TABLE 2.
Estrone Sulfate and CPIII transport kinetics by OATP2B1 and its genetic variants.
| Variant | Vmax a (pmol∙mg protein−1∙min−1) | Km a (µM) | CL (Vmax/Km) (µL∙mg protein−1 min−1) | |
|---|---|---|---|---|
| Estrone Sulfate | OATP2B1 Ref | 91.6 ± 5.2 | 5.9 ± 1.2 | 15.6 |
| c.76-84del | 70.2 ± 8.1 | 4.1 ± 1.8 | 17.0 | |
| c.332G>A | N.D. | N.D. | 0.25b | |
| c.601G>A | 68.1 ± 6.8 | 4.0 ± 1.6 | 17.1 | |
| c.917G>A | 46.2 ± 3.9 | 1.9 ± 0.7 | 24.8 | |
| c.935G>A | 63.9 ± 5.1 | 2.8 ± 1.0 | 22.5 | |
| c.1457C>T | N.D. | N.D. | 0.38b | |
| CPIII | OATP2B1 Ref. | 25.5 ± 1.5 | 0.034 ± 0.011 | 743 |
| c.76-84-del | 54.8 ± 5.2 | 0.051 ± 0.025 | 1,069 | |
| c.332G>A | 6.8 ± 0.8 | 0.055 ± 0.034 | 125 | |
| c.601G>A | 40.4 ± 4.9 | 0.052 ± 0.033 | 775 | |
| c.917G>A | 62.7 ± 8.0 | 0.058 ± 0.038 | 1,077 | |
| c.935G>A | 40.8 ± 3.1 | 0.066 ± 0.027 | 629 | |
| c.1457C>T | 40.5 ± 4.1 | 0.062 ± 0.032 | 649 |
a
Mean ± standard error of estimate.
b
Estimated uptake clearance based on linear regression; N.D., not determined.