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Quantifying Agonist Activity at G Protein-coupled Receptors

Quantifying Agonist Activity at G Protein-coupled Receptors

Published on: December 26, 2011

Conocimientos estructurales sobre la alostería del receptor acoplado a la proteína G

David M Thal¹, Alisa Glukhova², Patrick M Sexton²

¹Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Melbourne, Victoria, Australia. david.thal@monash.edu.

|July 6, 2018

Resumen

Los receptores acoplados a proteínas G (GPCR) son proteínas cruciales de la superficie celular que actúan alostéricamente. Estudios estructurales recientes revelan detalles atómicos de las transiciones alostéricas de GPCR, ofreciendo nuevas oportunidades de desarrollo terapéutico.

Área de la Ciencia:

La bioquímica
Biología molecular
Farmacología

Sus antecedentes:

Los receptores acoplados a proteínas G (GPCR) son proteínas integrales de la superficie celular que median la transducción de señales.
Los GPCR funcionan como proteínas alostéricas, que interactúan con diversas moléculas a través de dominios vinculados conformacionalmente.
Comprender los mecanismos alostéricos de la GPCR es vital para el descubrimiento de fármacos.

Objetivo del estudio:

Revisar estudios estructurales recientes de alta resolución de las GPCR.
Para aclarar los detalles atómicos de las transiciones alostéricas en GPCR.
Resaltar las oportunidades terapéuticas que presentan los sitios alostéricos farmacológicos en los GPCR.

Principales métodos:

Estudios estructurales de alta resolución (por ejemplo, criogenización, cristalografía de rayos X).
Análisis de los mecanismos de modulación alostérica.
Principios de diseño de fármacos basados en la estructura.

Principales resultados:

Estudios estructurales recientes proporcionan información a nivel atómico sobre las transiciones alostéricas de GPCR.
Los GPCR muestran diversos sitios alostéricos susceptibles a la orientación del fármaco.
La modulación alostérica ofrece una estrategia para desarrollar nuevas terapias.

Conclusiones:

Las estructuras de alta resolución son clave para comprender los mecanismos alostéricos de la GPCR.
La naturaleza alostérica de los GPCR presenta oportunidades significativas para el desarrollo de nuevos fármacos.
La orientación de los sitios alostéricos en los GPCR puede conducir a nuevas clases terapéuticas.

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