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Mecanismo de bloqueo del canal del receptor NMDA por MK-801 y memantina
Xianqiang Song1, Morten Ø Jensen2, Vishwanath Jogini2
1Vollum Institute, Oregon Health & Science University, Portland, OR, USA.
Nature
|April 20, 2018
Resumen
El receptor del N-metil-D-aspartato (NMDA)
Área de la Ciencia:
- La neurociencia
- Biología estructural
- Farmacología
Sus antecedentes:
- El receptor de N-metil-D-aspartato (NMDA) es crucial para la plasticidad sináptica y la memoria.
- Comprender la función del receptor NMDA es vital para el tratamiento de trastornos neurológicos.
- Las estructuras de alta resolución de los receptores NMDA faltan, lo que dificulta la comprensión mecanicista del bloqueo del canal iónico.
Objetivo del estudio:
- Para aclarar el mecanismo estructural del bloqueo del canal iónico del receptor NMDA.
- Para identificar el sitio de unión de los bloqueadores de los canales del receptor NMDA MK-801 y la memantina.
Principales métodos:
- Cristalización de un receptor truncado de NMDA GluN1-GluN2B.
- Cristalografía de rayos X para determinar la estructura del receptor.
- Simulaciones de dinámica molecular a larga escala.
Principales resultados:
- Se obtuvo una estructura cristalina de alta resolución del receptor NMDA.
- El sitio de unión para MK-801 fue mapeado dentro del vestíbulo del canal iónico.
- MK-801 y la memantina obstruyen físicamente la permeación de iones promoviendo el cierre de la puerta del canal.
Conclusiones:
- El estudio revela el mecanismo preciso del bloqueo del canal del receptor NMDA por MK-801 y la memantina.
- Las ideas estructurales explican cómo estos bloqueadores ocluyen el flujo de iones.
- Los hallazgos avanzan en la comprensión de la farmacología de los receptores NMDA y el desarrollo de fármacos para afecciones neurológicas.
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