Table 2.
Kinetic parameters for the inhibition of P450s by furan-containing compounds
| Chemical | Enzyme | Ki (μM) | kinact (min−1) | Partition ratioa |
|---|---|---|---|---|
| 4-Ipomeanol | Recombinant P450 3A4113 | 20 | 0.15 | 257 |
| Menthofuran | Recombinant P450 2A6146 | 0.84 | 0.25 | 3.5 ± 0.6 |
| Recombinant P450 2A6147 | 2.2 | 1 | 30 | |
| P450 2A6 activity in HLM146 | 2.5 | 0.22 | ||
| Bergamottin | Recombinant P450 3A4154,159 | 7.7 | 0.3 | ~27 |
| Recombinant P450 2B6159 | 5.2 | 0.087 | ~2 | |
| Recombinant ΔP450 2B6 K262R160 | 8.2 | 0.23 | ||
| Recombinant P450 3A5159 | 20 | 0.045 | ~20 | |
| L-754,394 | P450 3A4 activity in HLM163 | 7.5 | 1.62 | 1.4 |
| P450 2D6 activity in HLM 163 | 32 | 0.18 | 40 | |
| recombinant P450 3A4165 | 7.5 | 4 |
a
nmoles product formed per nmoles enzyme inactivated