Functional assay and high throughput screening for G-protein coupled receptors / 中国药理学通报

ABSTRACT

G-protein coupled receptor (GPCR) family is the large st group of therapeutic targets. High throughput screening (HTS) plays critical ro les in early stage of drug discovery. Based on signaling pathway stimulated by l igand binding on the GPCRs, many functional assay technologies have been develop ed for HTS. These technologies include Fluorometric microvolume assay technology (FMAT), Fluorescence polarization (FP), Competitive enzyme-linked immunosorben t assay (ELISA), Scintillation proximity assay (SPA), Melanophore assay, Reporte r gene assay and Calcium assay. The principles and applic- ations of these technologies were summarized in this review. We particularly emphasize those techniques of nonradioactive, su bstrate and cofactor free assays, which will be the major approaches for HTS, su ch as reporter gene and calcium assays.