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Related Concept Videos

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G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
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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.
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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.
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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...
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Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
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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.
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Interclass GPCR heteromerization affects localization and trafficking.

Rudy Toneatti1, Jong M Shin1, Urjita H Shah1

  • 1Department of Physiology and Biophysics, School of Medicine, Virginia Commonwealth University, Richmond, VA 23298, USA.

Science Signaling
|October 21, 2020
PubMed
Summary
This summary is machine-generated.

G protein-coupled receptor (GPCR) heteromerization influences receptor trafficking. Serotonin 5-HT2A receptors (5-HT2ARs) and metabotropic glutamate receptor 2 (mGluR2) heteromers alter subcellular distribution, suggesting heteromerization is a key sorting mechanism.

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Area of Science:

  • Neuroscience
  • Cell Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) regulate cellular activity.
  • GPCRs can form heteromers, influencing their function.
  • Membrane trafficking is crucial for GPCR regulation.

Purpose of the Study:

  • To investigate the role of serotonin 5-HT2A receptor (5-HT2A R) and metabotropic glutamate receptor 2 (mGluR2) heteromerization in receptor localization and trafficking.
  • To determine if heteromer formation is necessary for altered subcellular distribution.

Main Methods:

  • Coexpression of 5-HT2A R and mGluR2 in mammalian cells.
  • Pharmacological manipulation with agonists and antagonists (clozapine, M100907).
  • Use of TAT-tagged peptides and chimeric constructs to disrupt heteromerization.
  • Analysis of receptor localization in cells and mouse frontal cortex neurons.

Main Results:

  • 5-HT2A R and mGluR2 form functional heteromers.
  • Heteromerization altered the intracellular distribution of mGluR2.
  • Pharmacological blockade of 5-HT2A R affected mGluR2 density via heteromerization.
  • Disruption of heteromerization abolished 5-HT2A R-dependent trafficking effects.
  • 5-HT2A R expression increased intracellular mGluR2 localization in neurons.

Conclusions:

  • GPCR heteromerization is a novel mechanism for regulating receptor trafficking and sorting.
  • The interaction between 5-HT2A R and mGluR2 influences their subcellular localization.
  • Heteromer formation is essential for the observed trafficking changes.