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Related Concept Videos

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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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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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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Updated: Sep 2, 2025

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
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Probing GPCR Dimerization Using Peptides.

Zara Farooq1,2, Lesley A Howell2, Peter J McCormick1

  • 1Centre for Endocrinology, William Harvey Research Institute, Bart's and The London School of Medicine and Dentistry, Queen Mary University of London, Charterhouse Square, London, United Kingdom.

Frontiers in Endocrinology
|August 1, 2022
PubMed
Summary
This summary is machine-generated.

G protein-coupled receptors (GPCRs) form dimers and oligomers, influencing drug responses and diseases. Targeting these GPCR complexes presents challenges but offers future therapeutic potential.

Keywords:
GPCR (G protein coupled receptor)oligomerpeptidespharmacologyprotein-protein interactiontherapeutics targets

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Structural Biology

Background:

  • G protein-coupled receptors (GPCRs) are a major class of membrane proteins and key drug targets.
  • GPCRs form dimers and oligomers, impacting receptor function and disease.
  • GPCR oligomerization is increasingly recognized for its role in diseases like cancer and neurological disorders.

Purpose of the Study:

  • To review physiologically relevant GPCR dimers.
  • To discuss strategies for targeting GPCR-GPCR interactions.
  • To explore future directions in GPCR complex research.

Main Methods:

  • Literature review of GPCR oligomerization studies.
  • Analysis of techniques for targeting protein-protein interactions (PPIs).
  • Discussion of challenges in GPCR complex structural biology.

Main Results:

  • Evidence supports GPCRs existing and functioning as dimers and higher-order oligomers.
  • GPCR oligomers modulate pharmacological responses, impacting disease.
  • Targeting GPCR oligomers is challenging due to PPIs and lack of structural data.

Conclusions:

  • GPCR oligomers are critical in disease and represent a potential therapeutic avenue.
  • Developing strategies to target GPCR complexes is essential.
  • Future research should focus on structural insights and novel targeting techniques for GPCR oligomers.