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Related Concept Videos

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.
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...
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of cells.
Two...
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...

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Related Experiment Video

Updated: Jul 26, 2026

Imaging G-protein Coupled Receptor (GPCR)-mediated Signaling Events that Control Chemotaxis of Dictyostelium Discoideum
09:40

Imaging G-protein Coupled Receptor (GPCR)-mediated Signaling Events that Control Chemotaxis of Dictyostelium Discoideum

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A G protein-coupled receptor for UDP-glucose.

J K Chambers1, L E Macdonald, H M Sarau

  • 1Department of Vascular Biology, New Frontiers Science Park, SmithKline Beecham Pharmaceuticals, Southern Way, Harlow, Essex CM19 5AW, United Kingdom. Jon_Chambers-1@sbphrd.com

The Journal of Biological Chemistry
|February 7, 2001
PubMed
Summary

Uridine 5'-diphosphoglucose (UDP-glucose) activates a novel G protein-coupled receptor, KIAA0001. This finding suggests sugar-nucleotides may function as extracellular signaling molecules in various human tissues, including the brain.

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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

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Last Updated: Jul 26, 2026

Imaging G-protein Coupled Receptor (GPCR)-mediated Signaling Events that Control Chemotaxis of Dictyostelium Discoideum
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Imaging G-protein Coupled Receptor (GPCR)-mediated Signaling Events that Control Chemotaxis of Dictyostelium Discoideum

Published on: September 20, 2011

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
10:13

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
07:41

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

Area of Science:

  • Biochemistry
  • Pharmacology
  • Cell Biology

Background:

  • Uridine 5 '-diphosphoglucose (UDP-glucose) is primarily known as a precursor in carbohydrate biosynthesis.
  • Emerging evidence suggests UDP-glucose may have uncharacterized pharmacological activities.
  • The existence of a potential receptor for UDP-glucose was hypothesized.

Purpose of the Study:

  • To identify and characterize the receptor for UDP-glucose.
  • To investigate the pharmacological properties of UDP-glucose and related molecules.
  • To determine the tissue distribution of the identified receptor.

Main Methods:

  • Heterologous expression of the orphan G protein-coupled receptor KIAA0001 in yeast and mammalian cells.
  • Ligand-binding and activation assays using UDP-glucose and related compounds.
  • Pharmacological profiling by testing known P2Y receptor agonists.
  • Quantitative analysis of receptor expression in various human tissues.

Main Results:

  • UDP-glucose and certain related molecules were found to be potent activators of KIAA0001.
  • Known P2Y receptor agonists did not activate KIAA0001, highlighting novel receptor pharmacology.
  • KIAA0001 expression was detected across a broad range of human tissues, including the brain.

Conclusions:

  • The orphan G protein-coupled receptor KIAA0001 is activated by UDP-glucose, identifying it as a potential UDP-glucose receptor.
  • This discovery reveals a novel class of extracellular signaling molecules and their receptors.
  • The widespread expression suggests significant physiological roles for sugar-nucleotides beyond intermediary metabolism.