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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.
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...
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...
GPCR Desensitization01:12

GPCR Desensitization

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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Related Experiment Video

Updated: May 16, 2026

Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells
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Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells

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GPCR oligomerization: contribution to receptor biogenesis.

Kathleen Van Craenenbroeck1

  • 1Laboratory of Eukaryotic Gene Expression and Signal Transduction (LEGEST), Ghent University-UGent, K.L. Ledeganckstraat 35, 9000, Ghent, Belgium, Kathleen.VanCraenenbroeck@UGent.be.

Sub-Cellular Biochemistry
|November 20, 2012
PubMed
Summary

G protein-coupled receptor (GPCR) biogenesis involves strict regulation, including chaperone interactions and oligomerization in the endoplasmic reticulum, ensuring proper protein folding and cell surface expression.

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Last Updated: May 16, 2026

Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells
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Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells

Published on: April 9, 2018

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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HSV-Mediated Transgene Expression of Chimeric Constructs to Study Behavioral Function of GPCR Heteromers in Mice
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HSV-Mediated Transgene Expression of Chimeric Constructs to Study Behavioral Function of GPCR Heteromers in Mice

Published on: July 9, 2016

Area of Science:

  • Molecular Biology
  • Cell Biology
  • Biochemistry

Background:

  • G protein-coupled receptors (GPCRs) are typically thought to use the default secretory pathway.
  • Recent findings suggest GPCR trafficking is tightly regulated.
  • Interactions with endoplasmic reticulum (ER) chaperones are crucial for proper folding.

Purpose of the Study:

  • To review the critical role of GPCR oligomerization in receptor biogenesis.
  • To highlight the regulatory mechanisms governing GPCR trafficking from the ER.

Main Methods:

  • This review synthesizes existing literature on GPCR trafficking and biogenesis.
  • Focuses on the structural assembly of GPCRs within the ER.

Main Results:

  • GPCR folding and ER export are regulated by specific protein interactions, including chaperones.
  • GPCRs can assemble into quaternary structures within the ER.
  • This oligomerization is essential for correct receptor expression at the cell surface.

Conclusions:

  • GPCR biogenesis is a highly regulated process, not simply a default pathway.
  • Oligomerization within the ER is a key step for ensuring functional GPCRs reach the plasma membrane.