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. 2010 Jul;38(7):1039–1045. doi: 10.1124/dmd.109.030767

TABLE 1.

Kinetic parameters for phenacetin O-deethylation by purified CYP1A2 WT and mutants

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
a

Data are means of triplicate determinations.

b

kcat/Km represents substrate specificity.