title: Time-resolved Förster resonance energy transfer-based technologies to investigate G protein-coupled receptor machinery: high-throughput screening assays and future development.
abstract: High-throughput screening requires easy-to-monitor, rapid, robust, reliable, and miniaturized methods to test thousands of compounds on a target in a short period, in order to find active drugs. Only a few methods have been proved to fulfill all these requirements. New screening approaches based on fluorescence and especially on the principle of resonance energy transfer are being developed to study one of the main targets in the pharmaceutical industry, namely, the G protein-coupled receptors (GPCRs). Two types of approaches are clearly defined: generic approaches that are immediately applicable to a lot of targets such as second messenger kits or kinase kits; target-specific approaches that sense the receptor itself such as fluorescent ligands or fluorescent partners. This chapter focuses on sensors and approaches using the time-resolved Förster resonance energy transfer and homogeneous time-resolved fluorescence principle, their use, and their prospective applications for screening drugs acting on GPCRs.
authors.affiliation: CNRS, UMR-5203, Institut de Génomique Fonctionelle, Montpellier, F-34094, France.
authors.forename: Pauline
authors.initials: P
authors.lastname: Scholler
authors.forename: Jurriaan M
authors.initials: JM
authors.lastname: Zwier
authors.forename: Eric
authors.initials: E
authors.lastname: Trinquet
authors.forename: Philippe
authors.initials: P
authors.lastname: Rondard
authors.forename: Jean-Philippe
authors.initials: JP
authors.lastname: Pin
authors.forename: Laurent
authors.initials: L
authors.lastname: Prézeau
authors.forename: Julie
authors.initials: J
authors.lastname: Kniazeff
mesh_terms: D000818:Animals; D000906:Antibodies / Q000737:chemistry; D001667:Binding, Competitive; D015374:Biosensing Techniques; D002462:Cell Membrane / Q000378:metabolism; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D031541:Fluorescence Resonance Energy Transfer / Q000379:methods*; D005456:Fluorescent Dyes / Q000737:chemistry; D057809:HEK293 Cells; D057166:High-Throughput Screening Assays / Q000379:methods; D006801:Humans; D008024:Ligands; D011485:Protein Binding; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry*; D015398:Signal Transduction
chemical_list: D000906:Antibodies; D005456:Fluorescent Dyes; D008024:Ligands; D043562:Receptors, G-Protein-Coupled