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Molecular Pharmacology

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Research ArticleArticle

Adenosine Triphosphate-Dependent Transport of Anionic Conjugates by the Rabbit Multidrug Resistance-Associated Protein Mrp2 Expressed in Insect Cells

Rémon A. M. H. van Aubel, Marcel A. van Kuijck, Jan B. Koenderink, Peter M. T. Deen, Carel H. van Os and Frans G. M. Russel
Molecular Pharmacology June 1998, 53 (6) 1062-1067;
Rémon A. M. H. van Aubel
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Marcel A. van Kuijck
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Jan B. Koenderink
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Peter M. T. Deen
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Carel H. van Os
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Frans G. M. Russel
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Abstract

The multidrug resistance-associated protein Mrp2 is expressed in liver, kidney, and small intestine and mediates ATP-dependent transport of conjugated organic anions across the apical membrane of epithelial cells. We recently cloned a rabbit cDNA encoding a protein that on basis of highest amino acid homology and tissue distribution was considered to be the rabbit homolog of rat Mrp2. To investigate whether rabbit Mrp2 mediates ATP-dependent transport similar to rat Mrp2, we expressed rabbit Mrp2 in Spodoptera frugiperda (Sf9) cells using recombinant baculovirus. Mrp2 was expressed as an underglycosylated protein in Sf9 cells and to a higher level compared with rabbit liver and renal proximal tubules. Both 17β-estradiol-17-β-d-glucuronide ([3H]E217βG, 50 nm) and [3H]leukotriene C4 (3 nm) were taken up by Sf9-Mrp2 membrane vesicles in an ATP-dependent fashion. Uptake of [3H]E217βG was dependent on the osmolarity of the medium and saturable for ATP (Km = 623 μm). Leukotriene C4, MK571, phenolphthalein glucuronide, and fluorescein-methotrexate were good inhibitors of [3H]E217βG transport. The inhibitory potency of cyclosporin A and methotrexate was moderate, whereas fluorescein, α-naphthyl-β-d-glucuronide, andp-nitrophenyl-β-d-glucuronide did not inhibit transport. In conclusion, we show direct ATP-dependent transport by recombinant rabbit Mrp2 and provide new data on Mrp2 inhibitor specificity.

Footnotes

  • Send reprint requests to: Dr. F. G. M. Russel, University of Nijmegen, Department of Pharmacology 233, P.O. Box 9101, 6500 HB Nijmegen, The Netherlands. E-mail:f.russel{at}farm.kun.nl

  • This work was supported in part by the Netherlands Organization for Scientific Research through Grants 805–05.041 (J.B.K.) and 900.522.132 (M.A. van K.). P.M.T.D. is an investigator of the Royal Netherlands Academy of Arts and Sciences.

  • Abbreviations:
    MRP2
    multidrug resistance-associated protein 2
    cMOAT
    canalicular multispecific organic anion transporter
    TR−
    transport-deficient rat
    EHBR
    Eisai hyperbilirubinemic rat
    MRP1
    multidrug resistance-associated protein 1
    ABC
    ATP-binding cassette
    CFTR
    cystic fibrosis transmembrane conductance regulator
    LTC4
    leukotriene C4
    E217βG
    17β-estradiol-17-β-d-glucuronide
    FL
    fluorescein
    MTX
    methotrexate
    FL-MTX
    fluorescein methotrexate
    CsA
    cyclosporin A
    MK571
    3-([{3-(2-[7-chloro-2-quinolinyl]ethenyl)phenyl}-{(3-dimethyl-amino-3-oxopropyl)-thio}-methyl]thio)propanoic acid
    • Received January 2, 1998.
    • Accepted March 10, 1998.
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 53 (6)
Molecular Pharmacology
Vol. 53, Issue 6
1 Jun 1998
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Research ArticleArticle

Adenosine Triphosphate-Dependent Transport of Anionic Conjugates by the Rabbit Multidrug Resistance-Associated Protein Mrp2 Expressed in Insect Cells

Rémon A. M. H. van Aubel, Marcel A. van Kuijck, Jan B. Koenderink, Peter M. T. Deen, Carel H. van Os and Frans G. M. Russel
Molecular Pharmacology June 1, 1998, 53 (6) 1062-1067;

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Research ArticleArticle

Adenosine Triphosphate-Dependent Transport of Anionic Conjugates by the Rabbit Multidrug Resistance-Associated Protein Mrp2 Expressed in Insect Cells

Rémon A. M. H. van Aubel, Marcel A. van Kuijck, Jan B. Koenderink, Peter M. T. Deen, Carel H. van Os and Frans G. M. Russel
Molecular Pharmacology June 1, 1998, 53 (6) 1062-1067;
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