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Updated: Aug 15, 2026

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
11:49

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

Published on: July 28, 2014

Identification of a novel extracellular cation-sensing G-protein-coupled receptor

Min Pi1, Pieter Faber, George Ekema

  • 1Kidney Institute, Department of Internal Medicine, University of Kansas Medical Center, Kansas City, Kansas 66160, USA.

The Journal of Biological Chemistry
|October 4, 2005
PubMed

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G Protein-coupled Receptors

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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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G-Protein Gated Ion Channels

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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.
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GPCRs Regulate Adenylyl Cylase Activity

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Activation and Inactivation of G Proteins

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