Por favor, use este identificador para citar o enlazar a este item:
http://hdl.handle.net/10261/47805
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 | González-Bulnes, Patricia | - |
dc.contributor.author | Bobenchik, April M. | - |
dc.contributor.author | Augagneur, Yoann | - |
dc.contributor.author | Cerdan, Rachel | - |
dc.contributor.author | Vial, Henri J. | - |
dc.contributor.author | Llebaria, Amadeu | - |
dc.contributor.author | Ben Mamoun, Choukri | - |
dc.date.accessioned | 2012-04-02T10:51:56Z | - |
dc.date.available | 2012-04-02T10:51:56Z | - |
dc.date.issued | 2011 | - |
dc.identifier.citation | Journal of Biological Chemistry | es_ES |
dc.identifier.issn | 0021-9258 | - |
dc.identifier.uri | http://hdl.handle.net/10261/47805 | - |
dc.description.abstract | In the human malaria parasite Plasmodium falciparum, the synthesis of the major and essential membrane phospholipid, phosphatidylcholine, occurs via the CDP-choline and the serine decarboxylase phosphoethanolamine methylation (SDPM) pathways, which are fueled by host choline, serine, and fatty acids. Both pathways share the final two steps catalyzed by two essential enzymes, P. falciparum CTP:phosphocholine cytidylyltransferase (PfCCT) and choline-phosphate transferase (PfCEPT). We identified a novel class of phospholipid mimetics, which inhibit the growth of P. falciparum as well as Leishmania and Trypanosoma species. Metabolic analyses showed that one of these compounds, PG12, specifically blocks phosphatidylcholine biosynthesis from both the CDP-choline and SDPM pathways via inhibition of PfCCT. In vitro studies using recombinant PfCCT showed a dose-dependent inhibition of the enzyme by PG12. The potent antimalarial of this compound, its low cytotoxicity profile, and its established mode of action make it an excellent lead to advance for further drug development and efficacy in vivo. | es_ES |
dc.description.sponsorship | We thank the World Health Organization, Dr. Foluke Fakorede, and Dr. Reto Brun for the preliminary screening of compounds under the WHO/TDR Training in Tropical Diseases program; A. G. Fernández and J. Casas for discussions; A. Gonzalez- Roura for early synthetic work; and S. Gonzalez and M. Lavigne for technical support. | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | American Society for Biochemistry and Molecular Biology | es_ES |
dc.rights | closedAccess | es_ES |
dc.subject | Infectious diseases | es_ES |
dc.subject | Malaria | es_ES |
dc.subject | Parasite Metabolism | es_ES |
dc.subject | Phosphatidylcholine | es_ES |
dc.subject | Phospholipid | es_ES |
dc.title | PG12, a Phospholipid Analog with Potent Antimalarial Activity, Inhibits Plasmodium falciparum CTP:Phosphocholine Cytidylyltransferase Activity | es_ES |
dc.type | artículo | es_ES |
dc.identifier.doi | 10.1074/jbc.M111.268946 | - |
dc.description.peerreviewed | Peer reviewed | es_ES |
dc.relation.publisherversion | http://dx.doi.org/10.1074/jbc.M111.268946 | es_ES |
dc.identifier.e-issn | 1083-351X | - |
dc.identifier.pmid | 21705805 | - |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.openairetype | artículo | - |
item.grantfulltext | none | - |
item.cerifentitytype | Publications | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.fulltext | No Fulltext | - |
item.languageiso639-1 | en | - |
Aparece en las colecciones: | (IQAC) Artículos |
CORE Recommender
PubMed Central
Citations
10
checked on 06-abr-2024
SCOPUSTM
Citations
19
checked on 15-abr-2024
WEB OF SCIENCETM
Citations
17
checked on 23-feb-2024
Page view(s)
586
checked on 23-abr-2024
Google ScholarTM
Check
Altmetric
Altmetric
Artículos relacionados:
NOTA: Los ítems de Digital.CSIC están protegidos por copyright, con todos los derechos reservados, a menos que se indique lo contrario.