Selective Nonpeptidic Fluorescent Ligands for Oxytocin Receptor: Design, Synthesis, and Application to Time-Resolved FRET Binding Assay
| Autor: | Elsa Pflimlin, Thierry Durroux, Iuliia A. Karpenko, Thiéric Rodriguez, Jean-François Margathe, Elodie Dupuis, Marcel Hibert, Dominique Bonnet |
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| Rok vydání: | 2015 |
| Předmět: |
Models
Molecular High-throughput screening Peptide Ligands Oxytocin Drug Discovery High-Throughput Screening Assays Fluorescence Resonance Energy Transfer Humans Receptor Fluorescent Dyes chemistry.chemical_classification Molecular Structure Chemistry Ligand binding assay Combinatorial chemistry Fluorescence Oxytocin receptor Kinetics Förster resonance energy transfer Receptors Oxytocin Drug Design Biophysics Molecular Medicine Biological Assay Protein Binding |
| Zdroj: | Journal of Medicinal Chemistry. 58:2547-2552 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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