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Multidrug resistance-associated protein 1 (MRP1/ABCC1) and Multidrug resistance-associated protein 7 (MRP7/ABCC10) are members of the ATP-binding cassette (ABC) transporter superfamily, specifically the C subfamily [1, 5]. These proteins function as primary active transporters that utilize the energy of ATP hydrolysis to pump a diverse range of substrates, including chemotherapeutic drugs and endogenous organic anions, out of cells [2, 4]. MRP1 is ubiquitously expressed and is a major mediator of multidrug resistance (MDR) in various cancers, transporting drugs like vincristine and doxorubicin, as well as physiological substrates like leukotriene C4 [9, 15]. MRP7 is distinct for its ability to transport taxanes (e.g., paclitaxel and docetaxel), which are often poor substrates for other MRPs, thereby contributing to resistance in taxane-based therapies [3, 8]. Both transporters are significant therapeutic targets in oncology, where their inhibition aims to restore drug sensitivity in resistant tumors [7, 12]. However, clinical development of inhibitors has faced challenges due to potential toxicities from blocking the physiological transport functions of these proteins and complex drug-drug interactions [13, 14, 16].
ATP-dependent efflux of substrates across the plasma membrane, reducing intracellular drug accumulation.
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