title: Selective nonpeptidic fluorescent ligands for oxytocin receptor: design, synthesis, and application to time-resolved FRET binding assay.
abstract: The design and the synthesis of the first high-affinity fluorescent ligands for oxytocin receptor (OTR) are described. These compounds enabled the development of a TR-FRET based assay for OTR, readily amenable to high throughput screening. The validation of the assay was achieved by competition experiments with both peptide and nonpeptide OTR ligands as competitors. These probes represent the first selective fluorescent ligands for the oxytocin G protein-coupled receptor.
authors: Laboratoire d'Innovation Thérapeutique, UMR7200 CNRS/Université de Strasbourg, Labex MEDALIS, Faculté de Pharmacie , 74 route du Rhin, 67401 Illkirch, France.
authors: Iuliia A
authors: IA
authors: Karpenko
authors: Jean-François
authors: JF
authors: Margathe
authors: Thiéric
authors: T
authors: Rodriguez
authors: Elsa
authors: E
authors: Pflimlin
authors: Elodie
authors: E
authors: Dupuis
authors: Marcel
authors: M
authors: Hibert
authors: Thierry
authors: T
authors: Durroux
authors: Dominique
authors: D
authors: Bonnet
mesh_terms: D001681:Biological Assay; D015195:Drug Design; D031541:Fluorescence Resonance Energy Transfer / Q000379:methods*; D005456:Fluorescent Dyes / Q000138:chemical synthesis* / Q000494:pharmacology*; D057166:High-Throughput Screening Assays; D006801:Humans; D007700:Kinetics; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D010121:Oxytocin / Q000378:metabolism*; D011485:Protein Binding; D018045:Receptors, Oxytocin / Q000378:metabolism*
chemical_list: D005456:Fluorescent Dyes; D008024:Ligands; D018045:Receptors, Oxytocin; D010121:Oxytocin