Technical Articles

The glucagon receptor (GCGR) is a crucial member of the class B G protein-coupled receptor family, forming a core receptor network with GLP-1R and GIPR to regulate glucose homeostasis and energy metabolism. The endogenous ligand of GCGR is glucagon, primarily secreted by pancreatic α-cells, which plays a pivotal role in maintaining fasting blood glucose levels, promoting lipid oxidation, and increasing energy expenditure.

Glucagon-like peptide-1 receptor (GLP-1R) agonists have revolutionized the treatment of type 2 diabetes and obesity over the past decade. However, the efficacy ceiling of single-target drugs and gastrointestinal tolerance issues have prompted researchers to explore more complex multi-target synergistic strategies.

Glucagon receptor (GCGR), as an important member of the B-type G protein-coupled receptor (GPCR) family, plays a key role in maintaining blood glucose homeostasis, lipid metabolism and energy balance. It regulates liver glycogenolysis and gluconeogenesis by recognizing and responding to glucagon signals, and has become the focus of research on diabetes, obesity and related metabolic diseases.