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http://hdl.handle.net/10662/21482
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Campo DC | Valor | idioma |
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dc.contributor.author | Khiar Fernández, Nora | - |
dc.contributor.author | Zian, Debora | - |
dc.contributor.author | Vázquez Villa, Henar | - |
dc.contributor.author | Martínez Vázquez, Rafael Fernando | - |
dc.contributor.author | Escobar Peña, Andrea | - |
dc.contributor.author | Foronda Sainz, Román | - |
dc.contributor.author | Ray, Manisha | - |
dc.contributor.author | Puigdomenech Poch, Maria | - |
dc.contributor.author | Cincilla, Giovanni | - |
dc.contributor.author | Sánchez Martínez, Melchor | - |
dc.contributor.author | Kihara, Yasuyuki | - |
dc.contributor.author | Chun, Jerold | - |
dc.contributor.author | López Vales, Rubèn | - |
dc.contributor.author | López Rodríguez, María L. | - |
dc.contributor.author | Ortega Gutiérrez, Silvia | - |
dc.date.accessioned | 2024-06-10T12:19:47Z | - |
dc.date.available | 2024-06-10T12:19:47Z | - |
dc.date.issued | 2022 | - |
dc.identifier.uri | http://hdl.handle.net/10662/21482 | - |
dc.description.abstract | Spinal cord injuries (SCIs) irreversibly disrupt spinal connectivity, leading to permanent neurological disabilities. Current medical treatments for reducing the secondary damage that follows the initial injury are limited to surgical decompression and anti-inflammatory drugs, so there is a pressing need for new therapeutic strategies. Inhibition of the type 2 lysophosphatidic acid receptor (LPA2) has recently emerged as a new potential pharmacological approach to decrease SCI-associated damage. Toward validating this receptor as a target in SCI, we have developed a new series of LPA2 antagonists, among which compound 54 (UCM-14216) stands out as a potent and selective LPA2 receptor antagonist (Emax = 90%, IC50 = 1.9 μM, KD = 1.3 nM; inactive at LPA1,3–6 receptors). This compound shows efficacy in an in vivo mouse model of SCI in an LPA2-dependent manner, confirming the potential of LPA2 inhibition for providing a new alternative for treating SCI. | es_ES |
dc.description.sponsorship | This work has been supported by the Spanish Ministerio de Ciencia, Innovación y Universidades (PID2019-106279RB-I00 to M.L.L.-R. and S.O.-G., PID2020-120267RB-I00 to R.L.-V., predoctoral FPU grants to N.K.-F., D.Z., and A.E.-P., and Juan de la Cierva postdoctoral fellowship to R.F.M.), Comunidad de Madrid (PEJ Program) to R.F.-S., and grants from the National Institute of Health (NIH) R01NS103940 (Y.K.) and R01NS084398, R01MH051699 and Department of Defense DOD W81XWH-17-1-0455 (J.C.). R.L.-V. is the recipient of an ICREA Academia award. | es_ES |
dc.format.extent | 19 p. | es_ES |
dc.format.mimetype | application/pdf | en_US |
dc.language.iso | eng | es_ES |
dc.rights | Attribution 4.0 International | * |
dc.rights.uri | http://creativecommons.org/licenses/by/4.0/ | * |
dc.subject | Antagonists | es_ES |
dc.subject | Lipids | es_ES |
dc.subject | Receptors | es_ES |
dc.subject | Antagonistas | es_ES |
dc.subject | Lípidos | es_ES |
dc.subject | Receptores | es_ES |
dc.title | Novel Antagonist of the Type 2 Lysophosphatidic Acid Receptor (LPA2), UCM-14216, Ameliorates Spinal Cord Injury in Mice | es_ES |
dc.type | article | es_ES |
dc.description.version | peerReviewed | 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 |
europeana.dataProvider | Universidad de Extremadura. España | es_ES |
dc.identifier.bibliographicCitation | Nora Khiar-Fernández, Debora Zian, Henar Vázquez-Villa, R. Fernando Martínez, Andrea Escobar-Peña, Román Foronda-Sainz, Manisha Ray, Maria Puigdomenech-Poch, Giovanni Cincilla, Melchor Sánchez-Martínez, Yasuyuki Kihara, Jerold Chun, Rubèn López-Vales, María L. López-Rodríguez, and Silvia Ortega-Gutiérrez. Novel Antagonist of the Type 2 Lysophosphatidic Acid Receptor (LPA2), UCM-14216, Ameliorates Spinal Cord Injury in Mice. Journal of Medicinal Chemistry, 2022, 65(16), 10956-10974 DOI: 10.1021/acs.jmedchem.2c00046 | es_ES |
dc.type.version | publishedVersion | es_ES |
dc.contributor.affiliation | Universidad de Extremadura. Departamento de Química Orgánica e Inorgánica | es_ES |
dc.relation.publisherversion | https://pubs.acs.org/action/showCitFormats doi=10.1021%2Facs.jmedchem.2c00046&href=/doi/10.1021%2Facs.jmedchem.2c00046 | es_ES |
dc.identifier.doi | 10.1021/acs.jmedchem.2c00046 | - |
dc.identifier.publicationtitle | Journal of Medicinal Chemistry | es_ES |
dc.identifier.publicationissue | 16 | es_ES |
dc.identifier.publicationfirstpage | 10956 | es_ES |
dc.identifier.publicationlastpage | 10974 | es_ES |
dc.identifier.publicationvolume | 65 | es_ES |
dc.identifier.orcid | 0000-0002-3278-6074 | es_ES |
Colección: | DQOIN - Artículos |
Archivos
Archivo | Descripción | Tamaño | Formato | |
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LPA2-antagonists.pdf | Manuscript | 6,94 MB | Adobe PDF | Descargar |
acs_jmedchem_2c00046.pdf | 6,94 MB | Adobe PDF | Descargar |
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