Table 2

Comparative glucuronidation activities for UGT2B15*1 and UGT2B15*2

SubstratePooled HLM ActivityUGT2B15*1 ActivityUGT2B15*2 Activity
pmol/min/mgpmol/min/mg% HLMpmol/min/mg% UGT2B15*12-a
S-Oxazepam32 ± 23.4 ± 0.39.9 ± 0.80.21 ± 0.0820 ± 5
Eugenol7271 ± 1266229 ± 453.2 ± 0.610 ± 515 ± 5
Naringenin2856 ± 25887 ± 63.0 ± 0.22.2 ± 1.42-b 8 ± 3
4-Methylumbelliferone3182 ± 277152 ± 84.8 ± 0.313 ± 529 ± 6
Androstane-3a-diol1763 ± 14483 ± 104.7 ± 0.55.9 ± 1.52-b 23 ± 4
Dihydrotestosterone934 ± 19029 ± 33.1 ± 0.55.9 ± 1.72-b 67 ± 13

Glucuronidation activities for five different substrates were determined as described in Materials and Methods using pooled HLMs and UGT2B15*1 and UGT2B15*2 stably expressed in HEK-293 cells. Shown are the mean values ± S.D. of triplicate determinations. In addition to absolute values, activities are given as a percentage of HLM activity (for UGT2B15*1) and as a percentage of UGT2B15*1 (for UGT2B15*2).

  • 2-a Corrected for 3.3 times higher immunoreactive UGT2B15 protein in UGT2B15*1 compared with UGT2B15*2 microsomal preparations.

  • 2-b These activities for UGT2B15*2 were close to the quantitation limit of the assay (1 pmol/min/mg protein).