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Chemoproteomic Approach to Explore the Target Profile of GPCR ligands: Application to 5-HT1A and 5-HT6 Receptors

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dc.contributor.authorGamo, Ana M
dc.contributor.authorGonzález-Vera, Juan A
dc.contributor.authorRueda-Zubiaurre, Ainoa
dc.contributor.authorAlonso, Dulce
dc.contributor.authorVázquez-Villa, Henar
dc.contributor.authorMartín-Couce, Lidia
dc.contributor.authorPalomares, Óscar
dc.contributor.authorLopez, Juan Antonio
dc.contributor.authorMartín-Fontecha, Mar
dc.contributor.authorBenhamú, Bellinda
dc.contributor.authorLópez-Rodríguez, María L
dc.contributor.authorOrtega-Gutiérrez, Silvia
dc.contributor.funderMinisterio de Economía y Competitividad (España)
dc.contributor.funderComunidad de Madrid (España)
dc.contributor.funderComplutense University of Madrid (España)
dc.contributor.funderUnión Europea. Fondo Europeo de Desarrollo Regional (FEDER/ERDF)
dc.contributor.funderFundación ProCNIC
dc.date.accessioned2018-11-20T10:52:36Z
dc.date.available2018-11-20T10:52:36Z
dc.date.issued2016-01-22
dc.description.abstractDetermination of the targets of a compound remains an essential aspect in drug discovery. A complete understanding of all binding interactions is critical to recognize in advance both therapeutic effects and undesired consequences. However, the complete polypharmacology of many drugs currently in clinical development is still unknown, especially in the case of G protein-coupled receptor (GPCR) ligands. In this work we have developed a chemoproteomic platform based on the use of chemical probes to explore the target profile of a compound in biological systems. As proof of concept, this methodology has been applied to selected ligands of the therapeutically relevant serotonin 5-HT1A and 5-HT6 receptors, and we have identified and validated some of their off-targets. This approach could be extended to other drugs of interest to study the targeted proteome in disease-relevant systems.es_ES
dc.description.peerreviewedSíes_ES
dc.description.sponsorshipThis work was supported by grants from the Spanish Ministerio de Economia y Competitividad (MINECO, SAF2013-48271), and Comunidad de Madrid (S2010/BMD-2353). The authors thank Comunidad de Madrid and Universidad Complutense for predoctoral fellowships to A.M.G. and A.R.-Z., respectively, and to MINECO for Juan de la Cierva fellowship to J.A.G.-V.O.P.is a Ramony Cajal Scholar funded by MINECO and the European Social Fund. The Centro Nacional de Investigaciones Cardiovasculares is supported by the MINECO and the Pro-CNIC Foundation.
dc.format.number4es_ES
dc.format.page1313-21es_ES
dc.format.volume22es_ES
dc.identifier.citationChemistry. 2016; 22(4):1313-21es_ES
dc.identifier.doi10.1002/chem.201503101es_ES
dc.identifier.e-issn1521-3765es_ES
dc.identifier.issn0947-6539es_ES
dc.identifier.journalChemistry - A European Journales_ES
dc.identifier.pubmedID26560738es_ES
dc.identifier.urihttp://hdl.handle.net/20.500.12105/6638
dc.language.isoenges_ES
dc.relation.projectIDinfo:eu-repo/grantAgreement/ES/SAF2013-48271es_ES
dc.relation.publisherversionhttps://doi.org/10.1002/chem.201503101
dc.repisalud.institucionCNICes_ES
dc.repisalud.orgCNICCNIC::Unidades técnicas::Proteómica / Metabolómicaes_ES
dc.rights.accessRightsopen accesses_ES
dc.rights.licenseAttribution-NonCommercial-NoDerivatives 4.0 Internacional*
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/*
dc.subjectGPCRSes_ES
dc.subjectchemical probeses_ES
dc.subjectdrug discoveryes_ES
dc.subjectselectivity profilinges_ES
dc.subjectserotonin receptorses_ES
dc.subject.meshDrug Designes_ES
dc.subject.meshDrug Discoveryes_ES
dc.subject.meshHumanses_ES
dc.subject.meshLigandses_ES
dc.subject.meshReceptor, Serotonin, 5-HT1Aes_ES
dc.subject.meshReceptors, G-Protein-Coupledes_ES
dc.subject.meshReceptors, Serotonines_ES
dc.titleChemoproteomic Approach to Explore the Target Profile of GPCR ligands: Application to 5-HT1A and 5-HT6 Receptorses_ES
dc.typejournal articlees_ES
dc.type.hasVersionAMes_ES
dspace.entity.typePublication
relation.isAuthorOfPublicationd79f2bf1-6f13-4b5f-9ae3-4c0ea06e9dcb
relation.isAuthorOfPublication.latestForDiscoveryd79f2bf1-6f13-4b5f-9ae3-4c0ea06e9dcb

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