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Related Experiment Videos

High-throughput screening for ion channel modulators.

Margaret Falconer1, Fiona Smith, Sandha Surah-Narwal

  • 1Lead Discovery Technologies, Pfizer Global Research and Development, Sandwich, United Kingdom.

Journal of Biomolecular Screening
|November 6, 2003
PubMed
Summary
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Automated fluorescence assays using voltage-sensitive probes enable high-throughput screening of ion channel modulators. This technology accelerates the discovery of drugs targeting ion channels for major clinical indications.

Area of Science:

  • Pharmacology
  • Biophysics
  • Assay Development

Background:

  • Ion channels are crucial drug targets for major diseases.
  • Current screening methods lack the speed and biological relevance needed for drug discovery.
  • High-throughput screening (HTS) is essential for identifying novel ion channel modulators.

Purpose of the Study:

  • To develop and validate a fully automated system for high-throughput screening of ion channel function.
  • To enable rapid and biologically significant functional assays for ion channel drug discovery.
  • To facilitate the pharmacological characterization of ion channel modulators.

Main Methods:

  • Implementation of a Beckman/Sagian core system for automated functional fluorescence-based assays.
  • Utilizing voltage-sensitive fluorescent probes and fluorescence resonance energy transfer (FRET).

Related Experiment Videos

  • Monitoring ion channel activity with Aurora's Voltage/Ion Probe Reader (VIPR).

    • Main Results:

    • Successful establishment of a fully automated platform for ion channel screening.
    • Demonstrated robustness of fluorescence-based assays for measuring ion channel activity.
    • The system effectively screens for both inhibitors and activators of various ion channels.

    Conclusions:

    • Automated fluorescence assays provide a powerful tool for high-throughput screening of ion channel modulators.
    • This approach significantly enhances the efficiency and biological relevance of ion channel drug discovery.
    • The developed system is adaptable for studying diverse ion channels and identifying potential therapeutics.