Biological ActivityExendin-4 is a high affinity glucagon-like peptide 1 (GLP-1) receptor agonist (Kd = 136 pM); originally isolated from Heloderma suspectum venom. Exendin-4 potently induces cAMP formation without stimulating amylase release in pancreatic acini. Potentiates glucose-induced insulin secretion in isolated rat islets. Exendin-4 protects against glutamate-induced neurotoxicity, and in a mouse model of metabolic imblance it reduces neuroinflammation and enhances long-term-potentiation.
(Modifications: Ser-39 = C-terminal amide)
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Protection and reversal of excitotoxic neuronal damage by glucagon-like peptide-1 and exendin-4.
Perry et al.
Exendin-4 is a high potency agonist and truncated exendin-(9-39)-amide an antagonist at the glucagon-like peptide 1-(7-36)-amide receptor of Ins-Secr.g β-cells.
Goke et al.
Cloning and functional expression of the human islet GLP-1 receptor. Demonstration that exendin-4 is an agonist and exendin-(9-39) an antagonist of the receptor.
Thorens et al.
Isolation and characterization of exendin-4, an exendin-3 analogue, from Heloderma suspectum venom.
Eng et al.
Citations for Exendin-4
The citations listed below are publications that use Tocris products. Selected citations for Exendin-4 include:
8 Citations: Showing 1 - 8
Mitochondrial GTP Links Nutrient Sensing to β Cell Health, Mitochondrial Morphology, and Ins. Secretion Independent of OxPhos.
Authors: Jesinkey Et al.
Cell Rep 2019;28:759
Glucagon-like peptide-1 receptors within the nucleus of the solitary tract regulate alcohol-mediated behaviors in rodents.
Authors: Vallof Et al.
Crystal structure of the GLP-1 receptor bound to a peptide agonist.
GLP-1 acts on habenular avoidance circuits to control nicotine intake.
Nat Neurosci 2017;20(5):708
Novel and ultra-rare damaging variants in neuropeptide signaling are associated with disordered eating behaviors.
PLoS One 2017;12(8):e0181556
Gastrin: a distinct fate of neurogenin3 positive progenitor cells in the embryonic pancreas.
Authors: Suissa Et al.
ACS Chem Biol 2013;8:e70397
Glucagon-like peptide-1 protects against cardiac microvascular injury in diabetes via a cAMP/PKA/Rho-dependent mechanism.
Authors: Wang Et al.
PLoS One 2013;62:1697
Glucagon-like peptide-1 regulation of carbohydrate intake is differentially affected by obesogenic diets.
Authors: Pritchett and Hajnal
Obesity (Silver Spring) 2012;20:313
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