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A Fluorescence-based Lymphocyte Assay Suitable for High-throughput Screening of Small Molecules
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Scintillation proximity assays in high-throughput screening.

J Fraser Glickman1, Andres Schmid, Sandrine Ferrand

  • 1Novartis Institutes for BioMedical Research, Basel, Switzerland. fraser.glickman@novartis.com

Assay and Drug Development Technologies
|July 3, 2008
PubMed
Summary

Scintillation proximity assays (SPAs) are versatile tools for high-throughput screening (HTS), enabling the measurement of diverse drug target activities and binding. This review details SPA applications in screening millions of compounds for drug discovery.

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Drug Discovery

Background:

  • Scintillation proximity assays (SPAs) are valuable for high-throughput screening (HTS).
  • They measure activity and binding for diverse drug targets.
  • SPAs utilize principles of ligand-receptor binding and enzyme kinetics.

Purpose of the Study:

  • To provide a comprehensive review of Scintillation Proximity Assays (SPAs).
  • To detail the applications of SPAs in high-throughput screening (HTS).
  • To highlight major uses and suggest future research directions.

Main Methods:

  • Miniaturized, high-throughput assays are developed using SPA principles.
  • Millions of compounds are screened using these assays.
  • Commercially available radiolabeled molecules and affinity tags enable SPA development.

Main Results:

  • SPAs facilitate the measurement of diverse drug target activities and binding.
  • Synthetic radiotracers minimize disturbance of natural binding interactions.
  • The technique allows for screening of millions of compounds.

Conclusions:

  • Scintillation proximity assays are powerful tools for drug discovery and HTS.
  • The versatility of SPAs is enhanced by available radiolabeled molecules and affinity tags.
  • Further research can expand the applications of SPAs in identifying novel therapeutics.