Cross-pharmacology analysis of G protein-coupled receptors

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• dc.contributor.author Briansó, Ferran
• dc.contributor.author Carrascosa Baena, María Carmen, 1972-
• dc.contributor.author Oprea, Tudor I.
• dc.contributor.author Mestres i López, Jordi
• dc.date.accessioned 2019-02-12T08:49:44Z
• dc.date.available 2019-02-12T08:49:44Z
• dc.date.issued 2011
• dc.description.abstract The degree of applicability of chemogenomic approaches to protein families depends on the accuracy and completeness of pharmacological data and the corresponding level of pharmacological similarity observed among their protein members. The recent public domain availability of pharmacological data for thousands of small molecules on 204 G protein- coupled receptors (GPCRs) provides a firm basis for an in-depth cross-pharmacology analysis of this superfamily. The number of protein targets included in the cross-pharmacology profile of the different GPCRs changes significantly upon varying the ligand similarity and binding affinity criteria. However, with the exception of muscarinic receptors, aminergic GPCRs distinguish themselves from the rest of the members in the family by their remarkably high levels of pharmacological similarity among them. Clusters of non-GPCR targets related by cross-pharmacology with particular GPCRs are identified and the implications for unwanted side-effects, as well as for repurposing opportunities, discussed.
• dc.description.sponsorship This research was funded by the Instituto de Salud Carlos III, the Spanish Ministerio de Ciencia e Innovación (project reference BIO2008-02329) and the NIH grant 5U54MH084690-02.
• dc.format.mimetype application/pdf
• dc.identifier.citation Briansó F, Carrascosa MC, Oprea TI, Mestres J. Cross-pharmacology analysis of G protein-coupled receptors. Curr Top Med Chem. 2011;11(15):1956-63. DOI 10.2174/156802611796391285
• dc.identifier.doi http://dx.doi.org/10.2174/156802611796391285
• dc.identifier.issn 1568-0266
• dc.identifier.uri http://hdl.handle.net/10230/36554
• dc.language.iso eng
• dc.publisher Bentham Science Publishers
• dc.relation.ispartof Curr Top Med Chem. 2011;11(15):1956-63
• dc.relation.projectID info:eu-repo/grantAgreement/ES/3PN/BIO2008-02329
• dc.rights © Bentham Science Publishers. Article published in Briansó F, Carrascosa MC, Oprea TI, Mestres J. Curr Top Med Chem. 11(15), 2011. The published manuscript is available at EurekaSelect via http://www.eurekaselect.com/openurl/content.php?genre=article&doi=10.2174/156802611796391285
• dc.rights.accessRights info:eu-repo/semantics/openAccess
• dc.subject.keyword GPCR network
• dc.subject.keyword Ligand similarity
• dc.subject.keyword Target profile
• dc.subject.keyword Adverse effects
• dc.subject.keyword Drug repositioning
• dc.subject.keyword Pharmacological similarity
• dc.subject.keyword Cross-pharmacology analysis
• dc.subject.keyword Muscarinic receptors
• dc.subject.keyword Clusters of non-GPCR targets
• dc.subject.keyword GPCR-directed chemical libraries
• dc.subject.keyword Crosspharmacology signals
• dc.subject.keyword Chemogenomic Databases
• dc.title Cross-pharmacology analysis of G protein-coupled receptors
• dc.type info:eu-repo/semantics/article
• dc.type.version info:eu-repo/semantics/acceptedVersion