Fiche publication
Date publication
mars 2015
Auteurs
Membres identifiés du Cancéropôle Est :
Pr HIBERT Marcel
Tous les auteurs :
Karpenko IA, Margathe JF, Rodriguez T, Pflimlin E, Dupuis E, Hibert M, Durroux T, Bonnet D
Lien Pubmed
Résumé
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.
Référence
J Med Chem. 2015 Mar 12;58(5):2547-52