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Hybrid Peptide-Alkoxyamine Drugs: A Strategy for the Development of a New Family of Antiplasmodial Drugs

dc.rights.licenseopenen_US
dc.contributor.authorEMBO-IBOUANGA, Ange
dc.contributor.authorNGUYEN, Michel
dc.contributor.authorPALOQUE, Lucie
dc.contributor.authorCOUSTETS, Mathilde
hal.structure.identifierInstitut de Chimie Radicalaire [ICR]
dc.contributor.authorJOLY, Jean-Patrick
dc.contributor.authorAUGEREAU, Jean-Michel
dc.contributor.authorVANTHUYNE, Nicolas
dc.contributor.authorBIKANGA, Raphaël
dc.contributor.authorCOQUIN, Naomie
dc.contributor.authorROBERT, Anne
dc.contributor.authorAUDRAN, Gérard
dc.contributor.authorBOISSIER, Jérôme
hal.structure.identifierCentre de résonance magnétique des systèmes biologiques [CRMSB]
dc.contributor.authorMELLET, Philippe
dc.contributor.authorBENOIT-VICAL, Françoise
dc.contributor.authorMARQUE, Sylvain
dc.date.accessioned2024-11-14T12:16:16Z
dc.date.available2024-11-14T12:16:16Z
dc.date.issued2024-03-21
dc.identifier.issn1420-3049en_US
dc.identifier.urihttps://oskar-bordeaux.fr/handle/20.500.12278/203264
dc.description.abstractEnThe emergence and spread of drug-resistant Plasmodium falciparum parasites shed a serious concern on the worldwide control of malaria, the most important tropical disease in terms of mortality and morbidity. This situation has led us to consider the use of peptide-alkoxyamine derivatives as new antiplasmodial prodrugs that could potentially be efficient in the fight against resistant malaria parasites. Indeed, the peptide tag of the prodrug has been designed to be hydrolysed by parasite digestive proteases to afford highly labile alkoxyamines drugs, which spontaneously and instantaneously homolyse into two free radicals, one of which is expected to be active against P. falciparum. Since the parasite enzymes should trigger the production of the active drug in the parasite’s food vacuoles, our approach is summarized as “to dig its grave with its fork”. However, despite promising sub-micromolar IC50 values in the classical chemosensitivity assay, more in-depth tests evidenced that the anti-parasite activity of these compounds could be due to their cytostatic activity rather than a truly anti-parasitic profile, demonstrating that the antiplasmodial activity cannot be based only on measuring antiproliferative activity. It is therefore imperative to distinguish, with appropriate tests, a genuinely parasiticidal activity from a cytostatic activity.
dc.language.isoENen_US
dc.rightsAttribution 3.0 United States*
dc.rights.urihttp://creativecommons.org/licenses/by/3.0/us/*
dc.title.enHybrid Peptide-Alkoxyamine Drugs: A Strategy for the Development of a New Family of Antiplasmodial Drugs
dc.title.alternativeMoleculesen_US
dc.typeArticle de revueen_US
dc.identifier.doi10.3390/molecules29061397en_US
dc.subject.halSciences du Vivant [q-bio]en_US
dc.identifier.pubmed38543034en_US
bordeaux.journalMoleculesen_US
bordeaux.page1397en_US
bordeaux.volume29en_US
bordeaux.hal.laboratoriesCentre de Résonance Magnétique des Systèmes Biologiques (CRMSB) - UMR 5536en_US
bordeaux.issue6en_US
bordeaux.institutionUniversité de Bordeauxen_US
bordeaux.institutionCNRSen_US
bordeaux.peerReviewedouien_US
bordeaux.inpressnonen_US
bordeaux.import.sourcehal
hal.identifierhal-04765959
hal.version1
hal.popularnonen_US
hal.audienceInternationaleen_US
hal.exportfalse
workflow.import.sourcehal
dc.rights.ccPas de Licence CCen_US
bordeaux.COinSctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Molecules&rft.date=2024-03-21&rft.volume=29&rft.issue=6&rft.spage=1397&rft.epage=1397&rft.eissn=1420-3049&rft.issn=1420-3049&rft.au=EMBO-IBOUANGA,%20Ange&NGUYEN,%20Michel&PALOQUE,%20Lucie&COUSTETS,%20Mathilde&JOLY,%20Jean-Patrick&rft.genre=article


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