GLPR - Glucagon-Like Peptide 1 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-Like Peptide-1 Receptor (GLP-1 Receptor):

The GLP-1 receptor, also known as GLP-1R, is a G protein-coupled receptor primarily expressed in pancreatic β-cells, gastrointestinal tract, and central nervous system. It is activated by glucagon-like peptide 1 (GLP-1), an incretin hormone released from intestinal L cells in response to nutrient intake. GLP-1 receptor activation enhances glucose-dependent insulin secretion, suppresses glucagon release, slows gastric emptying, and promotes satiety, making it a target for diabetes and obesity treatments.

Glucagon-Like Peptide-2 Receptor (GLP-2 Receptor):

The GLP-2 receptor, also known as GLP-2R, is a G protein-coupled receptor primarily expressed in the gastrointestinal tract and central nervous system. It is activated by glucagon-like peptide 2 (GLP-2), a peptide hormone released from intestinal L cells in response to nutrient ingestion. GLP-2 receptor activation promotes intestinal growth, nutrient absorption, and mucosal integrity, making it a potential therapeutic target for gastrointestinal disorders such as short bowel syndrome.

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.