TABLE 4.
Inhibition by 4-CPI or BIF of 7-EFC O-Deethylation by H226Y, K186A, and CSM 8 mutants
|
P450
|
IC50
|
||
|---|---|---|---|
| BIF | 4-CPI | BIF/4-CPI | |
| μM | μM | ||
| H226Y | 0.80 (0.09)a | 0.010 (0.004) | 80 |
| K186A | 0.70 (0.02) | 0.014 (0.002) | 50 |
| R187A | 0.41 (0.02) | 0.033 (0.004) | 12 |
| R187K | 0.46 (0.02) | 0.024 (0.002) | 19 |
| F188A | 0.18 (0.03) | 0.007 (0.001) | 26 |
| D189A | 0.64 (0.16) | 0.009 (0.001) | 71 |
| Y190A | 0.55 (0.11) | 0.025 (0.005) | 22 |
| K191A | 1.0 (0.16) | 0.008 (0.001) | 125 |
| D192A | 0.56 (0.10) | 0.024 (0.006) | 23 |
a
Standard errors for fit to the sigmoidal curve using four-parameter logistic function are shown in parentheses. The variation between two or three experiments is ≤15%.