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Un nuevo agente antimalárico de múltiples etapas que inhibe la síntesis de proteínas
Beatriz Baragaña1, Irene Hallyburton1, Marcus C S Lee2
1Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, UK.
Nature
|June 19, 2015
Resumen
Un nuevo compuesto antipalúdico, DDD107498, muestra una potente actividad contra los parásitos Plasmodium. Dirigido al factor de alargamiento de la traducción 2 (eEF2), ofrece un nuevo enfoque para combatir la resistencia a los medicamentos y tratar la malaria.
Área de la Ciencia:
- Descubrimiento y desarrollo de fármacos.
- Parasitología Parasitología.
- Biología molecular La biología molecular.
Sus antecedentes:
- Necesidad urgente de nuevos fármacos antipalúdicos debido a la resistencia emergente.
- Los tratamientos existentes tienen limitaciones en el espectro y la eficacia.
- La malaria sigue siendo un desafío significativo para la salud mundial.
Objetivo del estudio:
- Descubrir y caracterizar un nuevo compuesto antimalárico.
- Para identificar el objetivo molecular del nuevo compuesto.
- Para evaluar el potencial terapéutico del compuesto contra los parásitos Plasmodium.
Principales métodos:
- Cribado de alto rendimiento de compuestos contra parásitos de la malaria en la etapa sanguínea.
- Pruebas in vitro e in vivo de DDD107498 contra múltiples etapas del ciclo de vida del parásito.
- Identificación del objetivo molecular a través de ensayos bioquímicos.
Principales resultados:
- Descubrimiento de DDD107498, un potente compuesto antipalúdico.
- DDD107498 exhibe actividad contra múltiples etapas del ciclo de vida de Plasmodium.
- El objetivo molecular de DDD107498 fue identificado como el factor de alargamiento de traducción 2 (eEF2).
- El compuesto demostró buenas propiedades farmacocinéticas y un perfil de seguridad aceptable.
Conclusiones:
- DDD107498 es un prometedor nuevo candidato a fármaco antipalúdico con un novedoso mecanismo de acción.
- Dirigirse al eEF2 representa una estrategia viable para desarrollar nuevas terapias antimaláricas.
- DDD107498 tiene potencial para el tratamiento de dosis única, el bloqueo de la transmisión y la quimioprotección.
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