TABLE 2

Kinetic parameters of T-5224 glucuronidation for G2 and G3 in recombinant human UGT isoforms

Each value represents a best-fit value ± computer-calculated S.E. of triplicate points.

GlucuronideUGT IsoformVmaxKmKsiVmax/Kmkcatkcat/Km
pmol · min1 · mg protein1μMμMμl · min1 · mg protein1s1M1 · s1
G21A1664 ± 4107.91 ± 5.891.54 ± 1.1183.97.20 × 10−3903
1A3112 ± 277.21 ± 2.6413.5 ± 5.015.51.82 × 10−3252
G31A1146 ± 735.56 ± 3.854.67 ± 3.1226.21.58 × 10−3284
1A3849 ± 48517.9 ± 11.82.55 ± 1.6747.51.38 × 10−2774
1A8206 ± 886.05 ± 3.443.64 ± 2.0034.01.84 × 10−3303