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Research ArticleGASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

Interaction of 2,3-Dimercapto-1-propane Sulfonate with the Human Organic Anion Transporter hOAT1

Florian Islinger, Michael Gekle and Stephen H. Wright
Journal of Pharmacology and Experimental Therapeutics November 2001, 299 (2) 741-747;
Florian Islinger
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Michael Gekle
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Stephen H. Wright
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Abstract

The kidney is the primary target organ in which inorganic mercury (Hg2+) accumulates and expresses its toxic effects. The chelating agent 2,3-dimercapto-1-propanesulfonic acid (DMPS) can rapidly reduce the renal burden of mercury and increase the urinary excretion of mercury. However, the cellular and molecular basis of its efficacy is still unknown. A number of previous studies implicated the “classical organic anion secretory pathway” in the secretion of DMPS and its chelation products. In this study we used the human ortholog of the organic anion transporter (hOAT1) expressed in theXenopus oocyte expression system to study the interaction of DMPS and its mercury chelates with hOAT1. [3H]PAH was used to show the transport activity of hOAT1 (Km = 3.9 ±1.3 μM). Uptake of [3H]para-aminohippuric acid (PAH) was inhibited by reduced DMPS (Ki = 22.4 ± 8.4 μM). We also investigated the interaction of oxidized DMPS with hOAT1 because it has been shown that at least 80% of DMPS in the blood is oxidized within 30 min. Oxidized DMPS also inhibited uptake of [3H]PAH (Ki = 66 ±13.6 μM). In contrast, we found no interaction of the DMPS-Hg chelate with hOAT1. To determine whether DMPS and oxidized DMPS are transported by hOAT1 we examined the effect of inwardly directed gradients these two compounds on efflux of [3H]PAH from HeLa cells transiently transfected with hOAT1. Gradients of both DMPS and oxidized DMPS significantlytrans-stimulated efflux of [3H]PAH. These data suggest that hOAT1 can transport DMPS and oxidized DMPS, whereas the DMPS-Hg chelate has no significant affinity for the transporter.

Footnotes

  • This work was supported in part by National Institutes of Health Grants DK56224 and ES04940.

  • Abbreviations:
    DMPS
    2,3-dimercapto-1-propanesulfonic acid
    BAL
    2,3-mercaptopropanol
    PAH
    para-aminohippuric acid
    OAT
    organic anion transporter
    hOAT1
    human ortholog of the organic anion transporter
    BSP
    sulfobromophthalein
    BSA
    bovine serum albumin
    MRP2
    multidrug resistance-associated protein 2
    • Received May 17, 2001.
    • Accepted July 21, 2001.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 299 (2)
Journal of Pharmacology and Experimental Therapeutics
Vol. 299, Issue 2
1 Nov 2001
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Research ArticleGASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

Interaction of 2,3-Dimercapto-1-propane Sulfonate with the Human Organic Anion Transporter hOAT1

Florian Islinger, Michael Gekle and Stephen H. Wright
Journal of Pharmacology and Experimental Therapeutics November 1, 2001, 299 (2) 741-747;

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Research ArticleGASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

Interaction of 2,3-Dimercapto-1-propane Sulfonate with the Human Organic Anion Transporter hOAT1

Florian Islinger, Michael Gekle and Stephen H. Wright
Journal of Pharmacology and Experimental Therapeutics November 1, 2001, 299 (2) 741-747;
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