Abstract
G protein-coupled receptors (GPCRs) are the largest family of cellular surface receptors and play a key role controlling a diverse array of developmental and physiological processes. Therefore, GPCRs constitute the targets of many modern therapeutics. Interestingly, GPCRs can interact (i.e., oligomerize) with other cell surface receptors and ion channels, thus leading to a fine-tuning modulation of physiological functions. In line with this, GPCR oligomerization has gained interest during the last years, since drugs targeting these molecular entities could open new GPCR-based pharmacotherapeutic avenues. Accordingly, different techniques assessing the occurrence of GPCR oligomerization in native tissue have emerged (i.e., immunoelectron microscopy, proximity ligation assay, etc.). From them, one of the most reliable approaches consists of using GPCR-fluorescent ligands engaging into a heteromerization-dependent time-resolved fluorescence resonance energy transfer (TR-FRET) process. Here, we review this methodology to reveal receptor-receptor interactions in brain tissue.
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Acknowledgments
This work was supported by Ministerio de Ciencia, Innovación y Universidades–Agencia Estatal de Investigación-FEDER-UE (SAF2017-87349-R MICIU/AEI/FEDER/UE) and Generalitat de Catalunya (2017SGR1604).We thank Centres de Recerca de Catalunya (CERCA) Programme/Generalitat de Catalunya for IDIBELL institutional support. We thank Esther Castaño and Benjamín Torrejón from the CCiT-Bellvitge Campus of the University of Barcelona. Also, this work was supported by research grants from the centre National de la Rcherche Scientifique, Institut National de la Santé et de la Recherche Médicale and by the Plateforme de Pharmacologie-Criblage of Montpellier and the Region Languedoc-Roussillon.
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Fernández-Dueñas, V., Durroux, T., Ciruela, F. (2021). Time-Resolved Fluorescence Resonance Energy Transfer Using Fluorescent Ligands to Study Native G Protein-Coupled Receptor Heteromerization in Brain. In: Lujan, R., Ciruela, F. (eds) Receptor and Ion Channel Detection in the Brain. Neuromethods, vol 169. Humana, New York, NY. https://doi.org/10.1007/978-1-0716-1522-5_8
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DOI: https://doi.org/10.1007/978-1-0716-1522-5_8
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