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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...
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...
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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Updated: May 25, 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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Published on: April 9, 2018

Characterization of CGRP receptor binding.

Alex C Conner1, Debbie L Hay, David R Poyner

  • 1Aston University, Aston Triangle, Birmingham, UK.

Current Protocols in Pharmacology
|February 2, 2012
PubMed
Summary
This summary is machine-generated.

This study presents a microcentrifugation assay for measuring Calcitonin Gene-Related Peptide (CGRP) receptor binding. The assay aids in determining ligand binding parameters and distinguishing CGRP receptors from related peptide receptors.

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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
16:16

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

Area of Science:

  • Pharmacology
  • Neuroscience
  • Biochemistry

Background:

  • Calcitonin Gene-Related Peptide (CGRP) receptors are crucial drug targets.
  • Accurate measurement of CGRP receptor binding is essential for drug discovery.
  • Existing assays face challenges like radioligand degradation and receptor expression variability.

Purpose of the Study:

  • To describe a novel microcentrifugation-based assay for quantifying CGRP receptor binding.
  • To detail protocols for using radioiodinated CGRP in displacement studies.
  • To provide a method for assessing ligand binding parameters at CGRP receptors.

Main Methods:

  • Utilized radioiodinated CGRP in displacement studies.
  • Employed a microcentrifugation-based assay with cell membrane homogenates.
  • Described a similar assay for intact cultured cells.
  • Adapted protocols for other radioligands and filtration-based assays.

Main Results:

  • The assay effectively determines binding parameters for ligands interacting with CGRP receptors.
  • Protocols were developed for both cell membrane homogenates and intact cells.
  • The method can be adapted for various radioligands and assay formats.
  • Identified radioligand degradation and receptor expression loss as key assay challenges.

Conclusions:

  • The described microcentrifugation assay offers a rapid and straightforward method for CGRP receptor binding studies.
  • This technique facilitates the characterization of novel CGRP receptor ligands.
  • The assay is valuable for differentiating CGRP receptors from those of related peptides like adrenomedullin and amylin.