TABLE 4

Glucuronidation activity of the three different UGT2B7 constructs and HLM

The rate values are means ± S.D. (n = 3). The relative expression values of the different UGT2B7 variants (Fig. 3B) are indicated in parentheses. The relative expression level of UGT2B7 in HLM could be determined (see Materials and Methods) and, therefore, its AZT glucuronidation rate could not be normalized.

Rate (pmol · min1 · mg1)Substrate2B7-TL (1.2)2B7-His (3.5)2B7-XHA (1.0)HLM
Actual4-MU2178 ± 1091547 ± 461589 ± 16
Epitestosterone548 ± 11440 ± 39463 ± 26
AZT157 ± 13143 ± 13157 ± 15240 ± 1
Normalized4-MU1794 ± 89447 ± 13**1589 ± 16
Epitestosterone451 ± 8.6127 ± 11***463 ± 26
AZT130 ± 1141 ± 1.7**157 ± 15*
  • The significance of the difference (either lower or higher) in the normalized rates between the -His and -XHC variants and the results with the -TL variant are indicated (p > 0.05): * p > 0.01; ** p > 0.001; *** p > 0.001.