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Molecular Basis for Reduced Estrone Sulfate Transport and Altered Modulator Sensitivity of TM6 and TM17 Mutants of MRP1 (ABCC1)
Drug Metabolism and Disposition, 04/28/09
Maeno K et al. - Multidrug resistance protein 1 (MRP1) confers drug resistance and also mediates cellular efflux of many organic anions. MRP1 also transports GSH and furthermore, this tripeptide stimulates transport of several substrates including estrone 3-sulfate. The differing abilities of the cysteinyl leukotriene derivatives leukotriene C4, D4 and F4 to inhibit estradiol glucuronide transport by wild-type and K332L mutant MRP1 provide further evidence that TM6-Lys332 is involved in the recognition of the gamma-Glu portion of substrates and modulators containing GSH or GSH-like moieties.
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