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De Novo Descubrimiento de marcos de cisteína para el desarrollo de bibliotecas de péptidos multicíclicos para el
Jinjing Li1, Hongtan Liu1, Shuling Xiao1
1The MOE Key Laboratory of Spectrochemical Analysis and Instrumentation, State Key Laboratory of Physical Chemistry of Solid Surfaces, Department of Chemistry, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen 361005, P. R. China.
Journal of the American Chemical Society
|December 13, 2023
Resumen
Los investigadores desarrollaron un nuevo método para descubrir nuevos marcos de cisteína para péptidos ricos en disulfuro (DRP). Este enfoque permite la creación de diversas bibliotecas DRP para el descubrimiento de potentes ligandos y fármacos peptídicos.
Área de la Ciencia:
- La bioquímica
- Biología estructural
- Diseño del péptido
Sus antecedentes:
- Los marcos de cisteína conservados son cruciales para la diversidad estructural de los péptidos ricos en disulfuro (DRP).
- Los métodos existentes para descubrir nuevas estructuras de cisteína con una robusta plegabilidad son limitados.
- El diseño de novo de los PDR requiere nuevas estrategias para el descubrimiento de marcos.
Objetivo del estudio:
- Desarrollar un método general para el descubrimiento de nuevos marcos de cisteína para péptidos ricos en disulfuro.
- Identificar marcos de cisteína con una robusta plegabilidad y compatibilidad con los sistemas de visualización de fagos.
- Para permitir el descubrimiento rápido de los ligandos peptídicos con altas afinidades de unión.
Principales métodos:
- Se ideó una estrategia basada en la piedra de toque, utilizando la plegabilidad oxidativa entre dos DRP en la superficie del fago.
- Se examinaron secuencias aleatorias para identificar estructuras únicas de cisteína.
- Los marcos identificados se utilizaron para desarrollar bibliotecas DRP multicíclicas.
Principales resultados:
- Se descubrieron nuevos marcos de cisteína con alta compatibilidad con la visualización de fagos y amplia tolerancia de secuencias.
- Los nuevos marcos facilitaron el desarrollo de bibliotecas DRP multicíclicas.
- Se descubrieron rápidamente los ligandos peptídicos con afinidades de unión de baja nanomolar y picomolar.
Conclusiones:
- La estrategia basada en "touchstone" ofrece un método sin precedentes para explorar la secuencia DRP y el espacio de la estructura.
- Este enfoque avanza significativamente en el diseño y el descubrimiento de ligandos y fármacos peptídicos multicíclicos.
- El estudio tiene el potencial de revolucionar el campo de la investigación de péptidos ricos en disulfuro.
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