Table 3

Kinetic parameters for CYP3A4 substrates showing sigmoidicity

SubstratePathwayVmaxS50nH factorCLmaxSmaxReference, System
min−1 μM μl/min/pmol CYP μM
Aflatoxin B13-hydroxylation8.1432.40.510.09650 Ueng et al., 1997, E. coli
Aflatoxin B13-hydroxylation1273.60.550.02135 Ueng et al., 1997, RFP
Aflatoxin B18,9-epoxidation0.9274.10.570.01936 Ueng et al., 1997, E. coli
Aflatoxin B18,9-epoxidation0.1333.80.560.00243 Ueng et al., 1997, RFP
Amitriptyline N-demethylation94901.50.530.010309 Shaw et al., 1997, RFP
Amitriptyline N-demethylation123301.40.550.020172 Ueng et al., 1997, E. coli
Carbamazepine10,11-epoxidation132211.480.530.031135 Korzekwa et al., 1998, VV
Diazepam3-hydroxylation301401.420.540.1276 Kenworthy, 1999, β-LM
Diazepam N-demethylation2.71521.200.640.01140 Kenworthy, 1999, β-LM
Estradiol2-hydroxylation3.7131.30.580.1665.1 Ueng et al., 1997, β-LM
NifedipineOxidation35371.40.550.5219 Shaw et al., 1997, RFP
NifedipineOxidation451420.501.6114 Shaw et al., 1997, BV
Progesterone6β-hydroxylation46321.10.741.064 Ueng et al., 1997, β-LM
Testosterone6β-hydroxylation19511.450.540.2029 Kenworthy, 1999, β-LM
Testosterone6β-hydroxylation150251.70.513.0520 Shaw et al., 1997, BV
Testosterone6β-hydroxylation541601.30.580.2063 Ueng et al., 1997, E. coli