Substrate | Pooled HLM Activity | UGT2B15*1 Activity | UGT2B15*2 Activity | ||
---|---|---|---|---|---|
pmol/min/mg | pmol/min/mg | % HLM | pmol/min/mg | % UGT2B15*12-a | |
S-Oxazepam | 32 ± 2 | 3.4 ± 0.3 | 9.9 ± 0.8 | 0.21 ± 0.08 | 20 ± 5 |
Eugenol | 7271 ± 1266 | 229 ± 45 | 3.2 ± 0.6 | 10 ± 5 | 15 ± 5 |
Naringenin | 2856 ± 258 | 87 ± 6 | 3.0 ± 0.2 | 2.2 ± 1.42-b | 8 ± 3 |
4-Methylumbelliferone | 3182 ± 277 | 152 ± 8 | 4.8 ± 0.3 | 13 ± 5 | 29 ± 6 |
Androstane-3a-diol | 1763 ± 144 | 83 ± 10 | 4.7 ± 0.5 | 5.9 ± 1.52-b | 23 ± 4 |
Dihydrotestosterone | 934 ± 190 | 29 ± 3 | 3.1 ± 0.5 | 5.9 ± 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).