An update on adenosine A2A receptors as drug target in Parkinson's disease

Adenosine receptors are G protein-coupled receptors (GPCRs) that mediate the physiological functions of adenosine. In the central nervous system adenosine A2A receptors (A2ARs) are highly enriched in striatopallidal neurons where they form functional oligomeric complexes with other GPCRs such us the...

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Autores: Vallano Ferraz, Antonio, Fernández Dueñas, Víctor, Pedrós, Consuelo, Arnau de Bolós, Josep M., Ciruela Alférez, Francisco
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2011
País:España
Institución:Universidad de Barcelona
Repositorio:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/62390
Acceso en línea:https://hdl.handle.net/2445/62390
Access Level:acceso abierto
Palabra clave:Malaltia de Parkinson
Adenosina
Proteïnes G
Parkinson's disease
Adenosine
G Proteins
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spelling An update on adenosine A2A receptors as drug target in Parkinson's diseaseVallano Ferraz, AntonioFernández Dueñas, VíctorPedrós, ConsueloArnau de Bolós, Josep M.Ciruela Alférez, FranciscoMalaltia de ParkinsonAdenosinaProteïnes GParkinson's diseaseAdenosineG ProteinsAdenosine receptors are G protein-coupled receptors (GPCRs) that mediate the physiological functions of adenosine. In the central nervous system adenosine A2A receptors (A2ARs) are highly enriched in striatopallidal neurons where they form functional oligomeric complexes with other GPCRs such us the dopamine D2 receptor (D2R). Furthermore, it is assumed that the formation of balanced A2AR/D2R receptor oligomers are essential for correct striatal function as the allosteric receptor-receptor interactions established within the oligomer are needed for properly sensing adenosine and dopamine. Interestingly, A2AR activation reduces the affinity of striatal D2R for dopamine and the blockade of A2AR with specific antagonists facilitates function of the D2R. Thus, it may be postulated that A2AR antagonists are pro-dopaminergic agents. Therefore, A2AR antagonists will potentially reduce the effects associated with dopamine depletion in Parkinson's disease (PD). Accordingly, this class of compounds have recently attracted considerable attention as potential therapeutic agents for PD pharmacotherapy as they have shown potential effectiveness in counteracting motor dysfunctions and also displayed neuroprotective and anti-inflammatory effects in animal models of PD. Overall, we provide here an update of the current state of the art of these A2AR-based approaches that are under clinical study as agents devoted to alleviate PD symptomsBentham Science Publishers2011info:eu-repo/semantics/articleinfo:eu-repo/semantics/acceptedVersionapplication/pdfhttps://hdl.handle.net/2445/62390Articles publicats en revistes (Patologia i Terapèutica Experimental)reponame:Dipòsit Digital de la UBinstname:Universidad de BarcelonaInglésVersió postprint del document publicat a: http://dx.doi.org/10.2174/187152711797247803CNS & Neurological Disorders-Drug Targets, 2011, vol. 10, num. 6, p. 659 -669http://dx.doi.org/10.2174/187152711797247803(c) Bentham Science Publishers, 2011info:eu-repo/semantics/openAccessoai:diposit.ub.edu:2445/623902026-05-27T06:46:51Z
dc.title.none.fl_str_mv An update on adenosine A2A receptors as drug target in Parkinson's disease
title An update on adenosine A2A receptors as drug target in Parkinson's disease
spellingShingle An update on adenosine A2A receptors as drug target in Parkinson's disease
Vallano Ferraz, Antonio
Malaltia de Parkinson
Adenosina
Proteïnes G
Parkinson's disease
Adenosine
G Proteins
title_short An update on adenosine A2A receptors as drug target in Parkinson's disease
title_full An update on adenosine A2A receptors as drug target in Parkinson's disease
title_fullStr An update on adenosine A2A receptors as drug target in Parkinson's disease
title_full_unstemmed An update on adenosine A2A receptors as drug target in Parkinson's disease
title_sort An update on adenosine A2A receptors as drug target in Parkinson's disease
dc.creator.none.fl_str_mv Vallano Ferraz, Antonio
Fernández Dueñas, Víctor
Pedrós, Consuelo
Arnau de Bolós, Josep M.
Ciruela Alférez, Francisco
author Vallano Ferraz, Antonio
author_facet Vallano Ferraz, Antonio
Fernández Dueñas, Víctor
Pedrós, Consuelo
Arnau de Bolós, Josep M.
Ciruela Alférez, Francisco
author_role author
author2 Fernández Dueñas, Víctor
Pedrós, Consuelo
Arnau de Bolós, Josep M.
Ciruela Alférez, Francisco
author2_role author
author
author
author
dc.subject.none.fl_str_mv Malaltia de Parkinson
Adenosina
Proteïnes G
Parkinson's disease
Adenosine
G Proteins
topic Malaltia de Parkinson
Adenosina
Proteïnes G
Parkinson's disease
Adenosine
G Proteins
description Adenosine receptors are G protein-coupled receptors (GPCRs) that mediate the physiological functions of adenosine. In the central nervous system adenosine A2A receptors (A2ARs) are highly enriched in striatopallidal neurons where they form functional oligomeric complexes with other GPCRs such us the dopamine D2 receptor (D2R). Furthermore, it is assumed that the formation of balanced A2AR/D2R receptor oligomers are essential for correct striatal function as the allosteric receptor-receptor interactions established within the oligomer are needed for properly sensing adenosine and dopamine. Interestingly, A2AR activation reduces the affinity of striatal D2R for dopamine and the blockade of A2AR with specific antagonists facilitates function of the D2R. Thus, it may be postulated that A2AR antagonists are pro-dopaminergic agents. Therefore, A2AR antagonists will potentially reduce the effects associated with dopamine depletion in Parkinson's disease (PD). Accordingly, this class of compounds have recently attracted considerable attention as potential therapeutic agents for PD pharmacotherapy as they have shown potential effectiveness in counteracting motor dysfunctions and also displayed neuroprotective and anti-inflammatory effects in animal models of PD. Overall, we provide here an update of the current state of the art of these A2AR-based approaches that are under clinical study as agents devoted to alleviate PD symptoms
publishDate 2011
dc.date.none.fl_str_mv 2011
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/acceptedVersion
format article
status_str acceptedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2445/62390
url https://hdl.handle.net/2445/62390
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Versió postprint del document publicat a: http://dx.doi.org/10.2174/187152711797247803
CNS & Neurological Disorders-Drug Targets, 2011, vol. 10, num. 6, p. 659 -669
http://dx.doi.org/10.2174/187152711797247803
dc.rights.none.fl_str_mv (c) Bentham Science Publishers, 2011
info:eu-repo/semantics/openAccess
rights_invalid_str_mv (c) Bentham Science Publishers, 2011
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Bentham Science Publishers
publisher.none.fl_str_mv Bentham Science Publishers
dc.source.none.fl_str_mv Articles publicats en revistes (Patologia i Terapèutica Experimental)
reponame:Dipòsit Digital de la UB
instname:Universidad de Barcelona
instname_str Universidad de Barcelona
reponame_str Dipòsit Digital de la UB
collection Dipòsit Digital de la UB
repository.name.fl_str_mv
repository.mail.fl_str_mv
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