GPCR activation: protonation and membrane potential
Protein & Cell
;
(12): 747-760, 2013.
Artículo
en Inglés
| WPRIM
| ID: wpr-757558
ABSTRACT
GPCR proteins represent the largest family of signaling membrane proteins in eukaryotic cells. Their importance to basic cell biology, human diseases, and pharmaceutical interventions is well established. Many crystal structures of GPCR proteins have been reported in both active and inactive conformations. These data indicate that agonist binding alone is not sufficient to trigger the conformational change of GPCRs necessary for binding of downstream G-proteins, yet other essential factors remain elusive. Based on analysis of available GPCR crystal structures, we identified a potential conformational switch around the conserved Asp2.50, which consistently shows distinct conformations between inactive and active states. Combining the structural information with the current literature, we propose an energy-coupling mechanism, in which the interaction between a charge change of the GPCR protein and the membrane potential of the living cell plays a key role for GPCR activation.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Conformación Proteica
/
Sitios de Unión
/
Transducción de Señal
/
Modelos Moleculares
/
Química
/
Proteínas de Unión al GTP
/
Receptores Acoplados a Proteínas G
/
Genética
/
Enlace de Hidrógeno
/
Potenciales de la Membrana
Tipo de estudio:
Estudio pronóstico
Límite:
Humanos
Idioma:
Inglés
Revista:
Protein & Cell
Año:
2013
Tipo del documento:
Artículo
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