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• Review •

Scintillation Proximity Assays in High Throughput Screening

Peng Gang1,2, Liu Bailing1, Wang Bin1,2, Li Chenying1,2   

  1. 1. Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu 610041, China;
    2. Graduate University of Chinese Academy of Sciences, Beijing 100049, China
  • Received: Revised: Online: Published:
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Originated from a radioimmunoassay method, scintillation proximity assay (SPA) is a homogenous, sensitive, fast and simple scintillant carrier-based platform. This platform can be used to screen lead compounds for drug targets and investigate their biological processes. SPA becomes an important method in high throughput screening (HTS) due to no separation step, easy binding of drug targets and measuring their activities. Because of the diversification and commercialization of radio-labeled molecules and affinity tags, as well as the development of scintillation readers and liquid handling technologies, SPAs have been widely applied in receptor binding, high throughput drug screening, enzyme assay, radioimmunoassay, protein-protein interaction,cell-based assay and so on. This review presents the principle of SPA, discusses the key technologies(includes scintillation carrier, scintillation reader and radiolabel molecule) and analyzes the evaluation system, as well as outlines the assay development and provides some examples in details related to HTS, summarizes the shortcomings and gives some potential outlooks for the future study. Recently, SPA and fluorescence-based screenings have been the hot researches for the high throughput screening drug. The innovations on screening techniques will definitely promote our comprehensive understanding of cellular system biology and dramatically advance the discovery process of leading compounds. Contents 1 Principle of SPA
2 Key elements of SPA
2.1 Choice of scintillation materials
2.2 Choice of scintillation readers
2.3 Choice of radio-label molecules
3 Evaluation factors of SPA
4 Assay developments
5 Applications
5.1 Application of receptor-ligand interactions
5.2 Application of enzyme assays
5.3 Application of HTS drugs
5.4 Application of RIAs
5.5 Application of cell-based assays
6 Shortcomings and outlooks
7 Conclusions
Key words: scintillation proximity assay (SPA), high throughput screening, scintillation carrier, radioimmunoassay, receptor-ligand binding, cell-based screening

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