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El receptor huérfano GPR158 sirve como receptor metabotrópico de la glicina: mGlyR

Thibaut Laboute¹, Stefano Zucca¹, Matthew Holcomb²

¹Department of Neuroscience, UF Scripps Biomedical Research, Jupiter, FL 33458, USA.

Science (New York, N.Y.)

|March 30, 2023

Resumen

Los investigadores descubrieron GPR158 como un nuevo receptor metabotrópico de glicina (mGlyR). Este hallazgo revela un nuevo sistema para cómo la glicina modula la actividad neuronal, impactando la cognición y los estados afectivos.

Área de la Ciencia:

La neurociencia
Biología molecular
Farmacología

Sus antecedentes:

La glicina es un neurotransmisor clave en los procesos neuronales fundamentales.
No se identificó el receptor metabotrópico para los efectos neuromoduladores lentos de la glicina.

Objetivo del estudio:

Identificar el receptor huérfano acoplado a la proteína G que media los efectos metabotrópicos de la glicina.
Para aclarar el mecanismo de la neuromodulación de la glicina a través de este receptor.

Principales métodos:

Identificación del receptor acoplado a la proteína G (GPCR).
Ensayos de unión de ligandos utilizando glicina y taurina.
Ensayos de inhibición del regulador de la proteína G que señala el complejo 7-G-proteína β5 (RGS7-Gβ5).
Medición de la producción de adenosina 3',5'-monofosfato (cAMP).
Evaluación de la excitabilidad neuronal en las neuronas corticales.

Principales resultados:

GPR158 fue identificado como un receptor metabotrópico de glicina (mGlyR).
La glicina y la taurina se unen al dominio Cache de GPR158, inhibiendo la actividad de RGS7-Gβ5.
La señalización de glicina a través de mGlyR suprime la producción de cAMP.
La glicina, pero no la taurina, modula la excitabilidad de las neuronas corticales a través de mGlyR.

Conclusiones:

El GPR158 funciona como un receptor metabotrópico de la glicina (mGlyR).
Este descubrimiento revela un sistema neuromodulador significativo para la glicina.
Los hallazgos tienen implicaciones para comprender la cognición y los estados afectivos.

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