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El perfil proteómico químico de las bromodomainas permite la evaluación de amplio espectro de los inhibidores de la
Xin Li1, Yizhe Wu1, Gaofei Tian1
1Department of Chemistry , The University of Hong Kong , Pokfulam Road , Hong Kong , China.
Journal of the American Chemical Society
|June 28, 2019
Resumen
Los investigadores desarrollaron la foto-bromosporina (foto-BS), una nueva sonda para evaluar la selectividad del inhibidor de la bromodomaína en las células vivas. Este método ayuda a identificar objetivos de fármacos y evitar efectos secundarios en enfermedades como el cáncer.
Área de la Ciencia:
- Epigenética y biología cromatínica
- Biología química y proteómica
- Descubrimiento y desarrollo de fármacos
Sus antecedentes:
- Las bromodomaínas son lectores epigenéticos de la acetilación de la lisina, cruciales para la regulación de la cromatina.
- La disfunción del bromodomaín está relacionada con enfermedades humanas, incluido el cáncer, lo que las convierte en objetivos terapéuticos.
- La evaluación de la selectividad del inhibidor de la bromodomaína es vital debido a las similitudes estructurales entre las bromodomaínas.
Objetivo del estudio:
- Desarrollar un nuevo método para evaluar la selectividad de los inhibidores de la bromodomaína en las células vivas.
- Establecer una plataforma de proteómica química para la elaboración de un perfil completo de los inhibidores de la bromodomaína.
- Identificar objetivos conocidos y nuevos de los inhibidores de la bromodomaína.
Principales métodos:
- Desarrollo de una sonda de fotoafinidad, foto-bromosporina (foto-BS).
- Enlace cruzado inducido por la luz de bromodomaínas y proteínas que contienen bromodomaínas (BCP) in vitro y en células vivas.
- Análisis proteómico para identificar los BCP capturados por ensayos de foto-BS y de competencia de inhibidores.
Principales resultados:
- Photo-BS permitió el perfil de amplio espectro de los inhibidores de la bromodomaína en las células vivas.
- Photo-BS capturó 28 de los 42 BCP conocidos de las células vivas.
- El método identificó objetivos de bromodomaína conocidos y no caracterizados previamente para la bromosporina y GSK6853.
Conclusiones:
- Photo-BS proporciona una herramienta robusta para evaluar la selectividad del inhibidor de la bromodomaína en un contexto celular.
- La plataforma proteómica química desarrollada permite una evaluación exhaustiva de la selectividad de los inhibidores frente a los BCP endógenos.
- Este enfoque ayuda en el diseño y desarrollo racional de inhibidores selectivos de la bromodomaína para aplicaciones terapéuticas.
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