Sitagliptin: Difference between revisions

<applet  load="" size="480" color="" frame="true"  spin="on" Scene ="Sitagliptin/Sitagliptin/1" align="right" caption="Sitagliptin, better known as Januvia, ([[1x70]])"/>

[[Diabetes|Type II Diabetes]] is a chronic metabolic disorder caused by pancrease β-cell dysfunction, deficiency in insulin secretion or insulin resistance, and/or increased hepatic glucose production. Numerous complex systems are involved in this disorder, with several protein serving as therapeutic targets. Dipeptidyl Peptidase-4 (DPP-4) is an antigenic membrane serine exopeptidase that cleaves proline dipeptides form the N-terminal end of protein substrates. DPP-4 plays a major role in [[glucose metabolism]] as it is responsible for the degradation of incretins, most notably Glucagon-like peptide-1 (GLP-1) and Glucose-dependent insulinotropic polypeptide (GIp). Incretins are a group of gastrointestinal hormones that stimulate insulin biosynthesis and inhibit glucagon secretion after consuming high glucose meals. Sitagliptin is a competitive inhibitor of DPP-4. By inhibiting DPP-4 and subsequently preventing the enzymatic degradation of GLP-1 and GIP, these incretins are able to potentiate the secretion of insulin and suppress the release of glucagon by the pancreas. The result is controlled blood-glucose levels, a major concern for [[Diabetes|diabetics]].