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A Chemically Stable Fluorescent Mimic of Dihydroartemisinin, Artemether, and Arteether with Conserved Bioactivity and Specificity Shows High Pharmacological Relevance to the Antimalarial Drugs.
Sissoko, Abdoulaye; Vásquez-Ocmín, Pedro; Maciuk, Alexandre; Barbieri, Daniela; Neveu, Gaëlle; Rondepierre, Laurine; Grougnet, Raphaël; Leproux, Pascale; Blaud, Magali; Hammad, Karim; Michel, Sylvie; Lavazec, Catherine; Clain, Jérôme; Houzé, Sandrine; Duval, Romain.
Afiliación
  • Sissoko A; Université de Paris, MERIT, IRD, F-75006 Paris, France.
  • Vásquez-Ocmín P; Laboratoire d'Excellence GR-Ex, Paris, France.
  • Maciuk A; Université Paris-Saclay, CNRS, BioCIS, F-92290 Châtenay-Malabry, France.
  • Barbieri D; Université Paris-Saclay, CNRS, BioCIS, F-92290 Châtenay-Malabry, France.
  • Neveu G; Laboratoire d'Excellence GR-Ex, Paris, France.
  • Rondepierre L; Université de Paris, U1016, INSERM, and UMR 8104, CNRS, F-75014 Paris, France.
  • Grougnet R; Laboratoire d'Excellence GR-Ex, Paris, France.
  • Leproux P; Université de Paris, U1016, INSERM, and UMR 8104, CNRS, F-75014 Paris, France.
  • Blaud M; Université de Paris, MERIT, IRD, F-75006 Paris, France.
  • Hammad K; Laboratoire d'Excellence GR-Ex, Paris, France.
  • Michel S; Université de Paris, CiTCoM, CNRS, F-75006 Paris, France.
  • Lavazec C; Université de Paris, CiTCoM, CNRS, F-75006 Paris, France.
  • Clain J; Université de Paris, CiTCoM, CNRS, F-75006 Paris, France.
  • Houzé S; Université de Paris, CiTCoM, CNRS, F-75006 Paris, France.
  • Duval R; Université de Paris, CiTCoM, CNRS, F-75006 Paris, France.
ACS Infect Dis ; 6(7): 1532-1547, 2020 07 10.
Article en En | MEDLINE | ID: mdl-32267151
Three novel tracers designed as fluorescent surrogates of artemisinin-derived antimalarial drugs (i.e., dihydroartemisinin, artemether, arteether, and artemisone) were synthesized from dihydroartemisinin. One of these tracers, corresponding to a dihydroartemisinin/artemether/arteether mimic, showed a combination of excellent physicochemical and biological properties such as hydrolytic stability, high inhibitory potency against blood-stage parasites, similar ring-stage survival assay values than the clinical antimalarials, high cytopermeability and specific labeling of live P. falciparum cells, alkylation of heme, as well as specific covalent labeling of drug-sensitive and drug-resistant P. falciparum proteomes at physiological concentrations, consistent with a multitarget action of the drugs. Our study demonstrates that probes containing the complete structural core of clinical artemisinin derivatives can be stable in biochemical and cellular settings, and recapitulate the complex mechanisms of these frontline, yet threatened, antimalarial drugs.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Artemisininas / Antimaláricos Idioma: En Revista: ACS Infect Dis Año: 2020 Tipo del documento: Article País de afiliación: Francia Pais de publicación: Estados Unidos
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Artemisininas / Antimaláricos Idioma: En Revista: ACS Infect Dis Año: 2020 Tipo del documento: Article País de afiliación: Francia Pais de publicación: Estados Unidos