Related Experiment Video
Updated: Jun 10, 2026
07:41
A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
G protein-coupled receptor oligomerization for what?
Francisco Ciruela1, Antoni Vallano, Josep M Arnau
1Unitat de Farmacologia, Departament de Patologia i Terapèutica Experimental, Facultat de Medicina, IDIBELL-Universitat de Barcelona, 08907 Barcelona, Spain. fciruela@ub.edu
Journal of Receptor and Signal Transduction Research
|August 20, 2010
Summary
G protein-coupled receptor (GPCR) oligomerization is increasingly accepted, enhancing signal transduction. This review explores how GPCR oligomers influence receptor function, from biosynthesis to signaling, potentially enabling complex signal processing.
Area of Science:
- Biochemistry
- Cell Biology
- Molecular Pharmacology
Background:
- G protein-coupled receptor (GPCR) oligomerization, once debated, is now widely accepted.
- GPCR oligomers are proposed to enhance the diversity and efficiency of extracellular signal transduction to G proteins.
- The precise mechanisms underlying GPCR oligomeric function remain largely unexplained.
Purpose of the Study:
- To revise the impact of GPCR oligomerization on key receptor functions.
- To discuss the proposed trans-conformational switching model for GPCR activation inhibition.
- To explore the role of heterotropic receptor-receptor allosteric regulations in GPCR function.
Main Methods:
- Literature review and synthesis of existing research on GPCR oligomerization.
- Analysis of proposed models for GPCR oligomer function.
- Discussion of experimental evidence supporting GPCR oligomerization's role in cellular processes.
Main Results:
- GPCR oligomerization influences receptor biosynthesis, plasma membrane diffusion, and velocity.
- Oligomerization impacts receptor pharmacology and signaling pathways.
- A trans-conformational switching model offers a potential mechanism for inhibiting receptor activation via allosteric regulation.
Conclusions:
- GPCR oligomerization is crucial for sophisticated cellular sensing and signal processing.
- Understanding GPCR oligomerization provides insights into receptor function and drug development.
- The supramolecular organization of GPCRs is essential for translating complex extracellular signals into cellular responses.
Related Concept Videos
01:21G-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.
01:21G-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.
01:15G 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...
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...
01:15G 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...
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...
01:30Transducer 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...
GPCRs are also called heptahelical, 7TM, or...
01:22Activation 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...