Table 1. Remaining activities (%) of UGTs inhibited by 100 μM TKIs.
| Lapatinib | Vandetanib | Imatinib | Axitinib | Pos. Ctrl. | |
|---|---|---|---|---|---|
| UGT1A1 | 30.8 ± 11.0 | 48.9 ± 4.9 | 34.1 ± 0.5 | 56.7 ± 3.4 | 37.0 ± 2.1 |
| UGT1A3 | 96.5 ± 7.5 | 104.1 ± 2.1 | 88.8 ± 5.1 | 47.8 ± 12.8 | 39.4 ± 6.8 |
| UGT1A4a | 40.7 ± 1.9 | 62.8 ± 0.0 | 59.1 ± 3.0 | 14.9 ± 1.8 | 20.3 ± 6.6 |
| UGT1A6 | 88.4 ± 5.9 | 55.1 ± 1.1 | 67.9 ± 7.1 | 85.8 ± 3.5 | 28.2 ± 10.0 |
| UGT1A7 | 37.7 ± 9.3 | 22.7 ± 2.7 | 8.5 ± 3.1 | 25.0 ± 2.5 | 25.6 ± 11.2 |
| UGT1A8 | 73.5 ± 10.6 | 56.0 ± 6.3 | 33.1 ± 9.0 | 54.6 ± 2.4 | 40.2 ± 5.3 |
| UGT1A9 | 51.1 ± 7.9 | 14.1 ± 4.7 | 49.2 ± 1.9 | 44.8 ± 0.2 | 15.2 ± 1.2 |
| UGT1A10 | 73.6 ± 4.8 | 49.0 ± 0.4 | 15.3 ± 9.5 | 55.5 ± 2.7 | 37.8 ± 8.0 |
| UGT2B4 | 105.1 ± 0.2 | 80.8 ± 6.6 | 71.0 ± 3.2 | 42.1 ± 1.6 | NDb |
| UGT2B7 | 90.5 ± 1.0 | 49.8 ± 3.7 | 29.8 ± 5.6 | 55.9 ± 9.7 | 16.4 ± 11.9 |
| UBT2B15 | 109.5 ± 3.1 | 79.2 ± 1.4 | 28.3 ± 3.3 | 49.3 ± 5.2 | 21.6 ± 11.9 |
| UBT2B17 | 94.8 ± 5.7 | 69.7 ± 3.1 | 14.7 ± 8.2 | 55.9 ± 0.3 | ND |
aTFP was used as a substrate, and for all other UGTs, 4-MU was used as substrate.
bno positive inhibitor available.