Kinetic parameters of the marker activities in microsomes from six human livers and baculovirus-infected insect cells expressing human CYP
Enzyme | KM | Vmax | CL | RAFCL |
---|---|---|---|---|
μM | pmol/min/pmol CYP | μl/min/pmol CYP | ||
Ethoxyresorufin O-deethylase activity | ||||
HLG 1 | 0.21 | 9.3 | 45.4 | 0.001 |
HLG 4 | 0.47 | 219.2 | 470.4 | 0.012 |
HLG 6 | 0.09 | 63.3 | 744.7 | 0.020 |
HLG 7 | 0.54 | 261.3 | 480.3 | 0.013 |
HLG 10 | 0.22 | 161.4 | 740.4 | 0.019 |
HLG 11 | 0.24 | 216.1 | 919.6 | 0.024 |
rec-CYP1A2 | 0.05 | 1976.1 | 38001.9 | |
Paclitaxel 6α-hydroxylase activity | ||||
HLG 1 | 3.63 | 0.583 | 0.161 | 0.081 |
HLG 4 | 3.00 | 0.573 | 0.191 | 0.096 |
HLG 6 | 2.66 | 0.224 | 0.084 | 0.042 |
HLG 7 | 4.55 | 0.319 | 0.070 | 0.035 |
HLG 10 | 2.58 | 0.342 | 0.132 | 0.067 |
HLG 11 | 3.78 | 0.423 | 0.112 | 0.056 |
rec-CYP2C8 | 2.85 | 5.667 | 1.988 | |
S-Mephenytoin 4′-hydroxylase activity | ||||
HLG 1 | 24.4 | 0.092 | 0.004 | 0.010 |
HLG 4 | 33.9 | 0.278 | 0.008 | 0.022 |
HLG 6 | 50.2 | 1.532 | 0.030 | 0.080 |
HLG 7 | 46.0 | 0.389 | 0.008 | 0.022 |
HLG 10 | 28.0 | 0.252 | 0.009 | 0.024 |
HLG 11 | 52.3 | 0.144 | 0.003 | 0.007 |
rec-CYP2C19 | 24.7 | 9.375 | 0.380 | |
Bufuralol 1′-hydroxylase activity | ||||
HLG 1 | 3.1 | 0.472 | 0.152 | 0.036 |
HLG 4 | 30.1 | 0.161 | 0.005 | 0.001 |
HLG 6 | 8.3 | 0.381 | 0.046 | 0.011 |
HLG 7 | 2.8 | 0.307 | 0.110 | 0.026 |
HLG 10 | 6.7 | 0.116 | 0.017 | 0.004 |
HLG 11 | 8.9 | 0.531 | 0.060 | 0.014 |
rec-CYP2D6 | 1.5 | 6.382 | 4.255 | |
Testosterone 6β-hydroxylase activity | ||||
HLG 1 | 36.9 | 13.7 | 0.372 | 0.078 |
HLG 4 | 32.9 | 12.4 | 0.375 | 0.079 |
HLG 6 | 42.7 | 12.4 | 0.290 | 0.061 |
HLG 7 | 46.0 | 7.1 | 0.155 | 0.033 |
HLG 10 | 39.5 | 23.1 | 0.585 | 0.122 |
HLG 11 | 44.2 | 4.0 | 0.091 | 0.019 |
rec-CYP3A4 | 34.6 | 165.4 | 4.780 |