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)
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