Karpenko Iuliia A, Margathe Jean-François, Rodriguez Thiéric, Pflimlin Elsa, Dupuis Elodie, Hibert Marcel, Durroux Thierry, Bonnet Dominique
Laboratoire d'Innovation Thérapeutique, UMR7200 CNRS/Université de Strasbourg, Labex MEDALIS, Faculté de Pharmacie , 74 route du Rhin, 67401 Illkirch, France.
J Med Chem. 2015 Mar 12;58(5):2547-52. doi: 10.1021/jm501395b. Epub 2015 Feb 12.
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.
本文描述了首个用于催产素受体（OTR）的高亲和力荧光配体的设计与合成。这些化合物推动了基于时间分辨荧光能量共振转移（TR-FRET）的OTR检测方法的发展，该方法易于进行高通量筛选。通过使用肽类和非肽类OTR配体作为竞争剂进行竞争实验，实现了对该检测方法的验证。这些探针是首个针对催产素G蛋白偶联受体的选择性荧光配体。
