TABLE 1.
CYP1A2 | Phenacetin O-Deethylation |
|||
---|---|---|---|---|
kcata | Kma | kcat/Kmb | [(kcat/Km)mutant/(kcat/Km)WT] | |
min | μM | μM/min | ||
WT | 1.28 ± 0.08 | 59.70 ± 1.82 | 0.02 ± 0.01 | 1.00 |
T124S | 0.29 ± 0.03 | 28.90 ± 1.10 | 0.01 ± 0.01 | 0.47 |
T223N | 0.30 ± 0.01 | 26.99 ± 0.01 | 0.01 ± 0.01 | 0.52 |
V227G | 0.38 ± 0.02 | 32.36 ± 2.93 | 0.01 ± 0.01 | 0.55 |
N312L | 0.31 ± 0.01 | 25.26 ± 0.01 | 0.01 ± 0.01 | 0.57 |
L382V | 3.03 ± 0.06 | 5.75 ± 0.57 | 0.53 ± 0.04 | 24.77 |
L382V/T223N | 3.91 ± 0.10 | 7.77 ± 0.80 | 0.51 ± 0.06 | 23.65 |
L382V/N312L | 3.05 ± 0.15 | 16.14 ± 2.05 | 0.19 ± 0.02 | 8.87 |
L382V/T223N/N312L | 3.67 ± 0.10 | 32.42 ± 11.31 | 0.12 ± 0.04 | 5.61 |
L382V/T124S/N312L | 2.81 ± 0.03 | 10.13 ± 2.40 | 0.28 ± 0.07 | 13.34 |
Data are means of triplicate determinations.
kcat/Km represents substrate specificity.