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Related Concept Videos

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...
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...
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.
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...

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Related Experiment Video

Updated: Jul 10, 2026

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

Basic concepts in G-protein-coupled receptor homo- and heterodimerization.

Rafael Franco1, Vicent Casadó, Antoni Cortés

  • 1Institut d'Investigació Biomèdica August Pi i Sunyer, Centro de Investigación Biomédica en Red sobre Enfermedades Neurodegenerativas and Departament de Bioquímica i Biologia Molecular, Universitat de Barcelona, Barcelona, Catalonia, Spain. rfranco@ub.edu

Thescientificworldjournal
|November 6, 2007
PubMed
Summary

G-protein-coupled receptors (GPCRs) form dimers and oligomers, altering their drug interactions and signaling. Understanding these GPCR complexes is crucial for developing new central nervous system (CNS) therapeutics.

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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
09:12

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

Published on: September 10, 2016

Area of Science:

  • Neuroscience
  • Molecular Biology
  • Pharmacology

Background:

  • G-protein-coupled receptors (GPCRs) were traditionally viewed as monomers.
  • Emerging evidence shows GPCRs form homodimers, heterodimers, and higher-order oligomers on cell surfaces.

Purpose of the Study:

  • To discuss the fundamental concepts and recent advancements in GPCR homo- and heteromerization.
  • To highlight the impact of GPCR dimerization on receptor pharmacology, trafficking, and signaling.

Main Methods:

  • Review of existing literature on GPCR oligomerization.
  • Analysis of binding data using dimer-based models.
  • Exploration of intramolecular cross-talk within GPCR dimers and heterodimers.

Main Results:

  • GPCR dimers and oligomers are the primary targets for neurotransmitters and drugs.
  • Dimerization induces cooperativity in the binding of agonists, antagonists, and allosteric modulators.
  • Heterodimerization significantly alters signaling pathways and receptor trafficking, with potential for coactivation.

Conclusions:

  • GPCR dimers represent the functional units for drug and neurotransmitter interactions.
  • Understanding GPCR heteromerization is key to developing novel therapeutics.
  • Heterodimer-specific or dual-acting drugs offer promising avenues for central nervous system (CNS) disorders.