TABLE 5

Characteristics of CYP2B6 variants expressed in COS-1 cellsa


Variant

Apoprotein

Km

Vmax

Vmax/Km
% CYP2B6.1 μM bupropion pmol/mg/min % CYP2B6.1
CYP2B6.1 wild type 100 65 215 100
CYP2B6.8 K139E 0 N.D. N.D. N.D.
CYP2B6.10 Q21L, R22C 120.3 72 192 80.6
CYP2B6.11 M46V 16.2 N.A. ∼4b ∼2b
CYP2B6.12 G99E 7.5 N.D. N.D. N.D.
CYP2B6.14 R140Q 82.5 117 48.7 12.5
CYP2B6.15 I391N
18.1
N.D.
N.D.
N.D.
  • N.D., not detectable after correction for background due to ∼4.4 ppm of contaminating product in bupropion substrate; N.A., not applicable due to linear relationship.

  • a All values are means of two independent experiments.

  • b At 1.6 mM substrate concentration.