Table 6 Kinetic parameters of zidovudine O-glucuronidation by single expressed UGT2B7*NHA and double expressed UGT1A1*NCFP/2B7*NHA systems.

From: Inter-isoform Hetero-dimerization of Human UDP-Glucuronosyltransferases (UGTs) 1A1, 1A9 and 2B7 and Impacts on Glucuronidation Activity

2B7*N or 1A1*N/2B7*N

Km (μM)

Vmax (pmol/min/unit)

CLint (nL/min/unit)

% of 2B7*NHA

2B7*1HA

508.2 ± 18.59

37.64 ± 0.50

74.06

100

1A1*1CFP/2B7*1HA

585.2 ± 17.52*

66.47 ± 0.76***

113.59***

153.4

1A1*1bCFP/2B7*1HA

490.3 ± 43.26

40.55 ± 1.26*

82.70*

111.7

2B7*71SHA

533.5 ± 25.61

68.80 ± 1.23

141.86

100

1A1*1CFP/2B7*71SHA

456.4 ± 13.43*

49.76 ± 0.51***

109.03**

84.6

1A1*1bCFP/2B7*71SHA

806.0 ± 62.58**

41.17 ± 1.38***

51.08***

39.62

2B7*2HA

570.1 ± 34.18

24.88 ± 0.57

48.01

100

1A1*1CFP/2B7*2HA

395.2 ± 12.61**

72.91 ± 0.77***

184.49***

422.6

1A1*1bCFP/2B7*2HA

621.9 ± 34.19

17.64 ± 0.38***

28.36***

59.1

  1. Asterisks indicate statistically significant differences compared with UGT2B7*NHA single expression systems (***P < 0.0001, **P < 0.005, *P < 0.05). Data are mean ± SD of three independent determinations.
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