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Research ArticlePERSPECTIVES IN PHARMACOLOGY

Regulation of Expression of the Multidrug Resistance-Associated Protein 2 (MRP2) and Its Role in Drug Disposition

Phillip M. Gerk and Mary Vore
Journal of Pharmacology and Experimental Therapeutics August 2002, 302 (2) 407-415; DOI: https://doi.org/10.1124/jpet.102.035014
Phillip M. Gerk
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Mary Vore
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Abstract

The multidrug resistance protein 2 (MRP2; ABCC2) is an ATP-binding cassette transporter accepting a diverse range of substrates, including glutathione, glucuronide, and sulfate conjugates of many endo- and xenobiotics. MRP2 generally performs excretory or protective roles, and it is expressed on the apical domain of hepatocytes, enterocytes of the proximal small intestine, and proximal renal tubular cells, as well as in the brain and the placenta. MRP2 is regulated at several levels, including membrane retrieval and reinsertion, translation, and transcription. In addition to transport of conjugates, MRP2 transports cancer chemotherapeutics, uricosurics, antibiotics, leukotrienes, glutathione, toxins, and heavy metals. Several mutagenesis studies have described critical residues for substrate binding and various naturally occurring mutations that eliminate MRP2 expression or function. MRP2 is important clinically as it modulates the pharmacokinetics of many drugs, and its expression and activity are also altered by certain drugs and disease states.

Footnotes

  • We gratefully acknowledge Public Health Service Grant GM55343 for support of the work from this laboratory cited here and the Reproductive Sciences Training Program (NIH T32 HD07436) for supporting P.M.G.

  • DOI: 10.1124/jpet.102.035014

  • Abbreviations:
    MRP
    multidrug resistance-associated protein (lower case refers to nonhuman)
    DNP-SG
    2,4-dinitrophenyl-S-glutathione
    E217G
    estradiol-17β(β-d-glucuronide)
    GY/TR−
    Groningen yellow/transport deficient Wistar rat
    EHBR
    Eisai hyperbilirubinemic Sprague-Dawley rat
    TM
    transmembrane domain
    MSD
    membrane-spanning domains
    NBD
    nucleotide-binding domain
    DJS
    Dubin-Johnson syndrome
    MDR
    multidrug resistance transporter
    PhIP
    2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine
    Bsep
    bile salt export pump
    PCN
    pregnenolone 16α-carbonitrile
    ER-8
    everted repeat with an 8-base pair spacer
    FXR
    farnesoid X receptor
    CAR
    constitutive androstane receptor
    PXR
    pregnane X receptor
    RXR
    retinoid X receptor
    RAR
    retinoic acid receptor
    SN-38
    7-ethyl-10-hydroxycamptothecin
    BQ-123
    cyclo(l-Leu-d-Trp-d-Asp-l-Pro-d-Val)
    MK571
    3-[[3-[2-(7-chloroquinolin-2-yl)vinyl]phenyl]-(2-dimethylcarbamoylethylsulfanyl)methylsulfanyl] propionic acid
    NEM-SG
    N-ethylmaleimide-glutathione
    OATP
    organic anion transporting polypeptide
    • Received February 20, 2002.
    • Accepted April 24, 2002.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 302 (2)
Journal of Pharmacology and Experimental Therapeutics
Vol. 302, Issue 2
1 Aug 2002
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Research ArticlePERSPECTIVES IN PHARMACOLOGY

Regulation of Expression of the Multidrug Resistance-Associated Protein 2 (MRP2) and Its Role in Drug Disposition

Phillip M. Gerk and Mary Vore
Journal of Pharmacology and Experimental Therapeutics August 1, 2002, 302 (2) 407-415; DOI: https://doi.org/10.1124/jpet.102.035014

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Research ArticlePERSPECTIVES IN PHARMACOLOGY

Regulation of Expression of the Multidrug Resistance-Associated Protein 2 (MRP2) and Its Role in Drug Disposition

Phillip M. Gerk and Mary Vore
Journal of Pharmacology and Experimental Therapeutics August 1, 2002, 302 (2) 407-415; DOI: https://doi.org/10.1124/jpet.102.035014
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