GPR119 Agonists for the Potential Treatment of Type 2 Diabetes and Related Metabolic Disorders

摘要: Type 2 diabetes (T2D) has reached epidemic proportions, and there is an unmet medical need for orally effective agents that regulate glucose homeostasis. GPR119, a class-A (rhodopsin-like) G protein-coupled receptor expressed primarily in the pancreas gastrointestinal tract, attracted considerable interest as T2D drug target recent years. The activation of GPR119 increases intracellular accumulation cAMP, leading to enhanced glucose-dependent insulin secretion from pancreatic β-cells increased release gut peptides GLP-1 (glucagon-like peptide 1), GIP (glucose-dependent insulinotropic peptide) PYY (polypeptide YY). Oral administration small molecule agonists been shown improve tolerance both rodents humans. This review summarizes research identification potential related metabolic disorders, provides overview progress made discovery active agonists.