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Inhibidores de péptidos bicíclicos permeables a las células contra las proteínas intracelulares
Wenlong Lian1, Bisheng Jiang, Ziqing Qian
1Department of Chemistry and Biochemistry, The Ohio State University , 484 West 12th Avenue, Columbus, Ohio 43210, United States.
Journal of the American Chemical Society
|June 28, 2014
Resumen
Los péptidos cíclicos se pueden hacer permeables a las células fusionándolos con péptidos que penetran en las células, creando péptidos bicíclicos. Esta estrategia produce potentes inhibidores de enzimas, mejorando su potencial terapéutico.
Área de la Ciencia:
- La bioquímica es la bioquímica.
- Biología Molecular Biología Molecular
- Química Medicinal La Química Medicinal es el campo de la Química Medicinal.
Sus antecedentes:
- Los péptidos cíclicos se muestran prometedores como terapias, pero luchan con la permeabilidad de la membrana celular.
- La entrada celular es un obstáculo importante para la aplicación terapéutica de muchos péptidos cíclicos.
Objetivo del estudio:
- Desarrollar péptidos cíclicos permeables a las células mediante su fusión con péptidos cíclicos que penetran en las células.
- Para crear nuevos inhibidores para la proteína tirosina fosfatasa 1B y la peptidil-prolyl cis-trans isomerasa (Pin1).
Principales métodos:
- Fusión de péptidos cíclicos con péptidos cíclicos que penetran en las células para formar estructuras bicíclicas.
- Evaluar la actividad inhibidora, la selectividad y la estabilidad proteolítica de los péptidos bicíclicos resultantes contra las enzimas diana.
Principales resultados:
- Generó con éxito péptidos bicíclicos permeables a las células con el reconocimiento del objetivo retenido.
- Desarrolló inhibidores potentes, selectivos y proteolíticamente estables para la proteína tirosina fosfatasa 1B y Pin1.
- Actividad biológica demostrada de los nuevos inhibidores de péptidos bicíclicos in vitro.
Conclusiones:
- La fusión con péptidos cíclicos que penetran en las células es una estrategia efectiva para mejorar la permeabilidad celular del péptido cíclico.
- Los péptidos bicíclicos resultantes son candidatos prometedores para el desarrollo terapéutico como inhibidores de enzimas.
- Este enfoque amplía la utilidad de los péptidos cíclicos en la investigación biológica y el descubrimiento de fármacos.
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