Basic concepts in G-protein-coupled receptor homo- and heterodimerization

Until recently, heptahelical G-protein-coupled receptors (GPCRs) were considered to be expressed as monomers on the cell surface of neuronal and non-neuronal cells. It is now becoming evident that this view must be overtly changed since these receptors can form homodimers, heterodimers, and higher-o...

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Autores: Franco Fernández, Rafael, Casadó, Vicent, Cortés Tejedor, Antonio, Ferrada, Carla, Mallol Montero, Josefa, Woods, Amina S., Lluís i Biset, Carme, Canela Campos, Enric I. (Enric Isidre), 1949-, Ferré, Sergi
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2007
País:España
Institución:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repositorio:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:recercat.cat:2445/122385
Acceso en línea:https://hdl.handle.net/2445/122385
Access Level:acceso abierto
Palabra clave:Receptors cel·lulars
Proteïnes G
Cell receptors
G Proteins
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spelling Basic concepts in G-protein-coupled receptor homo- and heterodimerizationFranco Fernández, RafaelCasadó, VicentCortés Tejedor, AntonioFerrada, CarlaMallol Montero, JosefaWoods, Amina S.Lluís i Biset, CarmeCanela Campos, Enric I. (Enric Isidre), 1949-Ferré, SergiReceptors cel·lularsProteïnes GCell receptorsG ProteinsUntil recently, heptahelical G-protein-coupled receptors (GPCRs) were considered to be expressed as monomers on the cell surface of neuronal and non-neuronal cells. It is now becoming evident that this view must be overtly changed since these receptors can form homodimers, heterodimers, and higher-order oligomers on the plasma membrane. Here we discuss some of the basics and some new concepts of receptor homo- and heteromerization. Dimers-oligomers modify pharmacology, trafficking, and signaling of receptors. First of all, GPCR dimers must be considered as the main molecules that are targeted by neurotransmitters or by drugs. Thus, binding data must be fitted to dimer-based models. In these models, it is considered that the conformational changes transmitted within the dimer molecule lead to cooperativity. Cooperativity must be taken into account in the binding of agonists-antagonists-drugs and also in the binding of the so-called allosteric modulators. Cooperativity results from the intramolecular cross-talk in the homodimer. As an intramolecular cross-talk in the heterodimer, the binding of one neurotransmitter to one receptor often affects the binding of the second neurotransmitter to the partner receptor. Coactivation of the two receptors in a heterodimer can change completely the signaling pathway triggered by the neurotransmitter as well as the trafficking of the receptors. Heterodimer-specific drugs or dual drugs able to activate the two receptors in the heterodimer simultaneously emerge as novel and promising drugs for a variety of central nervous system (CNS) therapeutic applications.Hindawi2018201820072018info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersion11 p.application/pdfapplication/pdfhttps://hdl.handle.net/2445/122385Articles publicats en revistes (Bioquímica i Biomedicina Molecular)reponame:Recercat. Dipósit de la Recerca de Catalunyainstname:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)InglésReproducció del document publicat a: https://doi.org/10.1100/tsw.2007.197Scientific World Journal, 2007, vol. 7, p. 48-57https://doi.org/10.1100/tsw.2007.197cc-by (c) Franco Fernández, Rafael et al., 2007http://creativecommons.org/licenses/by/3.0/esinfo:eu-repo/semantics/openAccessoai:recercat.cat:2445/1223852026-05-29T05:05:01Z
dc.title.none.fl_str_mv Basic concepts in G-protein-coupled receptor homo- and heterodimerization
title Basic concepts in G-protein-coupled receptor homo- and heterodimerization
spellingShingle Basic concepts in G-protein-coupled receptor homo- and heterodimerization
Franco Fernández, Rafael
Receptors cel·lulars
Proteïnes G
Cell receptors
G Proteins
title_short Basic concepts in G-protein-coupled receptor homo- and heterodimerization
title_full Basic concepts in G-protein-coupled receptor homo- and heterodimerization
title_fullStr Basic concepts in G-protein-coupled receptor homo- and heterodimerization
title_full_unstemmed Basic concepts in G-protein-coupled receptor homo- and heterodimerization
title_sort Basic concepts in G-protein-coupled receptor homo- and heterodimerization
dc.creator.none.fl_str_mv Franco Fernández, Rafael
Casadó, Vicent
Cortés Tejedor, Antonio
Ferrada, Carla
Mallol Montero, Josefa
Woods, Amina S.
Lluís i Biset, Carme
Canela Campos, Enric I. (Enric Isidre), 1949-
Ferré, Sergi
author Franco Fernández, Rafael
author_facet Franco Fernández, Rafael
Casadó, Vicent
Cortés Tejedor, Antonio
Ferrada, Carla
Mallol Montero, Josefa
Woods, Amina S.
Lluís i Biset, Carme
Canela Campos, Enric I. (Enric Isidre), 1949-
Ferré, Sergi
author_role author
author2 Casadó, Vicent
Cortés Tejedor, Antonio
Ferrada, Carla
Mallol Montero, Josefa
Woods, Amina S.
Lluís i Biset, Carme
Canela Campos, Enric I. (Enric Isidre), 1949-
Ferré, Sergi
author2_role author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Receptors cel·lulars
Proteïnes G
Cell receptors
G Proteins
topic Receptors cel·lulars
Proteïnes G
Cell receptors
G Proteins
description Until recently, heptahelical G-protein-coupled receptors (GPCRs) were considered to be expressed as monomers on the cell surface of neuronal and non-neuronal cells. It is now becoming evident that this view must be overtly changed since these receptors can form homodimers, heterodimers, and higher-order oligomers on the plasma membrane. Here we discuss some of the basics and some new concepts of receptor homo- and heteromerization. Dimers-oligomers modify pharmacology, trafficking, and signaling of receptors. First of all, GPCR dimers must be considered as the main molecules that are targeted by neurotransmitters or by drugs. Thus, binding data must be fitted to dimer-based models. In these models, it is considered that the conformational changes transmitted within the dimer molecule lead to cooperativity. Cooperativity must be taken into account in the binding of agonists-antagonists-drugs and also in the binding of the so-called allosteric modulators. Cooperativity results from the intramolecular cross-talk in the homodimer. As an intramolecular cross-talk in the heterodimer, the binding of one neurotransmitter to one receptor often affects the binding of the second neurotransmitter to the partner receptor. Coactivation of the two receptors in a heterodimer can change completely the signaling pathway triggered by the neurotransmitter as well as the trafficking of the receptors. Heterodimer-specific drugs or dual drugs able to activate the two receptors in the heterodimer simultaneously emerge as novel and promising drugs for a variety of central nervous system (CNS) therapeutic applications.
publishDate 2007
dc.date.none.fl_str_mv 2007
2018
2018
2018
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2445/122385
url https://hdl.handle.net/2445/122385
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Reproducció del document publicat a: https://doi.org/10.1100/tsw.2007.197
Scientific World Journal, 2007, vol. 7, p. 48-57
https://doi.org/10.1100/tsw.2007.197
dc.rights.none.fl_str_mv cc-by (c) Franco Fernández, Rafael et al., 2007
http://creativecommons.org/licenses/by/3.0/es
info:eu-repo/semantics/openAccess
rights_invalid_str_mv cc-by (c) Franco Fernández, Rafael et al., 2007
http://creativecommons.org/licenses/by/3.0/es
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv 11 p.
application/pdf
application/pdf
dc.publisher.none.fl_str_mv Hindawi
publisher.none.fl_str_mv Hindawi
dc.source.none.fl_str_mv Articles publicats en revistes (Bioquímica i Biomedicina Molecular)
reponame:Recercat. Dipósit de la Recerca de Catalunya
instname:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
instname_str Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
reponame_str Recercat. Dipósit de la Recerca de Catalunya
collection Recercat. Dipósit de la Recerca de Catalunya
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,812429

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