GLP1R

GLP-1R, or glucagon-like peptide-1 receptor, alias GLP-1 recepto, GLP-1-R, GLP-1R, which belongs to the class B1 G protein-coupled receptor (GPCR), is an important receptor for regulating blood glucose levels in vivo, and is widely regarded as a therapeutic target for type 2 diabetes and obesity.GLP-1R agonists mimic the action of natural GLP-1 by enhances insulin secretion and inhibits glucagon secretion in a glucose concentration-dependent manner, and is able to delay gastric emptying, reduce food intake, and lower blood glucose.The signalling of GLP-1R is mainly achieved by coupling with a variety of G proteins (e.g., Gαs, Gαi, Gαo, and Gαq/11) to activate different intracellular signalling pathways, such as the cAMP/PKA pathway, which in turn increases glucose sensitivity and stimulate insulin secretion.

The biological significance of GLP-1R is mainly reflected in its contribution to the maintenance of glucose homeostasis. It not only plays a role in lowering blood glucose, but also has multiple effects such as weight loss, antihypertensive and improving lipid profile. In addition, the research and development of GLP-1R agonists has become a hotspot in the treatment of diabetes and obesity, with a huge and continuously growing global market. With the deeper understanding of the structure and function of GLP-1R, the design and development of novel agonists have been progressing, providing new ideas and hope for the treatment of related metabolic diseases.