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Related Experiment Videos

Compound profiling for ABCC2 (MRP2) using a fluorescent microplate assay system.

Frank Förster1, Astrid Volz, Gert Fricker

  • 1Institute of Pharmacy and Molecular Biotechnology, Ruprecht-Karls-University, Heidelberg, Germany.

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V
|November 21, 2007
PubMed
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A new assay using the fluorescent dye Glutathione methylfluorescein (GSMF) allows rapid screening of drug interactions with the ABCC2 (MRP2) transporter. This method aids in identifying compounds that affect MRP2-mediated drug efflux.

Area of Science:

  • Biochemistry
  • Cell Biology
  • Pharmacology

Background:

  • The ATP-binding cassette (ABC) transporter ABCC2, also known as multidrug resistance-associated protein 2 (MRP2), plays a crucial role in the efflux of various xenobiotics and endogenous compounds.
  • Efficient screening methods are needed to identify drug interactions with MRP2, which can impact drug efficacy and toxicity.

Purpose of the Study:

  • To develop and validate a rapid, fluorescence-based assay for screening compounds that interact with the ABCC2 transporter.
  • To utilize the fluorescent dye Glutathione methylfluorescein (GSMF) for assessing MRP2-mediated drug efflux.

Main Methods:

  • Cultured MDCK cells overexpressing ABCC2 were used in a 96-well plate format.
  • Cells were incubated with chloromethylfluorescein-diacetate (CMFDA), which is converted to GSMF intracellularly.

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  • Intracellular fluorescence was measured to monitor GSMF formation and efflux in the presence of potential substrates and inhibitors.

    • Main Results:

    • The assay demonstrated energy-dependent GSMF extrusion by ABCC2-overexpressing cells.
    • Optimal incubation conditions and glutathione dependency were established.
    • Known MRP2 substrates and inhibitors significantly altered intracellular fluorescence and GSMF efflux, while inhibitors of other ABC transporters (ABCB1, ABCG2) had no effect.

    Conclusions:

    • The GSMF assay provides a robust and rapid microplate-based system for screening drug interactions with MRP2.
    • This assay is a valuable tool for drug profiling and understanding the role of MRP2 in drug disposition.