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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...
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.
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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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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GPR55 ligands promote receptor coupling to multiple signalling pathways.

Christopher M Henstridge1, Nariman Ab Balenga, Ralf Schröder

  • 1Division of Medical Sciences, Ninewells Hospital and Medical School, University of Dundee, Dundee, UK.

British Journal of Pharmacology
|February 9, 2010
PubMed
Summary

This study clarifies how cannabinoid ligands interact with G protein-coupled receptor 55 (GPR55). Findings reveal assay-dependent differences in ligand potency and efficacy, impacting GPR55 signaling.

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Area of Science:

  • Pharmacology
  • Cellular Signaling
  • Receptor Biology

Background:

  • G protein-coupled receptor 55 (GPR55) is activated by lysophosphatidylinositol (LPI) and potentially by cannabinoid ligands.
  • Cannabinoid receptor 1 (CB1) antagonists like AM251 and SR141716A have been suggested to interact with GPR55.
  • Understanding GPR55 pharmacology is crucial due to its role in various physiological processes.

Purpose of the Study:

  • To compare the pharmacological activity of selected cannabinoid ligands (AM251, AM281, SR141716A) with LPI at human GPR55.
  • To investigate the downstream signaling events triggered by GPR55 activation.
  • To evaluate a novel label-free assay for assessing GPR55 ligand activity.

Main Methods:

  • Functional assays including calcium (Ca2+) signaling and extracellular signal-regulated kinase (ERK1/2) activation.
  • Assessment of transcriptional regulators: nuclear factor of activated T cells (NFAT), nuclear factor-kappaB (NF-kappaB), and cAMP response element binding protein (CREB).
  • Measurement of receptor endocytosis and utilization of a dynamic mass redistribution assay.

Main Results:

  • GPR55 activation leads to diverse downstream signaling pathways.
  • The potency and efficacy of GPR55 ligands varied significantly depending on the functional assay used.
  • Differences in effector coupling were observed for distinct GPR55 ligands.

Conclusions:

  • The study resolves ambiguities regarding cannabinoid ligand pharmacology at GPR55.
  • Distinct GPR55 ligands exhibit unique effector coupling mechanisms.
  • These findings contribute to a better understanding of GPR55 signaling pathways.