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

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