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La nueva arma contra la farmacorresistencia de la malaria

Hasta ahora, el parásito de la malaria ha tenido una respuesta a todos los métodos de control que le han lanzado.

A pesar de los avances significativos en la lucha contra él, incluido el lanzamiento de una vacuna prometedora, pero que solo muestra alrededor del 30 por ciento de efectividad contra la enfermedad grave, y docenas de medicamentos, el parásito siempre regresa.

Actualmente, el tratamiento recomendado para la infección por paludismo es una terapia combinada de artemisinina, una combinación de medicamentos de acción rápida y lenta diseñados para tratar la infección por paludismo y prevenir la transmisión.

Sin embargo, las terapias combinadas no logran curar las infecciones en más del 50 por ciento de los pacientes en algunas regiones del sudeste asiático. Además, ahora también se ha detectado resistencia a las artemisininas en África, donde se producen la mayoría de las 600.000 muertes al año provocadas por la malaria.

Para ayudar a salvar vidas y mejorar la calidad de vida, se necesitan desesperadamente medicamentos innovadores que alcancen nuevos objetivos. Imagen: Getty Images

Para ayudar a salvar vidas y mejorar la calidad de vida, se necesitan desesperadamente medicamentos innovadores que alcancen nuevos objetivos y utilicen nuevos mecanismos de acción.

El profesor Leann Tilley, del Departamento de Bioquímica y Farmacología de la Universidad de Melbourne, forma parte de un equipo de investigación internacional que trabaja para abordar las preocupaciones mundiales de que los tratamientos antipalúdicos actuales están perdiendo rápidamente su eficacia.

El profesor Tilley y sus colegas han publicado un primer descubrimiento mundial en la revista Science que muestra que una clase de sustancias químicas que antes se pasaba por alto, conocida como sulfamatos de nucleósidos o “nukes”, puede hacer que las enzimas del parásito de la malaria involucradas en la síntesis de proteínas se autodestruyan.

Estos nuevos objetivos son muy efectivos porque las enzimas de síntesis de proteínas juegan un papel fundamental en el mantenimiento y crecimiento de las células.

Plasmodium falciparum (representado dentro de los glóbulos rojos) es el más letal de todos los parásitos de la malaria. Imagen: Getty Images

De particular importancia, se espera que los inhibidores de esta vía sean activos contra todas las etapas del parásito de la malaria, efectivos tanto para el tratamiento como para prevenir la transmisión a nuevas víctimas.

Específicamente, se descubrió que los sulfamatos de nucleósidos secuestran la propia maquinaria celular del parásito, induciendo a las enzimas involucradas en la producción de proteínas a crear sus propios inhibidores, deteniendo así los procesos que son esenciales para la supervivencia del parásito.

Este mecanismo no se había informado previamente para las enzimas de síntesis de proteínas.

Trabajando con el máximo organismo para el desarrollo de fármacos antipalúdicos, Medicines for Malaria Venture y Takeda Pharmaceuticals, así como con laboratorios de investigación de los cinco continentes, el gran equipo internacional comenzó su investigación con compuestos que Takeda estaba investigando para tratar el cáncer.

El equipo identificó una serie de compuestos que afectan al parásito de la malaria, pero no a las células humanas, pero no se entendió el mecanismo de toxicidad.

Representación esquemática del objetivo de un nuevo compuesto antipalúdico, ML901 (estructura coloreada), que muestra una inhibición altamente específica y potente del parásito de la malaria, pero no es tóxico para las células de los mamíferos. ML901 encuentra una grieta particular en una enzima llamada tirosina ARNt sintetasa (representada en rosa), parte de la maquinaria que utiliza el parásito de la malaria para generar las proteínas necesarias para reproducirse. El parásito se detiene rápidamente y no puede causar enfermedades ni transmitirse a otras personas a través de los mosquitos (púrpura).

El trabajo adicional del Dr. Stanley Xie y la Dra. Elyse Dunn, del Departamento de Bioquímica y Farmacología, en estrecha colaboración con colegas de Takeda Pharmaceuticals, permitió al equipo descubrir que los sulfamatos de nucleósidos secuestran las enzimas de síntesis de proteínas para formar conjugados covalentes de inhibidores y aminoácidos, un poco como superpegar una llave en una cerradura para que la cerradura ya no funcione.

Los colegas del Departamento de Bioquímica y Farmacología, el Dr. Riley Metcalf, el Dr. Craig Morton y el Profesor Asociado Mike Griffin resolvieron la estructura de la proteína.

La siguiente fase fue probar la ML901 en un conjunto de ensayos de malaria proporcionados por Medicines for Malaria Venture. Estos ensayos están diseñados para garantizar que los candidatos a fármacos cumplan los criterios para un mayor desarrollo.

El equipo demostró que ML901 es activo contra todas las etapas y cepas del parásito de la malaria probado. Es importante destacar que ML901 exhibe una actividad rápida y prolongada que proporciona una potente eliminación de parásitos en un modelo animal de paludismo humano que cumple los criterios para un tratamiento rápido y eficaz de los pacientes con paludismo.

Más información: Universidad de Melbourne

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