Tricyclic isoxazoles are novel inhibitors of the multidrug resistance protein (MRP1).

@article{Norman2002TricyclicIA,
  title={Tricyclic isoxazoles are novel inhibitors of the multidrug resistance protein (MRP1).},
  author={Bryan H. Norman and Joseph Michael Gruber and Sean P. Hollinshead and Joseph W. Wilson and James J. Starling and Kevin C L Law and Tracy D Self and Linda B. Tabas and Daniel C Williams and Donald C. Paul and Margaret M. Wagner and Anne H. Dantzig},
  journal={Bioorganic \& medicinal chemistry letters},
  year={2002},
  volume={12 6},
  pages={
          883-6
        }
}
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TLDR
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References

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TLDR
LY335979 is an extremely potent Pgp modulator, and not MRP1 or MRP2, modulator and has a significantly lower affinity for CYP3A than for Pgp, which is in good agreement with the previously determined K(i) value.
The MRP gene encodes an ATP-dependent export pump for leukotriene C4 and structurally related conjugates.
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TLDR
Transfecting two different eukaryotic expression vectors containing MRP complementary DNA into HeLa cells to study the pharmacological phenotype produced exclusively by overexpression of human MRP indicates that drug-resistant cell lines generated by transfection with MRp complementary DNA display some but not all of the characteristics of MRP-overexpressing cell lines produced by drug selection in vitro.
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TLDR
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TLDR
Evidence is provided of the ability of MRP to transport cysteinyl leukotriene C4 in membrane vesicles from MRP-transfected HeLa cells (T14), as well as drug-selected H69AR lung cancer cells which express high levels of MRp.
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TLDR
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TLDR
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