Breast cancer resistance protein (BCRP) is a member of the ATP-binding cassette (ABC) transporter family that plays a crucial role in drug transport and cellular efflux, particularly in relation to chemotherapy resistance in cancer cells. BCRP is known for its ability to transport a variety of substrates, including anticancer drugs, across cell membranes, impacting drug absorption, distribution, and excretion. Understanding BCRP is essential for addressing drug resistance mechanisms in breast cancer and other cancers.
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BCRP is also known as ABCG2 and is overexpressed in certain breast cancer types, contributing to reduced effectiveness of chemotherapy.
The protein can limit the bioavailability of many anticancer drugs by actively pumping them out of cancer cells, leading to treatment failure.
BCRP is expressed not only in breast tissue but also in various organs like the intestines, liver, and brain, affecting systemic drug distribution.
Inhibitors of BCRP are being researched as potential strategies to overcome drug resistance in cancer therapy.
Genetic polymorphisms in the BCRP gene can affect individual responses to treatment and the risk of developing drug resistance.
Review Questions
How does breast cancer resistance protein (BCRP) contribute to drug resistance in cancer treatment?
BCRP contributes to drug resistance by actively transporting various anticancer drugs out of the cancer cells, thereby reducing their intracellular concentrations and effectiveness. This transporter can limit the bioavailability of chemotherapy agents, making it difficult for these drugs to exert their therapeutic effects. Understanding the function of BCRP helps identify potential strategies to enhance drug efficacy against resistant cancer cells.
Discuss the implications of BCRP expression on the pharmacokinetics of anticancer drugs.
The expression of BCRP significantly impacts the pharmacokinetics of anticancer drugs by influencing their absorption, distribution, metabolism, and excretion. Since BCRP can pump drugs out of cells in organs such as the intestines and liver, it can reduce the systemic availability of these medications. This leads to lower therapeutic concentrations in tissues, which can result in inadequate treatment responses and necessitates consideration of BCRP inhibitors or alternative dosing strategies.
Evaluate the potential role of targeting BCRP in overcoming multidrug resistance in breast cancer therapy.
Targeting BCRP presents a promising strategy for overcoming multidrug resistance in breast cancer therapy. By inhibiting the action of BCRP, researchers aim to increase the retention of chemotherapeutic agents within cancer cells, thus enhancing their effectiveness. Clinical studies investigating BCRP inhibitors alongside standard chemotherapy are essential to determine their efficacy and safety, which could lead to improved treatment outcomes for patients with resistant breast cancers.
Related terms
ATP-binding cassette (ABC) transporters: A large family of membrane proteins that use ATP hydrolysis to transport various substrates across cellular membranes, involved in drug absorption and resistance.
A phenomenon where cancer cells become resistant to multiple drugs with different structures and mechanisms of action, often due to overexpression of transporters like BCRP.
pharmacokinetics: The study of how drugs are absorbed, distributed, metabolized, and excreted in the body, which is significantly influenced by transport proteins like BCRP.