Enzyme kinetic parameters for the dealkylation of BFC by recombinant CYP3A enzymes
S50 and Vmax were calculated by fitting data to the Hill (v = Vmax[S]n/(S50 + [S]n) equation using nonlinear regression analysis and SigmaPlot 7.1 (SPSS Science).
Enzyme | BFC Dealkylation | ||||||
|---|---|---|---|---|---|---|---|
| Vmax
a
| S50
b
| CLintc | n
d
| ||||
| CYP3A64 | 23.0 ± 0.6 | 10.6 ± 0.7 | 2.2 | 1.7 | |||
| CYP3A4 | 12.6 ± 0.4 | 13.5 ± 1.2 | 0.9 | 2.1 | |||
| CYP3A5 | 3.9 ± 0.1 | 11.0 ± 0.6 | 0.4 | 2.2 | |||
| CYP3A12 | 2.9 ± 0.1 | 13.2 ± 1.2 | 0.2 | 1.7 | |||
| CYP3A26 | 0.4 ± 0.0 | 10.9 ± 0.3 | <0.1 | 2.0 | |||
| CYP3A2 | 3.6 ± 0.1 | 13.1 ± 0.9 | 0.3 | 2.1 | |||
| CYP3A1 | 2.0 ± 0.1 | 9.4 ± 1.2 | 0.2 | 1.4 | |||
| CYP3A6 | 0.1 ± 0.0 | 16.0 ± 2.9 | <0.1 | 1.7 | |||