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ATP-binding cassette transporter G member 2 (ABCG2), also known as Breast cancer resistance protein (BCRP), is a membrane-bound half-transporter from the G subfamily of ATP-binding cassette (ABC) transporters[1][2]. This protein functions primarily as an efflux pump, utilizing ATP hydrolysis to export a wide range of substrates, including chemotherapeutic drugs, porphyrins, steroids, and other xenobiotics, out of cells[1][2][5]. ABCG2 is implicated in multidrug resistance in various cancers, affecting the absorption, distribution, and elimination of numerous pharmaceuticals[1][2]. In addition to its role in cancer, ABCG2 participates in physiological processes such as porphyrin homeostasis, and genetic variants have been linked to disorders such as gout[5]. It represents an important therapeutic target for overcoming drug resistance and modulating drug bioavailability.
Drug efflux (active transport of drugs out of cells via ATP hydrolysis) Limiting intracellular concentration of chemotherapeutics Modulating absorption and distribution of drugs
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