Overview
- Peptide CDMLK IASVHSQHIR, corresponding to amino acid residues 186-200 of rat GPR119 (Accession Q7TQN8). 2nd intracellular loop.
- Rat pancreas and mouse pancreas MS1 cells (1:400-1:1200).
Western blot analysis of rat pancreas (lanes 1 and 3) and mouse MS1 cells (lanes 2 and 4):1,2. Anti-GPR119 Antibody (#AGR-032), (1:400).
3,4. Anti-GPR119 Antibody, preincubated with GPR119 Blocking Peptide (#BLP-GR032).
Glucose-dependent insulinotropic receptor (GPR119) is a rhodopsin-type member of the G protein-coupled receptor (GPCRs) superfamily. Like all members, it has seven transmembrane spanning domains, an extracellular N-terminus and intracellular C-terminus. Activation of the receptor leads to a rise in intracellular cAMP – suggesting a stimulation of adenylate cyclase, possibly by Gαs coupling. It is expressed mostly in enteroendocrine cells of the gastrointenstinal tract and b-cells of the pancreas. It was stipulated that GPR119 is a close relative to the cannabinoid receptors1,2.
Phospholipids and fatty acid amides are endogenous ligands for GPR119. Notably, oleoethanolamide (OEA) seems to be an important agonist. Stimulation of GPR119 by its agonists causes b-cells to release insulin and enteroendocrine cells to release glucagon-like peptide-1 (GLP-1); this attribute makes GPR119 a strong therapeutic candidate for type-2 diabetes and obesity3,4. Furthermore, its ability to release GLP-1 upon stimulation by dietary fat has gained it the title "fat sensor"5 .
