Glucagon-like peptide-1 receptor: Difference between revisions

Latest revision as of 16:34, 16 February 2025

Glucagon-like peptide-1 receptor[edit]

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[edit]

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[edit]

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[edit]

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[edit]

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-'''Glucagon-like peptide-1 receptor''' ('''GLP-1R''') is a [[G protein-coupled receptor]] that binds [[glucagon-like peptide-1]] (GLP-1), a hormone involved in the regulation of [[blood glucose]] levels. The receptor is expressed in various tissues, including the [[pancreas]], [[brain]], and [[heart]], and plays a crucial role in glucose homeostasis and cardiovascular function.
+== Glucagon-like peptide-1 receptor ==
+[[File:GLP-1R_complex.png|thumb|right|300px|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 ==
-The GLP-1R is a member of the class B1 family of G protein-coupled receptors. It is a transmembrane protein composed of seven alpha-helical segments connected by three extracellular and three intracellular loops. The N-terminal domain of the receptor is responsible for ligand binding, while the C-terminal domain is involved in receptor activation and signal transduction.
+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 ==
-Upon binding of GLP-1, the GLP-1R activates the [[adenylate cyclase]] enzyme, leading to an increase in the intracellular concentration of [[cyclic AMP]] (cAMP). This, in turn, activates protein kinase A (PKA) and exchange protein directly activated by cAMP (EPAC), which mediate the downstream effects of GLP-1R activation.
-In the pancreas, GLP-1R activation stimulates insulin secretion from beta cells in a glucose-dependent manner. In the brain, it promotes satiety and reduces food intake. In the heart, it improves cardiac function and protects against ischemic injury.
+The primary function of GLP-1R is to mediate the effects of GLP-1, which include:
-== Clinical significance ==
+* Enhancing glucose-dependent insulin secretion from pancreatic beta cells.
-GLP-1R is a target for the treatment of type 2 diabetes. GLP-1R agonists, such as [[exenatide]] and [[liraglutide]], are used to increase insulin secretion, suppress glucagon release, and reduce appetite. These drugs have been shown to improve glycemic control and promote weight loss in patients with type 2 diabetes.
+* Inhibiting glucagon release from pancreatic alpha cells.
+* Slowing gastric emptying to regulate postprandial glucose levels.
+* Promoting satiety and reducing food intake.
-In addition, research is ongoing to explore the potential benefits of GLP-1R activation in the treatment of neurodegenerative diseases, such as [[Alzheimer's disease]] and [[Parkinson's disease]], and cardiovascular diseases.
+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 ==
-== See also ==
 * [[Glucagon-like peptide-1]]
+* [[Insulin]]
+* [[Type 2 diabetes mellitus]]
 * [[G protein-coupled receptor]]
-* [[Type 2 diabetes]]
-[[Category:G protein-coupled receptors]]
+{{Receptor-stub}}
-[[Category:Peptide hormone receptors]]
+[[Category:Receptors]]
 [[Category:Diabetes]]
-{{GPCR-stub}}
+[[Category:Endocrinology]]
-{{diabetes-stub}}
-{{medicine-stub}}