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http://hdl.handle.net/10261/143527
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Campo DC | Valor | Lengua/Idioma |
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dc.contributor.author | Estrada, Martín | - |
dc.contributor.author | Pérez, Concepción | - |
dc.contributor.author | Soriano, Elena | - |
dc.contributor.author | Pricl, Sabrina | - |
dc.contributor.author | Morales-García, José A. | - |
dc.contributor.author | Pérez Castillo, Ana | - |
dc.contributor.author | Rodríguez-Franco, María Isabel | - |
dc.date.accessioned | 2017-02-07T09:29:50Z | - |
dc.date.available | 2017-02-07T09:29:50Z | - |
dc.date.issued | 2016-07 | - |
dc.identifier | issn: 1756-8919 | - |
dc.identifier | e-issn: 1756-8927 | - |
dc.identifier.citation | Future Medicinal Chemistry 8(11): 1191-1207 (2016) | - |
dc.identifier.uri | http://hdl.handle.net/10261/143527 | - |
dc.description | et al. | - |
dc.description.abstract | [Background]: Neurogenic agents emerge as innovative drugs for the treatment of Alzheimer's disease (AD), whose pathological complexity suggests strengthening research in the multi-target directed ligands strategy. [Results]: By combining the lipoic acid structure with N-benzylpiperidine or N,N-dibenzyl(N-methyl)amine fragments, new multi-target directed ligands were obtained that act at three relevant targets in AD: σ-1 receptor (σR), β-secretase-1 (BACE1) and acetylcholinesterase (AChE). Moreover, they show potent neurogenic properties, good antioxidant capacity and favorable CNS permeability. Molecular modeling studies on AChE, σR and BACE1 highlight relevant drug-protein interactions that may contribute to the development of new disease-modifying drugs. [Conclusion]: New lipoic-based σ agonists endowed with neurogenic, antioxidant, cholinergic and amyloid β-peptide-reducing properties have been discovered for the potential treatment of AD. | - |
dc.description.sponsorship | Financial support from the Spanish Ministry of Economy and Competitiveness (MINECO, grants SAF2012-31035 and SAF2015-64948 to MIRF; grants SAF2010-16365 and SAF2014-52940-R to APC), Fundación de Investigación Médica Mutua Madrileña Automovilística (grant AP103952012 to MIRF), and Consejo Superior de Investigaciones Científicas (CSIC, grant PIE-201580E109 to MIRF) is gratefully acknowledged. ME thanks COLCIENCIAS (Colombia) for a Ph.D. fellowship. ES, and EL and SP thank CESGA (Santiago de Compostela, Spain) and CINECA (Bologna, Italy – Project SIMBIOSY) supercomputer centres, respectively, for providing access to computational resources. | - |
dc.publisher | Future Science | - |
dc.relation | info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/SAF2015-64948-C2-1-R | - |
dc.relation | info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/SAF2014-52940-R | - |
dc.relation.isversionof | Preprint | - |
dc.rights | openAccess | en_EN |
dc.subject | Lipoic acid | - |
dc.subject | Acetylcholinesterase (AChE) | - |
dc.subject | Beta-secretase-1 (BACE1) | - |
dc.subject | sigma-1 receptor (σ1R) | - |
dc.subject | Neurogenic properties | - |
dc.subject | N,N-dibenzyl(N-methyl)amine | - |
dc.subject | N-benzylpiperidine | - |
dc.subject | Multi-target directed ligands (MTDLs) | - |
dc.subject | Alzheimer’s disease | - |
dc.title | New neurogenic lipoic-based hybrids as innovative Alzheimer's drugs with σ-1 agonism and β-secretase inhibition | - |
dc.type | artículo | - |
dc.identifier.doi | 10.4155/fmc-2016-0036 | - |
dc.relation.publisherversion | https://doi.org/10.4155/fmc-2016-0036 | - |
dc.date.updated | 2017-02-07T09:29:51Z | - |
dc.description.version | Peer Reviewed | - |
dc.language.rfc3066 | eng | - |
dc.contributor.funder | Consejo Superior de Investigaciones Científicas (España) | - |
dc.contributor.funder | Fundación Mutua Madrileña | - |
dc.contributor.funder | Ministerio de Economía y Competitividad (España) | - |
dc.contributor.funder | Colciencias (Colombia) | - |
dc.relation.csic | Sí | - |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003339 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/100008061 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003329 | es_ES |
dc.identifier.pmid | 27402296 | - |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.openairetype | artículo | - |
item.grantfulltext | open | - |
item.cerifentitytype | Publications | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.fulltext | With Fulltext | - |
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