Glucagon-Like Peptide 1 Receptor Agonists Small Molecules and Peptides

Glucagon-like peptide 1 (GLP-1) receptors are members of the glucagon receptor family that also includes glucagon, GLP-2, secretin, GHRH and GIP receptors. GLP-1 receptors are found both centrally (hypothalamus and brainstem) and peripherally (pancreatic islet cells, stomach and heart).

GLP-1 receptors mediate the effects of the incretin axis; the functional connection between the intestine and the islets of Langerhans in the pancreas. Activation stimulates insulin release from the islet β-cells in a glucose-dependent manner and suppresses glucagon secretion from islet α-cells. In addition, GLP-1 receptors delay gastric emptying and regulate appetite. The human GLP-1 receptor gene is localized on chromosome 6p21.