i. | 4(2) | 34(3) | n.i. |
| CatS | 682(85) | n.i. | n.i. | n.i. | 293(36) | 14(1) |
| CatL | 281(30) | 19(3) | n.i. | 93(11) | n.i. | n.i. |
| CatK | 48(5) | n.i. | n.i. | 260(29) | 179(4) | n.i. |
a
n.i. = no inhibition; i.e., no evidence of irreversible inhibition was discernible within the considered time and concentration ranges. Data shown are mean values ± SEM of three experiments, each performed in duplicate.