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Related Experiment Videos

High-throughput receptor-binding methods for somatostatin receptor 2.

Elizabeth T Birzin1, Susan P Rohrer

  • 1Department of Atherosclerosis and Endocrinology, Merck Research Laboratories, Rahway, NJ 07065, USA. elizabeth_birzin@merck.com

Analytical Biochemistry
|July 26, 2002
PubMed
Summary

Three methods were developed to measure binding to human somatostatin receptor 2 (hSST2). All methods yielded similar results, with WGA-Flashplate assays being ideal for automated high-throughput screening.

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Assay Development

Background:

  • Human somatostatin receptor 2 (hSST2) is a key target in various physiological processes.
  • Quantifying ligand binding to hSST2 is crucial for drug discovery and development.
  • Existing screening methods may have limitations in throughput and automation.

Purpose of the Study:

  • To develop and validate three distinct high-throughput screening (HTS) methods for quantifying 125I-SS14 binding to hSST2.
  • To compare the performance and suitability of different assay formats for hSST2 ligand binding.
  • To assess the efficiency of these methods for determining drug efficacy (IC50 values).

Main Methods:

  • Development of microplate-based separation assays using Packard Unifilter and Millipore Multiscreen plates.

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  • Establishment of a homogeneous ligand-binding assay utilizing wheat germ agglutinin (WGA)-coated Flashplates.
  • Quantification of 125I-SS14 binding kinetics (apparent dissociation constants) and determination of IC50 values for 12 test compounds across all developed methods.

    • Main Results:

    • All three developed HTS methods successfully quantified 125I-SS14 binding to hSST2.
    • Consistent IC50 values were obtained for 12 tested compounds across all assay formats, indicating reliability.
    • The WGA-Flashplate assay demonstrated suitability for fully automated HTS, while Unifilter and Multiscreen plates are better for semi-automated and manual screening.

    Conclusions:

    • Validated HTS methods are available for assessing hSST2 binding.
    • The choice of method depends on the desired level of automation and screening capacity.
    • These assays provide robust tools for identifying novel modulators of hSST2 activity.