Activation of 7-BFC-debenzylation by LCA in human and chimpanzee wild-type (wt) CYP3A4, and in five human CYP3A4 mutants
The activity was determined using the standard NADPH system at 20 μM 7-BFC. The data are the mean ± S.D. of three independent experiments.
P450 | Activity | -Fold Activation | ||
|---|---|---|---|---|
| No LCA | 100 μM LCA | |||
| nmol/min/nmol P450 | ||||
| Chimpanzee wt | 2.05 ± 0.46 | 2.5 ± 0.43 | 1.22 ± 0.19 | |
| Human wt | 2.22 ± 0.15 | 6.23 ± 0.68 | 2.80 ± 0.31 | |
| H54R | 2.41 ± 0.28 | 4.65 ± 0.73 | 1.93 ± 0.33 | |
| Q78R | 2.37 ± 0.26 | 5.01 ± 0.75 | 2.11 ± 0.34 | |
| L129I | 2.53 ± 0.28 | 4.85 ± 0.78 | 1.85 ± 0.35 | |
| T224I | 2.61 ± 0.34 | 4.42 ± 0.63 | 1.69 ± 0.29 | |
| S478R | 2.05 ± 0.22 | 5.15 ± 0.82 | 2.51 ± 0.37 | |