title: G Protein-Coupled Receptor Multimers: A Question Still Open Despite the Use of Novel Approaches.
abstract: Heteromerization of G protein-coupled receptors (GPCRs) can significantly change the functional properties of involved receptors. Various biochemical and biophysical methodologies have been developed in the last two decades to identify and functionally evaluate GPCR heteromers in heterologous cells, with recent approaches focusing on GPCR complex stoichiometry and stability. Yet validation of these observations in native tissues is still lagging behind for the majority of GPCR heteromers. Remarkably, recent studies, particularly some involving advanced fluorescence microscopy techniques, are contributing to our current knowledge of aspects that were not well known until now, such as GPCR complex stoichiometry and stability. In parallel, a growing effort is being applied to move the field forward into native systems. This short review will highlight recent developments to study the stoichiometry and stability of GPCR complexes and methodologies to detect native GPCR dimers.
authors.affiliation: Amsterdam Institute for Molecules, Medicines and Systems, Division of Medicinal Chemistry, Faculty of Sciences, VU University Amsterdam, Amsterdam, The Netherlands (H.F.V.); Molecular Pharmacology Laboratory, Biofarma Research Group (GI-1685), University of Santiago de Compostela, Center for Research in Molecular Medicine and Chronic Diseases, Santiago de Compostela, Spain (M.C.); and Centre National de la Recherche Scientifique, Institut de Génomique Fonctionnelle, Université de Montpellier, Montpellier, France (J.-P.P.) h.f.vischer@vu.nl.
authors.forename: Henry F
authors.initials: HF
authors.lastname: Vischer
authors.affiliation: Amsterdam Institute for Molecules, Medicines and Systems, Division of Medicinal Chemistry, Faculty of Sciences, VU University Amsterdam, Amsterdam, The Netherlands (H.F.V.); Molecular Pharmacology Laboratory, Biofarma Research Group (GI-1685), University of Santiago de Compostela, Center for Research in Molecular Medicine and Chronic Diseases, Santiago de Compostela, Spain (M.C.); and Centre National de la Recherche Scientifique, Institut de Génomique Fonctionnelle, Université de Montpellier, Montpellier, France (J.-P.P.).
authors.forename: Marián
authors.initials: M
authors.lastname: Castro
authors.affiliation: Amsterdam Institute for Molecules, Medicines and Systems, Division of Medicinal Chemistry, Faculty of Sciences, VU University Amsterdam, Amsterdam, The Netherlands (H.F.V.); Molecular Pharmacology Laboratory, Biofarma Research Group (GI-1685), University of Santiago de Compostela, Center for Research in Molecular Medicine and Chronic Diseases, Santiago de Compostela, Spain (M.C.); and Centre National de la Recherche Scientifique, Institut de Génomique Fonctionnelle, Université de Montpellier, Montpellier, France (J.-P.P.).
authors.forename: Jean-Philippe
authors.initials: JP
authors.lastname: Pin
mesh_terms: D000818:Animals; D006801:Humans; D055503:Protein Multimerization; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry* / Q000378:metabolism
chemical_list: D043562:Receptors, G-Protein-Coupled