Table 6.
Effects of Caspase and Granzyme B Inhibitors on SAS-1 and SAS-2 Hydrolytic Activity
| Percent Activity of Noninhibited
|
|||
|---|---|---|---|
| Inhibitor | Preferred Protease Target | SAS-1 | SAS-2 |
| No inhibitor | - | 100% ± 3.0% | 100% ± 2.6% |
| Ac-VAD-CMKa | Pan-Caspase | 1% ± 0.6% | 1% ± 0.1% |
| B-YVAD-CMKa | Caspase-1 | 1% ± 0.1% | 1% ± 0.0% |
| Ac-WEHD-CHOa | Caspase-1 | 1% ± 0.5% | 1% ± 1.2% |
| Ac-LDESD-CHOa | Caspase-2 | 39% ± 2.4% | 49% ± 4.4% |
| Ac-VDVAD-CHOa | Caspase-2 | 1% ± 0.9% | 2% ± 0.8% |
| Ac-DEVD-CMKa | Caspase-3 | 90% ± 4.9% | 91% ± 5.6% |
| Ac-DMQD-CHOa | Caspase-3 | 1% ± 0.7% | 1% ± 0.4% |
| Ac-LEVD-CHOa | Caspase-4 | 1% ± 0.2% | 1% ± 0.9% |
| Ac-VEID-CHOa | Caspase-6 | 1% ± 0.2% | 1% ± 0.8% |
| Ac-IETD-CHOa | Caspase-8 | 1% ± 0.4% | 1% ± 1.5% |
| Ac-LEHD-CMKa | Caspase-9 | 47% ± 1.9% | 58% ± 5.2% |
| Ac-LEED-CHOa | Caspase-13 | 68% ± 3.2% | 67% ± 4.7% |
| Z-AAD-CMKa | Granzyme B | 1% ± 0.6% | 1% ± 1.0% |
Enzymes were preincubated with 200 μM inhibitor for 2 h and then assayed for Z-VAD-AFC hydrolytic activity for 1 h.
Z, benzyloxycarbonyl; Ac, acetyl; B, biotin.
Recognition sequence in single-letter amino acid code.