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.