Introduction of GPR119
The GPR119 receptor is a member of the G-protein-coupled receptor superfamily. It is a type A rhodopsin isolated G protein-coupled receptor that has seven transmembrane regions in its structure. GPR119 is coupled to G protein in the cytoplasm by G protein 3 subunits (α, β, γ). The GPCR peptide consists of seven transmembrane alpha helices at the N-terminus, three extracellular loops at the C-terminus, and three to four intracellular loops at the C-terminus. The N-terminus is extracellular and is often glycosylated; the C-terminus is intracellular and most likely phosphorylates; seven transmembrane alpha helices repeatedly cross the lipid bilayer of the cell membrane. In humans, GPR119 is mainly distributed on the surface of pancreatic β cells, liver and gastrointestinal endocrine cells.
|Basic Information of GPR119|
|Protein Name||Glucose-dependent insulinotropic receptor|
|Aliases||GPCR2, G protein-coupled receptor 119|
|Organism||Homo sapiens (Human)|
Function of GPR119 Membrane Protein
GPR119 can combine with Oleylethanolamide (OEA), Monoglyceride (2OG) and Cannabinoids, promote GLP-1 and GIP levels in vivo, proliferate islet beta cells, promote insulin secretion, reduce appetite, delay gastric row empty, so that glucose-dependent stimulation of insulin release increased, lowering blood sugar while suppressing appetite and weight loss. Studies have shown that the G protein is adsorbed on the inner surface of the cell membrane. When the agonist binds with GPR119, the protein stimulates the protein to increase the intracellular cyclic adenosine monophosphate concentration and stimulate intracellular stimulation-secretion coupling, thereby increasing hormone secretion.
Fig.1 The structure of GPR119 membrane protein.
Application of GPR119 in Literature
This article reports that GPR119 is a receptor for Oleoyl-LPI, upstream of ERK1/2 and cAMP/PKA/CREB pathways, and that Oleoyl-LPI can mediate GLP-1 secretion via GPR119.
This article reveals that GPR119 agonists have the ability to pharmacologically augment glucagon secretion, particularly in response to hypoglycemia in diabetic rodents.
The article evaluates the safety and pharmacokinetics of DS-8500a (GPR119 agonist) in healthy adult Japanese male subjects under fed conditions.
This article reports that they have found some novel spirocyclohexane derivatives by exploring alternative structures for the characteristically substituted piperidine or piperazine rings in GPR119 agonists.
This article shows that DS-8500a has a significant effect on glucose reduction in Japanese T2DM patients with a therapeutic effect of up to 12 weeks and is well tolerated.
GPR119 Preparation Options
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