Beneath the surface: endosomal GPCR signaling.
Trends Biochem Sci
; 49(6): 520-531, 2024 Jun.
Article
em En
| MEDLINE
| ID: mdl-38643023
ABSTRACT
G protein-coupled receptors (GPCRs) located at the cell surface bind extracellular ligands and convey intracellular signals via activation of heterotrimeric G proteins. Traditionally, G protein signaling was viewed to occur exclusively at this subcellular region followed by rapid desensitization facilitated by ß-arrestin (ßarr)-mediated G protein uncoupling and receptor internalization. However, emerging evidence over the past 15 years suggests that these ßarr-mediated events do not necessarily terminate receptor signaling and that some GPCRs continue to activate G proteins after having been internalized into endosomes. Here, we review the recently elucidated mechanistic basis underlying endosomal GPCR signaling and discuss physiological implications and pharmacological targeting of this newly appreciated signaling mode.
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Base de dados:
MEDLINE
Assunto principal:
Endossomos
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Transdução de Sinais
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Receptores Acoplados a Proteínas G
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article