BCRP
Breast Cancer Resistance Protein (BCRP)
The Breast Cancer Resistance Protein (BCRP), also known as ATP-binding cassette sub-family G member 2 (ABCG2), is a protein that in humans is encoded by the *ABCG2* gene. BCRP is a member of the ATP-binding cassette (ABC) transporter family, which is involved in the transport of various molecules across extracellular and intracellular membranes.
Function[edit | edit source]
BCRP functions as a xenobiotic transporter, playing a crucial role in the efflux of drugs and xenobiotics from cells. It is known for its ability to confer multidrug resistance (MDR) to cancer cells by actively transporting a wide range of chemotherapeutic agents out of the cells, thereby reducing their intracellular concentrations and effectiveness.
BCRP is expressed in various tissues, including the placenta, liver, intestine, and blood-brain barrier, where it serves protective roles by limiting the absorption and distribution of potentially harmful substances.
Clinical Significance[edit | edit source]
BCRP is of significant interest in the field of oncology due to its role in drug resistance. Overexpression of BCRP in cancer cells is associated with resistance to several anticancer drugs, including mitoxantrone, topotecan, and methotrexate. This makes BCRP a target for overcoming drug resistance in cancer therapy.
In addition to its role in cancer, BCRP is also involved in the pharmacokinetics of various drugs, affecting their absorption, distribution, metabolism, and excretion (ADME). It is important in the context of drug-drug interactions and personalized medicine.
Genetic Variability[edit | edit source]
The *ABCG2* gene exhibits genetic polymorphisms that can influence the expression and function of BCRP. These polymorphisms can affect an individual's response to drugs and susceptibility to certain diseases. For example, the Q141K polymorphism is associated with altered BCRP function and has been studied in relation to drug pharmacokinetics and disease risk.
Research and Development[edit | edit source]
Research on BCRP continues to explore its role in drug resistance and its potential as a therapeutic target. Inhibitors of BCRP are being developed to enhance the efficacy of chemotherapeutic agents by preventing drug efflux from cancer cells.
Also see[edit | edit source]
- Multidrug resistance
- ATP-binding cassette transporter
- Chemotherapy
- Pharmacokinetics
- Genetic polymorphism
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Contributors: Prab R. Tumpati, MD
