Cell-based high-throughput screening assay for identification of G-protein-coupled receptors agonists and antagonists

Abstract

The GPCRs are the target of a significant portion of all approved drugs and also represent an important parcel of potential drug targets for new indications. Activation of GPCRs can be detected by the utilization of functional cell-based assays like measuring transient intracellular calcium mobilization. The emergence of the fluorescent imaging plate reader and Ca2+-sensitive fluorescent dyes has made the high-content screening of GPCR possible. Here was applied a dual automated FLIPR platform to testing a large collection of compounds to identification of both agonist and antagonists form a single screen of GPCR