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http://hdl.handle.net/10662/21888
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Campo DC | Valor | idioma |
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dc.contributor.author | González Gil, Inés | - |
dc.contributor.author | Zian, Debora | - |
dc.contributor.author | Vázquez Villa, Henar | - |
dc.contributor.author | Hernández Torres, Gloria | - |
dc.contributor.author | Martínez Vázquez, Rafael Fernando | - |
dc.contributor.author | Khiar Fernández, Nora | - |
dc.contributor.author | Rivera, Richard | - |
dc.contributor.author | Kihara, Yasuyuki | - |
dc.contributor.author | Devesa, Isabel | - |
dc.contributor.author | Mathivanan, Sakthikumar | - |
dc.contributor.author | Valle, Cristina Rosell del | - |
dc.contributor.author | Zambrana Infantes, Emma | - |
dc.contributor.author | Puigdomenech, María | - |
dc.contributor.author | Cincilla, Giovanni | - |
dc.contributor.author | Sánchez Martínez, Melchor | - |
dc.contributor.author | Rodríguez de Fonseca, Fernando | - |
dc.contributor.author | Ferrer Montiel, Antonio V. | - |
dc.contributor.author | Chun, Jerold | - |
dc.contributor.author | López Vales, Rubén | - |
dc.contributor.author | López Rodríguez, María L. | - |
dc.contributor.author | Ortega Gutiérrez, Silvia | - |
dc.date.accessioned | 2024-07-12T08:51:27Z | - |
dc.date.available | 2024-07-12T08:51:27Z | - |
dc.date.issued | 2020 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | http://hdl.handle.net/10662/21888 | - |
dc.description | Publicado en : Journal of Medicinal Chemistry 2020 63 (5), 2372-2390 DOI: 10.1021/acs.jmedchem.9b01287 | - |
dc.description.abstract | Neuropathic pain (NP) is a complex chronic pain state with a prevalence of almost 10% in the general population. Pharmacological options for NP are limited and slightly effective, so there is a need of developing more efficacious NP attenuating drugs. Activation of the type 1 lysophosphatidic acid (LPA1) receptor is a crucial factor in the initiation of NP. Hence, it is conceivable that a functional antagonism strategy could lead to NP mitigation. Here we describe a new series of LPA1 agonists among which derivative (S)-17 (UCM-05194) stands out as the most potent and selective LPA1 receptor agonist described so far (Emax=118%, EC50=0.24 μM, KD=19.6 nM; inactive at autotaxin and LPA2–6 receptors). This compound induces characteristic LPA1-mediated cellular effects and prompts the internalization of the receptor leading to its functional inactivation in primary sensory neurons and to an efficacious attenuation of the pain perception in an in vivo model of NP. | es_ES |
dc.format.extent | 51 p. | es_ES |
dc.format.mimetype | application/pdf | en_US |
dc.language.iso | eng | es_ES |
dc.publisher | ACS Publications | es_ES |
dc.relation.replaces | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7344333 | es_ES |
dc.rights | Attribution-NonCommercial-NoDerivatives 4.0 International | * |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/ | * |
dc.subject | Agonists | es_ES |
dc.subject | Lipids | es_ES |
dc.subject | Receptors | es_ES |
dc.subject | Agonistas | es_ES |
dc.subject | Lípidos | es_ES |
dc.subject | Receptores | es_ES |
dc.title | A novel agonist of the type 1 lysophosphatidic acid receptor (LPA1), UCM-05194, shows efficacy in neuropathic pain amelioration | es_ES |
dc.type | article | es_ES |
dc.description.version | notPeerReviewed | es_ES |
europeana.type | TEXT | en_US |
dc.rights.accessRights | openAccess | es_ES |
dc.subject.unesco | 2306 Química Orgánica | es_ES |
dc.subject.unesco | 2302.18 Lípidos | es_ES |
dc.subject.unesco | 3207.11 Neuropatología | es_ES |
europeana.dataProvider | Universidad de Extremadura. España | es_ES |
dc.identifier.bibliographicCitation | Inés González-Gil, Debora Zian, Henar Vázquez-Villa, Gloria Hernández-Torres, R. Fernando Martínez, Nora Khiar-Fernández, Richard Rivera, Yasuyuki Kihara, Isabel Devesa, Sakthikumar Mathivanan, Cristina Rosell del Valle, Emma Zambrana-Infantes, María Puigdomenech, Giovanni Cincilla, Melchor Sanchez-Martinez, Fernando Rodríguez de Fonseca, Antonio V. Ferrer-Montiel, Jerold Chun, Rubén López-Vales, María L. López-Rodríguez, and Silvia Ortega-Gutiérrez.. (2019). A novel agonist of the type 1 lysophosphatidic acid receptor (LPA1), UCM-05194, shows efficacy in neuropathic pain amelioration. J. Med. Chem. 51 p. | es_ES |
dc.type.version | draft | es_ES |
dc.contributor.affiliation | Universidad de Extremadura. Departamento de Química Orgánica e Inorgánica | es_ES |
dc.relation.publisherversion | https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b01287 | es_ES |
dc.identifier.publicationtitle | Journal of Medicinal Chemistry | es_ES |
dc.identifier.orcid | 0000-0002-3278-6074 | es_ES |
Colección: | DQOIN - Artículos |
Archivos
Archivo | Descripción | Tamaño | Formato | |
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acs_jmedchem_9b01287_draft.pdf | 2,53 MB | Adobe PDF | Descargar |
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