Glucagon-like peptide-1 receptor

Glucagon-like peptide-1 receptor

Structure of the GLP-1 receptor complex.

The glucagon-like peptide-1 receptor (GLP-1R) is a G protein-coupled receptor (GPCR) that plays a crucial role in the regulation of glucose metabolism and insulin secretion. It is primarily expressed in the pancreatic beta cells, but is also found in the central nervous system, heart, and gastrointestinal tract.

Structure

GLP-1R is a member of the class B family of GPCRs. It consists of a large extracellular domain, seven transmembrane helices, and an intracellular domain. The receptor is activated by the binding of its endogenous ligand, glucagon-like peptide-1 (GLP-1), which is an incretin hormone.

Function

The primary function of GLP-1R is to mediate the effects of GLP-1, which include:

• Enhancing glucose-dependent insulin secretion from pancreatic beta cells.
• Inhibiting glucagon release from pancreatic alpha cells.
• Slowing gastric emptying to regulate postprandial glucose levels.
• Promoting satiety and reducing food intake.

These actions make GLP-1R a critical target for the treatment of type 2 diabetes mellitus.

Clinical Significance

GLP-1R agonists, such as exenatide and liraglutide, are used as therapeutic agents in the management of type 2 diabetes. These drugs mimic the action of GLP-1, leading to improved glycemic control and weight loss in patients.

Related pages

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

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