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Peptide-Alkoxyamine Drugs: An Innovative Approach to Fight Schistosomiasis: “Digging Their Graves with Their Forks”

dc.rights.licenseopenen_US
dc.contributor.authorEMBO-IBOUANGA, Ange
dc.contributor.authorNGUYEN, Michel
hal.structure.identifierInstitut de Chimie Radicalaire [ICR]
dc.contributor.authorJOLY, Jean-Patrick
dc.contributor.authorCOUSTETS, Mathilde
dc.contributor.authorAUGEREAU, Jean-Michel
dc.contributor.authorPALOQUE, Lucie
dc.contributor.authorVANTHUYNE, Nicolas
dc.contributor.authorBIKANGA, Raphaël
dc.contributor.authorROBERT, Anne
dc.contributor.authorBENOIT-VICAL, Françoise
dc.contributor.authorAUDRAN, Gérard
hal.structure.identifierCentre de résonance magnétique des systèmes biologiques [CRMSB]
dc.contributor.authorMELLET, Philippe
dc.contributor.authorBOISSIER, Jérôme
dc.contributor.authorMARQUE, Sylvain
dc.date.accessioned2024-11-14T08:22:48Z
dc.date.available2024-11-14T08:22:48Z
dc.date.issued2024-06-06
dc.identifier.issn2076-0817en_US
dc.identifier.urihttps://oskar-bordeaux.fr/handle/20.500.12278/203259
dc.description.abstractEnThe expansion of drug resistant parasites sheds a serious concern on several neglected parasitic diseases. Our recent results on cancer led us to envision the use of peptide-alkoxyamines as a highly selective and efficient new drug against schistosome adult worms, the etiological agents of schistosomiasis. Indeed, the peptide tag of the hybrid compounds can be hydrolyzed by worm’s digestive enzymes to afford a highly labile alkoxyamine which homolyzes spontaneously and instantaneously into radicals—which are then used as a drug against Schistosome adult parasites. This approach is nicely summarized as digging their graves with their forks. Several hybrid peptide-alkoxyamines were prepared and clearly showed an activity: two of the tested compounds kill 50% of the parasites in two hours at a concentration of 100 µg/mL. Importantly, the peptide and alkoxyamine fragments that are unable to generate alkyl radicals display no activity. This strong evidence validates the proposed mechanism: a specific activation of the prodrugs by the parasite proteases leading to parasite death through in situ alkyl radical generation.
dc.description.sponsorshipCaractérisations moléculaires et cellulaires de voies de signalisation de la douleur: contrôle de la douleur dans l'ulcère de buruli comme source d'inspiration pour la conception rationnelle de nouveaux analgésiques puissantsen_US
dc.language.isoENen_US
dc.rights.urihttp://creativecommons.org/licenses/by/
dc.subject.enschistosoma
dc.subject.enalkoxyamines
dc.subject.enprodrug
dc.subject.ennew concept
dc.title.enPeptide-Alkoxyamine Drugs: An Innovative Approach to Fight Schistosomiasis: “Digging Their Graves with Their Forks”
dc.typeArticle de revueen_US
dc.identifier.doi10.3390/pathogens13060482en_US
dc.subject.halSciences du Vivant [q-bio]en_US
bordeaux.journalPathogensen_US
bordeaux.page482en_US
bordeaux.volume13en_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-04765955
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=Pathogens&rft.date=2024-06-06&rft.volume=13&rft.issue=6&rft.spage=482&rft.epage=482&rft.eissn=2076-0817&rft.issn=2076-0817&rft.au=EMBO-IBOUANGA,%20Ange&NGUYEN,%20Michel&JOLY,%20Jean-Patrick&COUSTETS,%20Mathilde&AUGEREAU,%20Jean-Michel&rft.genre=article


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