hBCRP (ABCG2)
➦ The ATP-dependent efflux transporter BCRP (Breast Cancer Resistance Protein) functions as a xenobiotic transporter which may play a major role in multi-drug resistance. It likely serves as a cellular defense mechanism in response to mitoxantrone and anthracycline exposure. Recently it has been shown to transport organic anions but also steroids like cholesterol, estradiol, progesterone, and testosterone.
| Main localization: | Liver, kidney, placenta (apical membranes) |
| Transporter assay: | Vesicle-based transporter assay (potential inhibitors or substrates) |
| Probe substrates: | Estrone-3-sulfate |
| Probe inhibitors: | Ko143, Elacridar, Sulfasalazine |
| Regulatory relevance: | FDA and EMA guidance |
| Important interacting drugs: | Elacridar (GF120918), Statins, Ritonavir, Cyclosporine |
| From other species: | mBcrp |
➦ Concentration dependent inhibition of hBCRP-mediated ES uptake by the probe inhibitor Elacridar (GF120918)
