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Desarrollo de sondas basadas en la actividad para ubiquitina y vías de señalización de proteínas similares a la

Heeseon An¹, Alexander V Statsyuk

¹Department of Chemistry, Center for Molecular Innovation and Drug Discovery, Chemistry of Life Processes Institute, Northwestern University , Silverman Hall, 2145 Sheridan Road, Evanston, Illinois 60208, United States.

Journal of the American Chemical Society

|October 22, 2013

Resumen

Los investigadores desarrollaron ABP1, una nueva sonda de moléculas pequeñas. Esta herramienta detecta proteínas activas similares a la ubiquitina (UBL) y monitorea la actividad de la enzima E1 en las células, ayudando al desarrollo de fármacos.

Área de la Ciencia:

La bioquímica es la bioquímica.
Biología celular Biología celular.
Biología Molecular Biología Molecular

Sus antecedentes:

La ubiquitina y las proteínas similares a la ubiquitina (UBL) son reguladores cruciales de diversos procesos celulares.
Las proteínas UBL, a pesar de la variación de la secuencia, comparten una estructura 3D común (pliegue β-grasp).
Las enzimas E1 que activan la UBL son fundamentales para la señalización de la UBL y son objetivos farmacológicos emergentes.

Objetivo del estudio:

Desarrollar un método para descubrir proteínas UBL.
Para crear una herramienta para el monitoreo de la actividad de la enzima E1 intracelular.
Para permitir la evaluación de los mecanismos inhibidores de la enzima E1.

Principales métodos:

Desarrollo de una sonda de moléculas pequeñas basada en el mecanismo, ABP1.1.
Utilizando ABP1 para detectar proteínas UBL activas en células intactas.
Empleando ABP1 para monitorear la actividad de la enzima E1 intracelular.

Principales resultados:

ABP1 detecta y descubre con éxito las proteínas UBL activas.
ABP1 permite el monitoreo de la actividad de la enzima E1 intracelular.
ABP1 puede perfilar la selectividad de los inhibidores de la enzima E1 in vitro y en las células.

Conclusiones:

ABP1 es una herramienta valiosa para el estudio de los sistemas UBL.
La sonda facilita la investigación de los mecanismos de acción de los inhibidores de la enzima E1.
ABP1 ayuda en el descubrimiento y desarrollo de fármacos dirigidos a las vías UBL.

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