TABLE 5.
Inhibitor profiles of trypanosomal CaaX proteases
| Compounda | Mean % activityb ± SEM for: |
|
|---|---|---|
| T. brucei Rce1 | T. brucei Ste24 | |
| TPCK | 21.6 ± 5.1 | 24.5 ± 5.0 |
| FKBK | 34.4 ± 6.0 | 30.0 ± 3.5 |
| EDTA | 92.0 ± 11.1 | 79.2 ± 10.2 |
| EGTA | 94.6 ± 5.5 | 75.7 ± 3.2 |
| 1 | 30.7 ± 4.8 | 59.4 ± 5.9 |
| 2 | 22.1 ± 4.7 | 24.1 ± 5.3 |
| 3 | 18.6 ± 2.7 | 14.9 ± 5.8 |
| 4 | 23.9 ± 9.5 | 31.3 ± 10.9 |
| 5 | 34.2 ± 9.4 | 35.1 ± 8.6 |
| 6 | 19.3 ± 4.0 | 28.0 ± 2.4 |
| 7 | 18.4 ± 3.8 | 28.6 ± 2.2 |
| 8 | 16.1 ± 3.3 | 14.6 ± 5.4 |
| 9 | 15.4 ± 3.7 | 20.6 ± 3.8 |
a
TPCK, FKBK, EDTA, and EGTA were used at 200 μM. Compounds 1 to 9 are as previously identified and were used at 100 μM (28).
b
Values are relative to an appropriate untreated control treated with H2O (EDTA and EGTA) or DMSO (TPCK, FKBK, compounds 1 to 9).