TABLE 1

Rates of O-deethylation and 3-hydroxylation of 7-ethoxycoumarin by various CYP102A1 mutants

Assays were performed using 2.0 mM 7-ethoxycoumarin as described under Materials and Methods. Values are the mean ± S.D. of triplicate determinations.


Enzyme

O-Deethylation

3-Hydroxylation
nmol product/min/nmol P450
Wild type 0.11 ± 0.01 0.14 ± 0.01
Mutant
1 0.78 ± 0.01 1.7 ± 0.1
2 0.89 ± 0.01 0.86 ± 0.02
3 0.98 ± 0.04 1.1 ± 0.1
4 0.22 ± 0.01 0.35 ± 0.01
5 2.7 ± 0.1 2.5 ± 0.1
6 0.44 ± 0.02 1.3 ± 0.1
7 1.1 ± 0.1 1.6 ± 0.1
8 11 ± 1 18 ± 1
9 6.7 ± 0.1 12 ± 1
10 5.8 ± 0.4 17 ± 1
11 0.65 ± 0.01 2.3 ± 0.1
12 0.68 ± 0.01 1.6 ± 0.1
13 3.1 ± 0.1 13 ± 1
14 2.3 ± 0.1 7.7 ± 0.1
15 2.6 ± 0.1 8.6 ± 0.1
16 2.8 ± 0.1 15 ± 1
17
2.9 ± 0.2
16 ± 1