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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...
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 Receptors01:21

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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BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells
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GPR119 as a fat sensor.

Harald S Hansen1, Mette M Rosenkilde, Jens J Holst

  • 1Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, 2200 Copenhagen, Denmark. hsh@farma.ku.dk

Trends in Pharmacological Sciences
|May 8, 2012
PubMed
Summary

The G protein-coupled receptor 119 (GPR119) is a key target for diabetes drug development. Its activation by dietary fats, particularly 2-monoacylglycerol, stimulates insulin and GLP-1 release.

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Area of Science:

  • Biochemistry
  • Endocrinology
  • Pharmacology

Background:

  • G protein-coupled receptor 119 (GPR119) is primarily found in pancreatic beta cells and enteroendocrine cells.
  • GPR119 is a significant target for novel anti-diabetic medications, aiming to enhance insulin and GLP-1 secretion.
  • Endogenous lipids, including oleoylethanolamide and oleic acid derivatives, activate GPR119.

Purpose of the Study:

  • To investigate the role of GPR119 in mediating the effects of dietary fats on GLP-1 release.
  • To identify endogenous ligands that activate GPR119 and elucidate their mechanisms of action.
  • To understand the physiological significance of GPR119 activation for glucose homeostasis.

Main Methods:

  • Analysis of GPR119 expression in pancreatic and intestinal tissues.
  • Investigation of GPR119 activation by various endogenous lipids, including 2-monoacylglycerol.
  • Assessment of insulin and GLP-1 release in response to GPR119 agonists.

Main Results:

  • Dietary fat stimulation of GLP-1 release is significantly mediated by the luminal formation of 2-monoacylglycerol acting on GPR119.
  • GPR119 activation in pancreatic beta cells and enteroendocrine cells promotes insulin and GLP-1 secretion, respectively.
  • Endogenous lipids like N-oleoyl-dopamine and 1-oleoyl-lysophosphatidylcholine also activate GPR119.

Conclusions:

  • GPR119 acts as a 'fat sensor' in the gut, linking dietary fat intake to incretin hormone release.
  • Understanding GPR119's endogenous ligands and activation pathways is vital for developing next-generation anti-diabetic drugs.
  • Targeting GPR119 offers a promising therapeutic strategy for managing type 2 diabetes.