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Published on: February 21, 2019
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Mechanisms governing GPCR anterograde transport
Kevin Assoumou1, Sofia Papadogkonaki1, Itziar Muneta-Arrate1
1Department of Cell Physiology and Metabolism, University of Geneva, Switzerland.
FEBS Letters
|May 27, 2025
Summary
This review details how G protein-coupled receptors (GPCRs) are transported within cells. Understanding GPCR transport mechanisms is key for developing new therapies for diseases linked to these crucial membrane proteins.
Area of Science:
- Cell Biology
- Molecular Biology
- Neuroscience
Background:
- G protein-coupled receptors (GPCRs) are the largest family of human membrane proteins.
- GPCRs mediate cellular responses to external signals, impacting neurotransmission and cardiovascular function.
- Proper transport of GPCRs through the secretory pathway is essential for cell surface expression and ligand responsiveness.
Purpose of the Study:
- To provide a comprehensive overview of the cellular mechanisms governing GPCR folding, modification, and transport.
- To highlight regulatory proteins and signaling cues that modulate GPCR anterograde transport.
- To discuss therapeutic strategies for diseases involving misfolded GPCRs.
Main Methods:
- Literature review of cellular mechanisms
- Analysis of motif-driven interactions
- Discussion of pharmacological rescue strategies
Main Results:
- GPCR transport is orchestrated by specific cellular mechanisms and protein interactions.
- Signaling cues and specialized pathways regulate GPCR delivery, including to neuronal processes.
- Misfolded GPCR mutants often show intracellular retention, which can be pharmacologically addressed.
Conclusions:
- Anterograde transport plays a critical role in regulating GPCR function.
- Targeting GPCR transport mechanisms offers potential therapeutic avenues for various diseases.
- Insights into agonist-driven signaling within secretory organelles are emerging.
Keywords:
G protein‐coupled receptorGolgi apparatusanterograde transportendoplasmic reticulumneuronpharmacological chaperonepost‐translational modificationsecretory pathwaysignalingtrafficking motifMore Related Videos
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