GCGR - Glucagon receptor | Elisa - Clia - Antibody - Protein

Background

The Glucagon Receptor Family includes several G protein-coupled receptors (GPCRs) that are activated by peptide hormones of the glucagon superfamily, such as glucagon, glucagon-like peptide 1 (GLP-1), and glucagon-like peptide 2 (GLP-2), GHRH Receptor, Secretin receptor and Glucagon receptor.The glucagon receptor was first identified in the 1970s, followed by the discovery of related receptors such as GLP-1 receptor and GLP-2 receptor in subsequent years. Glucagon receptor family members are expressed in various tissues including the pancreas, liver, gastrointestinal tract, brain, heart, and adipose tissue.

Structural Features:

 Members of the glucagon receptor family are seven-transmembrane domain receptors, typical of GPCRs. They consist of an extracellular N-terminus, seven transmembrane helices connected by intracellular and extracellular loops, and an intracellular C-terminus. Each receptor within the family has a specific binding site for its respective peptide ligand.

Glucagon Receptor:

The glucagon receptor is a G protein-coupled receptor primarily expressed in the liver, pancreas, and adipose tissue. It is activated by glucagon, a peptide hormone released from pancreatic α-cells in response to low blood glucose levels. Glucagon receptor activation stimulates hepatic glucose production, glycogenolysis, and lipolysis, raising blood glucose levels and providing energy during fasting and stress conditions.

Physiological Functions:

• Glucose Metabolism: The glucagon receptor regulates glucose homeostasis by promoting glycogenolysis, gluconeogenesis, and hepatic glucose output.
• Energy Homeostasis: GLP-1 and GLP-2 receptors play roles in the regulation of energy balance, appetite, and satiety, with GLP-1 promoting insulin secretion and GLP-2 promoting intestinal growth and nutrient absorption.
• Gastrointestinal Function: GLP-1 and GLP-2 receptors influence gastrointestinal motility, nutrient absorption, and gut hormone secretion.

Clinical Implications:

• Diabetes: Dysregulation of glucagon receptor signaling contributes to the pathogenesis of diabetes mellitus, with impaired glucagon action observed in type 2 diabetes.
• Obesity: GLP-1 receptor agonists are used as therapeutics for obesity and metabolic syndrome due to their effects on appetite suppression and weight loss.
• Gastrointestinal Disorders: GLP-2 receptor agonists have potential applications in the treatment of gastrointestinal disorders such as short bowel syndrome and inflammatory bowel disease.

Therapeutic Potential:

• Diabetes Therapies: Glucagon receptor antagonists and GLP-1 receptor agonists are utilized for the management of type 2 diabetes mellitus, either alone or in combination with other antidiabetic drugs.
• Obesity Treatments: GLP-1 receptor agonists are approved for the treatment of obesity and may be beneficial for weight management in obese individuals.
• Gastrointestinal Therapies: GLP-2 receptor agonists are being investigated for their potential to improve nutrient absorption and intestinal function in patients with gastrointestinal disorders.