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dc.contributor.author | Gamo, Ana M | |
dc.contributor.author | González-Vera, Juan A | |
dc.contributor.author | Rueda-Zubiaurre, Ainoa | |
dc.contributor.author | Alonso, Dulce | |
dc.contributor.author | Vázquez-Villa, Henar | |
dc.contributor.author | Martín-Couce, Lidia | |
dc.contributor.author | Palomares, Óscar | |
dc.contributor.author | Lopez, Juan Antonio | |
dc.contributor.author | Martín-Fontecha, Mar | |
dc.contributor.author | Benhamú, Bellinda | |
dc.contributor.author | López-Rodríguez, María L | |
dc.contributor.author | Ortega-Gutiérrez, Silvia | |
dc.date.accessioned | 2018-11-20T10:52:36Z | |
dc.date.available | 2018-11-20T10:52:36Z | |
dc.date.issued | 2016-01-22 | |
dc.identifier.citation | Chemistry. 2016; 22(4):1313-21 | es_ES |
dc.identifier.issn | 0947-6539 | es_ES |
dc.identifier.uri | http://hdl.handle.net/20.500.12105/6638 | |
dc.description.abstract | Determination 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.sponsorship | This 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.language.iso | eng | es_ES |
dc.type.hasVersion | AM | es_ES |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/ | * |
dc.subject | GPCRS | es_ES |
dc.subject | chemical probes | es_ES |
dc.subject | drug discovery | es_ES |
dc.subject | selectivity profiling | es_ES |
dc.subject | serotonin receptors | es_ES |
dc.subject.mesh | Drug Design | es_ES |
dc.subject.mesh | Drug Discovery | es_ES |
dc.subject.mesh | Humans | es_ES |
dc.subject.mesh | Ligands | es_ES |
dc.subject.mesh | Receptor, Serotonin, 5-HT1A | es_ES |
dc.subject.mesh | Receptors, G-Protein-Coupled | es_ES |
dc.subject.mesh | Receptors, Serotonin | es_ES |
dc.title | Chemoproteomic Approach to Explore the Target Profile of GPCR ligands: Application to 5-HT1A and 5-HT6 Receptors | es_ES |
dc.type | journal article | es_ES |
dc.rights.license | Attribution-NonCommercial-NoDerivatives 4.0 Internacional | * |
dc.identifier.pubmedID | 26560738 | es_ES |
dc.format.volume | 22 | es_ES |
dc.format.number | 4 | es_ES |
dc.format.page | 1313-21 | es_ES |
dc.identifier.doi | 10.1002/chem.201503101 | es_ES |
dc.contributor.funder | Ministerio de Economía y Competitividad (España) | |
dc.contributor.funder | Comunidad de Madrid (España) | |
dc.contributor.funder | Complutense University of Madrid (España) | |
dc.contributor.funder | Unión Europea. Fondo Europeo de Desarrollo Regional (FEDER/ERDF) | |
dc.contributor.funder | Fundación ProCNIC | |
dc.description.peerreviewed | Sí | es_ES |
dc.identifier.e-issn | 1521-3765 | es_ES |
dc.relation.publisherversion | https://doi.org/10.1002/chem.201503101 | |
dc.identifier.journal | Chemistry - A European Journal | es_ES |
dc.repisalud.orgCNIC | CNIC::Unidades técnicas::Proteómica / Metabolómica | es_ES |
dc.repisalud.institucion | CNIC | es_ES |
dc.relation.projectID | info:eu-repo/grantAgreement/ES/SAF2013-48271 | es_ES |
dc.rights.accessRights | open access | es_ES |