Introduction of GCGR
The glucagon receptor (GCGR) is a 62 kDa protein that is activated by glucagon and is a member of the class B G-protein coupled family of receptors, coupled to G alpha i, Gs and to a lesser extent G alpha q. GCGR is encoded by the GCGR gene in humans. It was reported that stimulation of the receptor leads to activation of adenylate cyclase and improved levels of intracellular cAMP.
|Basic Information of GCGR|
|Protein Name||Glucagon receptor|
|Aliases||GGR, GL-R, glucagon receptor|
|Organism||Homo sapiens (Human)|
Function of GCGR Membrane Protein
Glucagon is a pancreatic peptide hormone that, as a counterregulatory hormone for insulin, stimulates glucose release through the liver and maintains glucose homeostasis. The GCGR is a Class B GPCR that first described as a glucagon binding entity functionally linked to adenylyl cyclase. It has a key role in maintenance of glucose homeostasis and, as such, is considered to be a valuable target for the treatment of diabetes. In the past years, considerable progress has been made in the identification of the molecular determinants of the GCGR that are important for ligand binding and signal transduction, in the development of glucagon analogs and of nonpeptide small molecules acting as receptor antagonists, and in the characterization of the mechanisms related to the regulation of expression of the glucagon receptor gene.
Fig.1 Two classical GCGR-mediated intracellular signal pathways in glucagon-targeted cells.
Application of GCGR Membrane Protein in Literature
This article reports that Glucagon secretory responses to propionate were not related to the prenatal nutrition history, but negatively affected by the postnatal obesogenic diet. The pancreatic α-cell compared to β-cells may thus be less sensitive towards late gestation malnutrition, whereas hepatic glucagon signaling appears to be a target of prenatal programming.
This article reveals that hyperglucagonemia in type 2 diabetes promotes colon cancer progression via GCGR-mediated regulation of AMPK and MAPK pathways.
The article reports that Compound 9r forms a broad hydrophobic interaction with the receptor binding pocket, making the possibility of a further investigation into GCGR antagonists reasonable.
This article shows that early in vertebrate evolution diverse regulatory mechanisms emerged for the control of glucose metabolism by proglucagon-derived peptides and their receptors and that in ray-finned fish they included subfunctionalization and neofunctionalization of these genes.
This article evaluates that they designed and synthesized a series of thiophene-containing biaryl glucagon receptor (GCGR) antagonists. The two compounds 14f and 14h of this series showed good GCGR binding and cAMP functional activity.
GCGR Preparation Options
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