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Related Concept Videos

G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high affinity and are together...
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical, 7TM, or...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...

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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Published on: June 9, 2017

G-protein regulatory network governs receptor internalization dynamics.

Jacob B Rowe1, Shubhi Pandey1, Ryan A Mayer2

  • 1Department of Physiology and Biophysics, University of Miami Miller School of Medicine, Miami, FL 33136.

Proceedings of the National Academy of Sciences of the United States of America
|June 9, 2026
PubMed
Summary

G protein-coupled receptor (GPCR) internalization is dynamically controlled by G-protein signaling regulation. Understanding this interplay is crucial for deciphering GPCR function and associated diseases.

Keywords:
G proteinsGNAO1 disorderGPCRinternalization

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Area of Science:

  • Cellular Biology
  • Biochemistry
  • Neuroscience

Background:

  • G protein-coupled receptors (GPCRs) are vital for cellular communication and physiological functions.
  • GPCR signaling is modulated by internalization, a process affecting cellular localization and signaling diversity.
  • The impact of G-protein cycle regulation on GPCR internalization remains incompletely understood.

Purpose of the Study:

  • To systematically investigate how G-protein cycle regulation influences GPCR internalization.
  • To elucidate the mechanisms governing GPCR internalization dynamics.
  • To explore the role of G-protein variants in GPCR internalization.

Main Methods:

  • Systematic analysis of G-protein cycle components (GEFs, AGS, RGS) and their effect on GPCR internalization.
  • Investigation of the interplay between G-protein component balance, GPCR kinase activity, and receptor localization.
  • Examination of disease-associated GαoA variants in the context of GPCR internalization regulation.

Main Results:

  • GPCR internalization is modulated by the timing of G-protein activation/deactivation and G-protein cycle lifetime.
  • G-protein component balance and activity, alongside GPCR kinase activity, dictate GPCR spatial distribution.
  • Disease-associated GαoA variants disrupt the regulatory network controlling GPCR internalization.

Conclusions:

  • GPCR internalization is not a static property but is dynamically regulated by G-protein activation kinetics, cycle duration, and Gα/Gβγ availability.
  • Dysregulation of GPCR internalization dynamics due to altered G-protein networks may contribute to complex disease phenotypes.
  • This study establishes key principles governing GPCR internalization, linking G-protein signaling to receptor trafficking and cellular function.