TABLE 3

Kinetic parameters of wild-type and L48V UGT1A4 for trans-androsterone, imipramine, cyproheptadine, and tigogenin


Substrate

Parameter

Wild Type

L48V
trans-Androsterone Vmaxa (pmol/min/mg) 107.3 35.7
Kmb (μM) 254.7 8.2
Imipramine Vmax (pmol/min/mg) 872.8 294.9
Km (μM) 1442.0 275.8
Cyproheptadine Vmax (pmol/min/mg) 342.6 203.3
Km (μM) 227.5 86.4
Tigogenin Vmax (pmol/min/mg) 158.6 81.4

Km (μM)
7.8
6.7
  • a Vmax, maximum velocity.

  • b Km, Michaelis constant.