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起源于放射性免疫分析的临近闪烁分析法(scintillation proximity assay,SPA)是一种均相、灵敏、快速和简便的基于闪烁载体的分析平台。该平台可用于筛选药物靶点的先导化合物和研究其生理过程。由于无需分离,易于固定药物靶点和检测其活性,SPA成为一种重要的高通量筛选方法。由于放射性标记分子和亲和标签分子的多样化和商业化、以及液闪计数器和液相操作等技术的发展,SPA已经广泛用于受体结合、高通量药物筛选、酶分析、放射性免疫分析、蛋白质-蛋白质相互作用和细胞水平分析等方面。本文阐述了SPA原理,讨论了其关键技术(包括闪烁载体、液闪计数器和放射性标记分子),分析了其评价体系;同时简述了SPA分析的发展,并介绍了其在高通量筛选中的应用实例,归纳了存在的问题,给出了未来的发展趋势。目前,基于SPA和荧光分析方法已成为高通量药物筛选的热点研究领域,这些筛选技术的革新必然提升我们对细胞体系生物学的全面理解和促进先导化合物筛选过程的显著进步。
The scintillation proximity assay (SPA), which originated in radioimmunoassay, is a homogeneous, sensitive, fast, and simple scintillation vector based assay platform. The platform can be used to screen lead compounds for drug targets and to study their physiological processes. SPA is an important high-throughput screening method because it requires no separation, it is easy to fix drug targets and test its activity. SPA has been used extensively in receptor binding, high-throughput drug screening, enzyme assays, radioimmunoassays, radioimmunoassays, radioimmunoassays, immunoassays, radioimmunoassay, immunoassay, radioimmunoassay, radioimmunoassay etc. due to the diversification and commercialization of radiolabeled and affinity tagged molecules, Protein-protein interactions and cell-level analysis. This article describes the principle of SPA, discusses its key technologies (including scintillating vectors, liquid scintillation counters and radiolabeled molecules), analyzes its evaluation system, and briefly describes the development of SPA analysis, and introduces its high-throughput screening The application examples are summarized, the existing problems are summarized, and the future development trends are given. At present, the SPA-based and fluorescence analysis methods have become a hot research area for high-throughput drug screening. The innovation of these screening technologies will inevitably enhance our overall understanding of the biology of the cell system and significant progress in screening the lead compounds.