The Glucagon Receptor (GCGR), also known as glucagon-binding protein or GL-R, is a GPCR regulating glucose metabolism. Activated by glucagon, GCGR triggers gluconeogenesis and glycogenolysis, crucial for glucose homeostasis. It plays a vital role in metabolic disorders like obesity and type 2 diabetes.
GCGR signals through cAMP and β-arrestin pathways. The cAMP cascade promotes glucose release during fasting, while β-arrestin regulates receptor desensitization. Dysregulation of these pathways leads to insulin resistance, excess glucose, and lipid metabolism issues, making GCGR a key obesity research target.
Eurofins DiscoverX's cAMP Hunter™ GCGR Bioassay Kit provides a reliable cell-based assay to measure drug potency and detect neutralizing antibodies. From characterization to QC lot-release, it ensures GCGR-targeting compounds' quality and supports drug discovery for metabolic diseases.
In the cAMP Hunter GCGR Bioassay Kit, CHO-K1 cells overexpressing glucagon receptor (GCGR) utilize the natural coupling status of the GPCR to Gαs to monitor activation of the receptor. When GCGR is activated by glucagon, it stimulates adenylate cyclase, which in turn enables the production of cAMP. The resulting increase in cellular cAMP levels is measured using a homogenous, gain-of-signal competitive immunoassay based on Enzyme Fragment Complementation (EFC) technology.
The signal from the assay is directly proportional to the amount of cellular cAMP in the well, i.e., the higher the GCGR activation, the greater the cellular cAMP levels, and the larger the signal produced in the assay.