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Related Concept Videos

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 Receptors01:15

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...
Dose-Response Relationship: Selectivity and Specificity01:25

Dose-Response Relationship: Selectivity and Specificity

Drugs exert their therapeutic effects by interacting with receptors, enzymes, or ion channels that are present throughout the human body. The strength and duration of the interaction between a drug and its target receptor are characterized by the selectivity and specificity of the drug. Selectivity refers to a drug's strong preference for its intended target over other targets. For instance, isoprenaline, a non-selective β-adrenergic agonist, interacts with both β1- and β2-adrenergic receptors...
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: May 21, 2026

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

Functional selectivity in GPCR heterocomplexes.

J González-Maeso1, S C Sealfon

  • 1Department Psychiatry, Mount Sinai School of Medicine, New York, New York, USA.

Mini Reviews in Medicinal Chemistry
|June 12, 2012
PubMed
Summary
This summary is machine-generated.

G protein-coupled receptors (GPCRs) can activate multiple pathways. Different drug molecules stabilize distinct receptor shapes, leading to varied signaling outcomes, a concept known as functional selectivity.

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Comparing the Affinity of GTPase-binding Proteins using Competition Assays
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Last Updated: May 21, 2026

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

Comparing the Affinity of GTPase-binding Proteins using Competition Assays
10:37

Comparing the Affinity of GTPase-binding Proteins using Competition Assays

Published on: October 8, 2015

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
08:21

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Published on: June 28, 2019

Area of Science:

  • Pharmacology
  • Biophysics
  • Molecular Biology

Background:

  • G protein-coupled receptors (GPCRs) are key drug targets capable of activating multiple intracellular signaling pathways.
  • GPCRs can adopt various active conformations, influencing their signaling bias.
  • Functional selectivity describes an agonist's ability to preferentially activate specific pathways linked to a single receptor.

Purpose of the Study:

  • To explore the phenomenon of functional selectivity in G protein-coupled receptors (GPCRs).
  • To investigate the role of GPCR heterocomplexes in mediating functional selectivity.
  • To understand how different agonists stabilize distinct GPCR active conformations.

Main Methods:

  • Biophysical studies to characterize receptor conformations.
  • Pharmacological assays to measure pathway activation.
  • In vitro and in vivo studies of GPCR heterocomplex formation.

Main Results:

  • Agonists stabilize specific GPCR active conformations, leading to differential pathway activation.
  • GPCRs form heterocomplexes, which may influence functional selectivity.
  • Evidence suggests GPCR heterocomplexes play a role in drug responses.

Conclusions:

  • Functional selectivity is a crucial concept in understanding GPCR signaling.
  • GPCR heterocomplexes represent a novel mechanism potentially involved in functional selectivity.
  • Further research into GPCR conformation and heterocomplexes is warranted for drug development.