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Target intelligence / Profile preview
Breast Cancer Resistance Protein (BCRP)
- Target
- BCRP
- Molecular classification
- Transporter, ATP-binding cassette transporter family, ABC transporter
01
Overview
Breast cancer resistance protein (BCRP), also known as ATP-binding cassette sub-family G member 2 (ABCG2), is a membrane-bound efflux transporter belonging to the ATP-binding cassette (ABC) superfamily. It functions primarily as an efflux transporter, using energy from ATP hydrolysis to pump a wide range of substrates—including many chemotherapeutic agents—out of cells. Overexpression of BCRP in tumor cells leads to active efflux of anticancer drugs from these cells, reducing intracellular drug accumulation and causing multidrug resistance. It is an important therapeutic target for overcoming MDR in cancers expressing high levels of this protein.
- Other names
- ABCG2MXRABCPATP-binding cassette sub-family G member 2
02
Mechanism of action
Efflux of substrates (chemotherapeutics, metabolites, xenobiotics) via ATP hydrolysis.
03
Biological functions
Efflux transportDrug resistanceXenobiotic detoxificationRegulation of drug bioavailability
04
Disease associations
CancerMultidrug resistancePhototoxicityProtoporphyria
05
Safety considerations
Potential for drug-drug interactions due to altered drug dispositionInhibition of BCRP may increase exposure to toxic compoundsReversal of multidrug resistance can increase drug toxicity
06
Interacting drugs
Mitoxantrone
7 more in the full profile.
07
Biomarkers
BCRP expression levels in tumor tissueBCRP activity
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