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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...
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...
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.

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Related Experiment Video

Updated: Jun 6, 2026

HSV-Mediated Transgene Expression of Chimeric Constructs to Study Behavioral Function of GPCR Heteromers in Mice
07:30

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

Published on: July 9, 2016

Exploring a role for heteromerization in GPCR signalling specificity.

Raphael Rozenfeld1, Lakshmi A Devi

  • 1Department of Pharmacology and Systems Therapeutics, Mount Sinai School of Medicine, New York, NY 10029, USA.

The Biochemical Journal
|December 17, 2010
PubMed
Summary
This summary is machine-generated.

G-protein-coupled receptors (GPCRs) are key drug targets. New research explores how GPCR heteromers, complexes of different GPCRs, offer unique signaling specificity for developing more targeted and effective therapies.

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HSV-Mediated Transgene Expression of Chimeric Constructs to Study Behavioral Function of GPCR Heteromers in Mice
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Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization
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Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization

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Visualizing the Conformational Dynamics of Membrane Receptors Using Single-Molecule FRET
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Published on: August 17, 2022

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Drug Discovery

Background:

  • G-protein-coupled receptors (GPCRs) are crucial for physiological processes and represent significant therapeutic targets.
  • Existing drugs targeting GPCRs are numerous, yet research continues to refine ligand design for improved efficacy.
  • GPCRs are located at the cell surface, mediating communication between the extracellular and intracellular environments.

Purpose of the Study:

  • To explore the phenomenon of 'ligand-directed signal specificity' for developing novel therapeutics.
  • To investigate the role of GPCR heteromers in modulating receptor signaling.
  • To establish GPCR heteromer targeting as a novel therapeutic strategy.

Main Methods:

  • Investigating GPCR pharmacology and ligand interactions.
  • Analyzing the formation and signaling properties of GPCR heteromers.
  • Examining disease-specific dysregulation involving GPCRs.

Main Results:

  • Ligand-directed signal specificity allows distinct downstream effects from the same GPCR.
  • GPCR heteromers exhibit unique signaling profiles, differing from individual receptors.
  • Heteromer-directed signaling specificity offers a mechanism for fine-tuning cellular responses.

Conclusions:

  • Targeting GPCR heteromers presents a promising strategy for achieving highly specific therapeutic effects.
  • Understanding heteromer-directed signaling specificity can lead to the development of drugs with improved efficacy and reduced side effects.
  • GPCR heteromers play significant roles in normal physiology and disease states.