TABLE 5

Phenacetin O-deethylation rates and comparisons for CYP2A6 and mutations thereof. All assays used 250 μM phenacetin.

Protein
Rate of Product Formationa
(Activitymutant/ActivityCYP2A13)
pmol/min/pmol
2A6 0.08 ± 0.04 1.00
   V110L 0.31 ± 0.11 3.90
   V117A –b N.A.
   I208S –b N.A.
   S213A 0.08 ± 0.00 0.95
   I300F 0.21 ± 0.04 2.66
   G301A 0.07 ± 0.01 0.84
   V365M 0.13 ± 0.03 1.69
   I366L –b N.A.
   S369G 0.21 ± 0.05 2.59
   R372H 0.14 ± 0.09 1.73
   V365M/I366L 0.12 ± 0.04 1.50
   I300F/G301A 0.63 ± 0.09 7.85
   I208S/I300F/G301A 0.81 ± 0.12 10.17
   I300F/G301A/S369G 1.02 ± 0.09 12.86
   I208S/I300F/G301A/S369G
3.03 ± 0.29
38.08

  • N.A., not applicable

  • ↵ a Data represent the average of two independent experiments each conducted in triplicate

  • ↵ b –, value below the detection limit of our system (0.026 pmol/min/pmol)