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Related Experiment Videos

GPCR signalling from within the cell.

Yuh-Jiin I Jong1, Steven K Harmon1, Karen L O'Malley1

  • 1Department of Neuroscience, Washington University School of Medicine, St. Louis, MO, USA.

British Journal of Pharmacology
|September 6, 2017
PubMed
Summary
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Emerging research reveals G protein-coupled receptors (GPCRs) function not only on the cell surface but also within cells. Intracellular GPCRs play key roles in biological functions, suggesting new therapeutic targets.

Area of Science:

  • Molecular Pharmacology
  • Cell Biology
  • Neurobiology

Background:

  • G protein-coupled receptors (GPCRs) traditionally signal from the cell surface.
  • Emerging evidence indicates GPCRs are present on and signal from intracellular membranes.
  • These intracellular GPCRs exhibit distinct signaling, desensitization, and distribution patterns.

Purpose of the Study:

  • To review the emerging roles and significance of intracellular GPCRs.
  • To highlight the dynamic functions of intracellular GPCRs in various biological processes.
  • To discuss the therapeutic implications of targeting intracellular GPCRs.

Main Methods:

  • Literature review of recent studies on GPCR localization and function.
  • Analysis of data supporting intracellular GPCR activation and signaling.

Related Experiment Videos

  • Synthesis of findings on the biological roles of intracellular GPCRs.

    • Main Results:

    • GPCRs are found on diverse intracellular membranes, not just the cell surface.
    • Intracellular GPCRs can be activated in situ or after endocytosis.
    • These receptors are implicated in learning, memory, contractility, and angiogenesis.

    Conclusions:

    • Intracellular GPCRs represent a significant signaling paradigm beyond the cell surface.
    • Understanding intracellular GPCR functions is crucial for elucidating complex biological processes.
    • Targeting both cell surface and intracellular GPCRs may yield novel therapeutic strategies.