Abstract
Serotonin receptors—with the exception of the 5-HT3 receptor—are members of the G protein-coupled receptor (GPCR) superfamily. These membrane proteins participate in a wide range of signal transduction pathways. Alterations of their activities often occur in pathological and psychopathological disorders. Therefore, these receptors determine major targets for drug discovery. Currently, the concept of GPCR oligomerization has become widely accepted. Functional heteromers have key significance for receptor expression, ligand binding, signaling, and desensitization. Formation of heteromers among serotonin receptors or between serotonin receptors and other GPCRs enables communication between different protomers within the protein complex and signaling diversification. Receptor heteromers may possess biochemical and pharmacological characteristics that are distinct from those of monomers. Therefore, the knowledge of receptor interaction with their partners has crucial relevance for novel, more selective drug design. The chapter demonstrates the methodology used for the detection of receptor heteromers in heterologous cellular expression systems as well as in native tissues. Evaluation of data focuses on strategies based on the Förster resonance energy transfer (FRET) phenomenon, especially HTRF and FLIM techniques, as well as on proximity ligation assay (PLA) approaches.
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Acknowledgements
Presented methods are used in projects financed from European Union within Regional Development Fund. Grants for innovation —PARENT/BRIDGE Programme—POMOST/2011-4/5, grant from the Ministry of Science N N401 009640 and JUVENTUS IP2011031571 project.
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Łukasiewicz, S., Błasiak, E., Szafran-Pilch, K., Dziedzicka-Wasylewska, M. (2015). Novel Approaches to Serotonin Receptor Interaction Studies. In: Blenau, W., Baumann, A. (eds) Serotonin Receptor Technologies. Neuromethods, vol 95. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4939-2187-4_1
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DOI: https://doi.org/10.1007/978-1-4939-2187-4_1
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