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Related Concept Videos

G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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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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G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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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.
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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Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

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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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Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

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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.
GPCRs are also called heptahelical,...
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GPCR Desensitization01:12

GPCR Desensitization

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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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Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

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Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
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Updated: Dec 30, 2025

Inhibitory Synapse Formation in a Co-culture Model Incorporating GABAergic Medium Spiny Neurons and HEK293 Cells Stably Expressing GABAA Receptors
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G Protein-Coupled Glutamate and GABA Receptors Form Complexes and Mutually Modulate Their Signals.

Hakushun Sakairi1, Yuji Kamikubo1, Masayoshi Abe2

  • 1Department of Pharmacology , Juntendo University School of Medicine , Hongo 2-1-1 , Bunkyo-ku, Tokyo 113-8421 , Japan.

ACS Chemical Neuroscience
|January 25, 2020
PubMed
Summary
This summary is machine-generated.

This study shows that gamma-aminobutyric acid (GABA) and glutamate receptors physically interact on cell surfaces, influencing each other's signaling pathways. This molecular crosstalk is crucial for understanding complex neural responses and synaptic plasticity.

Keywords:
B-type gamma-amino butyric acid receptorGPCRcomplex formationlive cell imagingmetabotropic glutamate receptorsignaling crosstalk

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HSV-Mediated Transgene Expression of Chimeric Constructs to Study Behavioral Function of GPCR Heteromers in Mice
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Area of Science:

  • Neuroscience
  • Molecular Biology
  • Cellular Signaling

Background:

  • Protein interactions form complex molecular networks governing cellular functions.
  • Interactions between G protein-coupled receptors (GPCRs), particularly neurotransmitter GPCRs, are key to neural responses.
  • The B-type gamma-aminobutyric acid (GABA) receptor (GBR) and type-1 metabotropic glutamate receptor (mGluR1) are distinct GPCRs involved in neurotransmission.

Purpose of the Study:

  • To investigate the physical and functional interaction between GBR and mGluR1.
  • To provide evidence for GPCR complex formation and mutual signaling modulation.
  • To enhance understanding of molecular integration in neural networks.

Main Methods:

  • Utilized stable cell lines and rat cerebella for experimentation.
  • Employed cell-surface imaging and coimmunoprecipitation analysis to detect GPCR interaction.
  • Applied fluorometry to assess the modulation of signal transduction between GPCRs.

Main Results:

  • Confirmed physical interaction between GBR and mGluR1 on the cell surface.
  • Demonstrated that these GPCRs mutually modulate their respective signal transduction pathways.
  • Provided evidence for the intrinsic ability of mGluR1 and GBR to form complexes.

Conclusions:

  • mGluR1 and GBR directly interact and influence each other's signaling.
  • This GPCR interaction contributes to the complexity of molecular networks underlying synaptic plasticity.
  • Findings advance the understanding of neurotransmission and GPCR function.