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Chapitre D'ouvrage Année : 2019

Time-resolved FRET based assays to characterize hetero-oligomer pharmacology

Résumé

Although G protein-coupled receptor (GPCR) oligomerization is a matter of debate, it has been shown that the nature of the GPCR partners within the oligomers can influence the pharmacological properties of the receptors. Therefore, finding specific ligands for homo-or hetero-oligomers opens new perspectives for drug discovery. However, no efficient experimental strategy to screen for such ligands existed yet. Indeed, conventional binding strategies do not discriminate ligand binding on GPCR monomers, homo-or hetero-oligomers. To address this issue, we recently developed a new assay based on a time-resolved FRET method that is easy to implement and that can focus on ligand binding specifically on the hetero-oligomer.
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Dates et versions

hal-03563498 , version 1 (09-02-2022)

Identifiants

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Joyce Heuninck, Candide Hounsou, Elodie Dupuis, Eric Trinquet, Bernard Mouillac, et al.. Time-resolved FRET based assays to characterize hetero-oligomer pharmacology. Mario Tiberi. G Protein-Coupled Receptor Signaling: Methods and Protocols, 1947, Springer New York, pp.151-168, 2019, Methods in Molecular Biology, 978-1-4939-9120-4. ⟨10.1007/978-1-4939-9121-1_8⟩. ⟨hal-03563498⟩
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