Por favor, use este identificador para citar o enlazar a este item:
http://hdl.handle.net/10261/97131
COMPARTIR / EXPORTAR:
SHARE CORE BASE | |
Visualizar otros formatos: MARC | Dublin Core | RDF | ORE | MODS | METS | DIDL | DATACITE | |
Campo DC | Valor | Lengua/Idioma |
---|---|---|
dc.contributor.author | García de la Torre, Beatriz | - |
dc.contributor.author | Hornillos, Valentín | - |
dc.contributor.author | Luque-Ortega, Juan Román | - |
dc.contributor.author | Abengozar, M. A. | - |
dc.contributor.author | Amat-Guerri, Francisco | - |
dc.contributor.author | Ulises Acuña, A. | - |
dc.contributor.author | Rivas, Luis | - |
dc.contributor.author | Andreu, David | - |
dc.date.accessioned | 2014-05-23T08:03:27Z | - |
dc.date.available | 2014-05-23T08:03:27Z | - |
dc.date.issued | 2014-04 | - |
dc.identifier | doi: 10.1007/s00726-013-1661-3 | - |
dc.identifier | issn: 0939-4451 | - |
dc.identifier | issn: 1438-2199 | - |
dc.identifier.citation | Amino Acids 46(4): 1047-1058 (2014) | - |
dc.identifier.uri | http://hdl.handle.net/10261/97131 | - |
dc.description.abstract | Therapeutic application of many drugs is often hampered by poor or denied access to intracellular targets. A case in point is miltefosine (MT), an orally active antiparasitic drug, which becomes ineffective when parasites develop dysfunctional uptake systems. We report here the synthesis of a fluorescent BODIPY-embedding MT analogue with appropriate thiol functionalization allowing linkage to the cell-penetrating Tat(48-60) peptide through disulfide or thioether linkages. The resulting constructs are efficiently internalized into the otherwise MT-invulnerable R40 Leishmania strain, resulting in fast parasite killing, and hence successful avoidance of the resistance. In the disulfide-linked conjugate, an additional fluoro tag on the Tat moiety allows to monitor its reductive cleavage within the cytoplasm. Terminally differentiated cells such as peritoneal macrophages, impervious to MT unless infected by Leishmania, can uptake the drug in its Tat-conjugated form. The results afford proof-of-principle for using CPP vectors to avert drug resistance in parasites, and/or for tackling leishmaniasis by modulating macrophage uptake. © 2014 Springer-Verlag Wien. | - |
dc.publisher | Springer Nature | - |
dc.rights | openAccess | - |
dc.subject | BODIPY | - |
dc.subject | Cell-penetrating peptides | - |
dc.subject | Miltefosine | - |
dc.subject | Dual fluorescent labeling | - |
dc.subject | Reversion of resistance | - |
dc.subject | Monitoring of intracellular drug delivery | - |
dc.title | A BODIPY-embedding miltefosine analog linked to cell-penetrating Tat(48-60) peptide favors intracellular delivery and visualization of the antiparasitic drug | - |
dc.type | artículo | - |
dc.identifier.doi | 10.1007/s00726-013-1661-3 | - |
dc.relation.publisherversion | http://dx.doi.org/10.1007/s00726-013-1661-3 | - |
dc.embargo.terms | 2015-04-01 | - |
dc.date.updated | 2014-05-23T08:03:27Z | - |
dc.description.version | Peer Reviewed | - |
dc.language.rfc3066 | eng | - |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.cerifentitytype | Publications | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.grantfulltext | open | - |
item.openairetype | artículo | - |
item.fulltext | With Fulltext | - |
Aparece en las colecciones: | (IQOG) Artículos (CIB) Artículos (IQF) Artículos |
Ficheros en este ítem:
Fichero | Descripción | Tamaño | Formato | |
---|---|---|---|---|
Bodipy_Torre.pdf | 807,54 kB | Adobe PDF | Visualizar/Abrir |
CORE Recommender
SCOPUSTM
Citations
21
checked on 20-abr-2024
WEB OF SCIENCETM
Citations
18
checked on 26-feb-2024
Page view(s)
433
checked on 05-may-2024
Download(s)
462
checked on 05-may-2024
Google ScholarTM
Check
Altmetric
Altmetric
NOTA: Los ítems de Digital.CSIC están protegidos por copyright, con todos los derechos reservados, a menos que se indique lo contrario.