GCG Inhibitors

GCG, commonly referred to as glucagon, is a 29-amino acid peptide hormone produced in the alpha cells of the pancreatic islets. It plays a pivotal role in glucose metabolism and homeostasis, especially in conditions when blood glucose levels drop. When blood glucose levels decrease, GCG is released into the bloodstream, instigating a series of physiological responses aimed at raising blood glucose levels. Its primary action is to stimulate hepatic glucose production by promoting glycogenolysis, wherein stored glycogen in the liver is broken down to release glucose. Additionally, GCG promotes gluconeogenesis, a metabolic pathway that results in the generation of glucose from certain non-carbohydrate substrates.

Besides its role in glucose metabolism, GCG has effects on lipid metabolism, including the stimulation of lipolysis in adipose tissue, leading to the release of free fatty acids into the bloodstream. GCG inhibitors are chemical compounds designed to modulate the activity of glucagon. These inhibitors can interfere with the binding of GCG to its receptor, the glucagon receptor, or disrupt downstream signaling events post-receptor binding. By inhibiting the action of GCG, these compounds can modulate the metabolic processes that GCG regulates.