Table 2

Inactivation by mifepristone (20 μM) of wild-type and mutant CYP3A enzymes

P450ki(min−1)2-a
CYP3A42-b 0.17
P107S 0.18
F108L 0.14
S119A2-c 0.19
I120L 0.17
N206S 0.12
L210F 2-c 0.15
V296A 0.15
T309A0.24
I369V 2-c 0.13
A370F2-c 0.19
M371I 0.12
V376T 0.18
S478D 0.15
L479T 0.17
G480Q 0.19
212K/214G/219L/224I/225L/230T0.19
CYP3A52-c 0.01

CYP3A4 → CYP3A5 mutants are shown in bold.

  • ↵2-a  Mean of inactivation constants of wild type and various CYP3A4 mutants by methanol (control) was 0.03 min−1.

  • ↵2-b  Inactivation of wild type CYP3A4 by mifepristone was determined using solubilized membrane preparation as well as purified protein with no significant difference in theki.

  • ↵2-c  Purified proteins.