GLP1R

GLP1R

GLP1R (Glucagon-Like Peptide-1 Receptor) is a protein that in humans is encoded by the GLP1R gene. This receptor is a member of the G protein-coupled receptor family and plays a crucial role in the regulation of glucose metabolism and insulin secretion.

Function

GLP1R is primarily expressed in the pancreas, particularly in the beta cells of the islets of Langerhans. It is activated by the glucagon-like peptide-1 (GLP-1), an incretin hormone that enhances the secretion of insulin in response to food intake. The activation of GLP1R leads to an increase in intracellular cyclic AMP (cAMP) levels, which in turn promotes insulin release. This receptor also has effects on gastric emptying, appetite regulation, and cardiovascular function.

Clinical Significance

GLP1R is a target for the treatment of type 2 diabetes mellitus. Agonists of GLP1R, such as exenatide and liraglutide, are used to improve glycemic control in diabetic patients. These drugs mimic the action of GLP-1, leading to increased insulin secretion, decreased glucagon release, and slowed gastric emptying.

Structure

The GLP1R protein consists of 463 amino acids and has seven transmembrane domains, characteristic of G protein-coupled receptors. The receptor undergoes conformational changes upon binding to GLP-1, which facilitates the activation of downstream signaling pathways.

Research

Ongoing research is focused on developing new GLP1R agonists with improved efficacy and safety profiles. Additionally, studies are being conducted to understand the role of GLP1R in other physiological processes and its potential therapeutic applications beyond diabetes, such as in obesity and cardiovascular disease.

See Also

• G protein-coupled receptor
• Glucagon-like peptide-1
• Insulin
• Type 2 diabetes mellitus
• Exenatide
• Liraglutide