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Related Experiment Videos

Development of a versatile platform for nuclear receptor screening using AlphaScreen.

Nathalie Rouleau1, Sophie Turcotte, Marie-Hélène Mondou

  • 1PerkinElmer BioSignal, Montreal, Quebec, Canada. nathalie.rouleau@perkinelmer.com

Journal of Biomolecular Screening
|July 8, 2003
PubMed
Summary

A new AlphaScreen assay effectively identifies compounds that modulate nuclear receptor (NR) activity by detecting NR-coactivator interactions. This sensitive and versatile method aids in discovering potential therapeutic agents targeting transcription regulation.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Nuclear receptors (NRs) regulate gene transcription via interactions with coactivators.
  • These interactions depend on the LXXLL motif present in coactivators.
  • Modulating NR activity is crucial for therapeutic interventions.

Purpose of the Study:

  • To develop a sensitive assay for identifying and characterizing compounds that modulate NR activity.
  • To demonstrate the versatility of the AlphaScreen technology for NR research.
  • To enable efficient screening of NR modulators.

Main Methods:

  • Utilized AlphaScreen technology to detect NR-coactivator interactions.
  • Employed estrogen and retinoic acid receptors as model systems.

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  • Designed assays using various antibodies for receptor or domain capture.
  • Differentiated between agonists and antagonists based on coactivator recruitment.

    • Main Results:

    • The AlphaScreen assay demonstrated high sensitivity, requiring nanomolar concentrations of reagents.
    • The assay successfully differentiated between agonists and antagonists.
    • Competition isotherms ranked known antagonists by potency.
    • The assay proved versatile for targeting different interaction sites.

    Conclusions:

    • The AlphaScreen NR assay is a versatile, sensitive, and robust tool for drug discovery.
    • This assay facilitates efficient screening of compounds modulating NR activity.
    • The technology aids in characterizing NR modulators for therapeutic development.