Table 1. Reported Kinetic Parameters for Transport of BCRP Substrates.
Km and Vmax are the transport affinity constant and the maximal rate of BCRP-mediated transport, respectively. Transport studies were carried out using BCRP-enriched plasma membrane vesicles unless otherwise indicated.
| Substrate | Expression system | Km (μM) | Vmax (nmol/min/mg protein) | Reference |
|---|---|---|---|---|
| Estrone 3-sulfate | K562 human myelogenous leukaemia cells | 6.8 ± 1.4 | 1.4 ± 0.3 | [132] |
| The yeast Pichia pastoris | 3.6 ± 0.3 | 0.055 ± 0.002 | [69] | |
| SN-38 | PC-6 human small cell lung cancer cells | 4.0 | 0.714 | [133] |
| SN-38-glucuronide | PC-6 human small cell lung cancer cells | 26 | 0.833 | [133] |
| Methotrexate | HEK293 cells | 1340 ± 180 | 0.687 ± 0.087 | [122] |
| Sf9 insect cells | 6000 | N/R | [134] | |
| E217βG | HEK293 cells | 44.2 ± 4.3 | 0.103 ± 0.017 | [122] |
| 4-MUS | P388 mouse lymphoma cells | 12.9 ± 2.1 | N/R | [135] |
| E3040S | P388 mouse lymphoma cells | 26.9 ± 4.0 | N/R | [135] |
| Hematoporphyrin | Sf9 insect cells | 17.8 | 0.654 | [120] |
| Glyburidea | HEK293 cells | 13.1 ± 1.2 | 0.101 ± 0.034 | [32] |
| Sulfasalazine | Mammalian cells | 0.70 ± 0.03 | 0.052 ± 0.001 | [136] |
a
The Km and Vmax values for glyburide are apparent kinetic parameters estimated in cellular accumulation experiments. SN-38, 7-ethyl-10-hydroxycamptothecin; E217βG, 17β-estradiol 17-(β-D-glucuronide); 4-MUS, 4-methylumbelliferone sulfate; E3040, 6-hydroxy-5,7-dimethyl-2-methylamino-4-(3-pyridylmethyl)benzothiazole; E3040S, E3040 sulfate; N/R, not reported.