Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export
2000

How MRP2 Protein Affects Drug and Glutathione Transport

publication

Author Information

Author(s): Evers R, Haas M de, Sparidans R, Beijnen J, Wielinga P R, Lankelma J, Borst P

Primary Institution: The Netherlands Cancer Institute

Hypothesis

The study investigates the relationship between the transport of vinblastine and sulfinpyrazone by MRP2 and glutathione export.

Conclusion

The transport of sulfinpyrazone and vinblastine by MRP2 is linked to glutathione export, but at high concentrations, sulfinpyrazone is transported without glutathione.

Supporting Evidence

  • MRP1 routes to the lateral plasma membrane, while MRP2 routes to the apical plasma membrane in polarized MDCKII cells.
  • MRP1 transports daunorubicin, and MRP2 transports vinblastine.
  • Glutathione transport in MDCKII-MRP1 cells is inhibited by various organic anion transport inhibitors.
  • GSH export in MDCKII-MRP2 cells is stimulated by low concentrations of sulfinpyrazone or indomethacin.

Takeaway

This study shows that a protein called MRP2 helps move certain drugs and a substance called glutathione in cells, but too much of one drug can change how this works.

Methodology

The study used polarized MDCKII cells to examine the transport of drugs and glutathione.

Digital Object Identifier (DOI)

10.1054/bjoc.2000.1262

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