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MRP2 and 3 in health and disease

P Borst1, N Zelcer, K van de Wetering

  • 1Division of Molecular Biology, The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands. p.borst@nki.nl

Cancer Letters
|January 3, 2006
PubMed

Insights

Multidrug resistance proteins (MRPs) transport organic anions. Human MRP2 shows allosteric control, unlike rat MRP2, and MRP3 facilitates drug-glucuronide export, not bile salt metabolism.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Multidrug resistance-associated proteins (MRPs) are ATP-binding cassette transporters.
  • MRP2 is crucial for organic anion transport from the liver into bile.
  • MRP3's role in bile salt metabolism is debated.

Purpose of the Study:

  • To investigate the allosteric control of human and rat MRP2.
  • To clarify the physiological role of MRP3 using knockout mice.
  • To highlight challenges in extrapolating findings from rodent models to humans.

Main Methods:

  • Comparative analysis of human and rat MRP2 function.
  • Utilizing Mrp3 knockout (KO) mouse models.
  • Investigating cellular export of drug-glucuronide conjugates.

Main Results:

  • Human MRP2 exhibits allosteric control, whereas rat MRP2 does not.
  • MRP3 knockout mice data do not support a major role in bile salt metabolism.
  • MRP3 is implicated in the cellular export of drug-glucuronide conjugates.

Conclusions:

  • Species-specific differences exist in MRP2 regulation.
  • MRP3's primary function involves drug-glucuronide conjugate transport.
  • Caution is needed when applying findings from murine MRP studies to human physiology.

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