Table 1

Kinetic parameters for the transport of DNP-SG and E217βG by wild-type Mrp2, K325M, and R586L

E217βGDNP-SG
KmIC50KmIC50
μM μM
Wild-type Mrp23.91  ± 0.9313.3  ± 2.31-163 80.8  ± 7.019.3  ± 3.51-163 1-154
K325M0.40  ± 0.051-160 N.D.N.D.360  ± 891-160
R586L1.40  ± 0.461-160 2.30  ± 1.171-160 308  ± 511-160 59.5  ± 9.81-163

K m and IC50 values were calculated on the basis of the data shown in Figs. 4 and 5, respectively. Each represents the obtained parameter ± computer calculated S.D. Comparison ofK m values for E217βG and DNP-SG, respectively, was performed by ANOVA followed by Dunnett's test, whereas that of IC50 and K m values for E217βG and DNP-SG, respectively, was performed by Student'st test.

    • N.D., not determined.

    • 1-160p < 0.01, significantly different from wild-type Mrp2.

    • 1-163p < 0.01 and

    • 1-154p < 0.001, significantly different from respective K m value.