IC50 values of cysteinyl leukotriene derivatives on the uptake of [3H]E217βG
| IC50 | Wild-Type Mrp2 | K325M | R586L |
|---|---|---|---|
| μM | |||
| LTC4 | 0.65 ± 0.12 | 16.0 ± 9.02-150 | 5.95 ± 4.2 |
| LTD4 | 5.48 ± 0.98 | 11.0 ± 3.4 | 13.1 ± 5.9 |
| LTE4 | 9.83 ± 1.4 | 14.7 ± 4.2 | 4.83 ± 1.3 |
| LTF4 | 10.0 ± 4.6 | 15.2 ± 5.9 | 9.27 ± 2.7 |
| MK571 | 2.62 ± 1.1 | 3.26 ± 0.88 | 2.50 ± 0.69 |
The effect of a series of cysteinyl leukotrienes on the uptake of [3H]E217βG (55 nM) was examined at 37°C in membrane vesicles expressing wild-type Mrp2, K325M, and R586L. The IC50 values were calculated by subtracting the uptake into GFP-control vesicles from that of Mrp2-expressing vesicles. Each represents the obtained parameter ± computer-calculated S.D.
↵2-150 p < 0.05, significantly different from wild-type Mrp2 by ANOVA followed by Dunnett's test.