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Los péptidos macrocíclicos como fármacos candidatos: avances recientes y desafíos pendientes
Alexander A Vinogradov1, Yizhen Yin1, Hiroaki Suga1
1Department of Chemistry, Graduate School of Science , The University of Tokyo , 7-3-1 Hongo , Bunkyo-ku, Tokyo 113-0033 , Japan.
Journal of the American Chemical Society
|February 16, 2019
Resumen
Las terapias con péptidos son prometedoras, pero se enfrentan a desafíos con la estabilidad y la entrega. Esta revisión explora estrategias como la macrociclización y los aminoácidos no nativos para mejorar las propiedades de los medicamentos peptídicos para mejorar el éxito terapéutico.
Área de la Ciencia:
- Química medicinal
- Descubrimiento de drogas
- Biotecnología
Sus antecedentes:
- Los péptidos son terapéuticos atractivos debido a su accesibilidad sintética y su unión específica.
- La baja estabilidad metabólica y la permeabilidad celular limitan el éxito clínico de los fármacos peptídicos.
- La orientación a las superficies de proteínas "indrugables" es una ventaja clave de las terapias con péptidos.
Objetivo del estudio:
- Revisar estrategias para mejorar las propiedades farmacológicas de los péptidos.
- Analizar el progreso y los desafíos en la mejora de la farmacología de los péptidos.
- Discutir el equilibrio de las consideraciones contradictorias para los candidatos óptimos a fármacos péptidos.
Principales métodos:
- Revisión de las técnicas de macrociclización para el desarrollo de fármacos peptídicos.
- Análisis de la incorporación de aminoácidos no proteogénicos en el diseño de los péptidos.
- Examen de las estrategias de conjugación para mejorar las características de los péptidos.
Principales resultados:
- La macrociclización, los aminoácidos no nativos y la conjugación mejoran la estabilidad metabólica del péptido y la permeabilidad celular.
- Estas modificaciones pueden superar las limitaciones de los péptidos bioactivos de novo descubiertos.
- Los avances recientes demuestran la viabilidad de mejorar las propiedades farmacológicas individuales.
Conclusiones:
- La optimización de los candidatos a fármacos péptidos requiere equilibrar múltiples propiedades farmacológicas.
- La interfaz de consideraciones contradictorias es crucial para el avance de las terapias con péptidos.
- Las modificaciones estratégicas ofrecen una vía para superar las limitaciones inherentes a los péptidos para el desarrollo de fármacos.
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