PMID- 21966329 OWN - NLM STAT- PubMed-not-MEDLINE DCOM- 20111110 LR - 20211020 IS - 1874-1045 (Electronic) IS - 1874-1045 (Linking) VI - 5 IP - Suppl 2 DP - 2011 TI - Medicinal Chemistry and Applications of Incretins and DPP-4 Inhibitors in the Treatment of Type 2 Diabetes Mellitus. PG - 82-92 LID - 10.2174/1874104501105010082 [doi] AB - Diabetes mellitus (DM) is a major metabolic disorder currently affecting over 200 million people worldwide. Approximately 90% of all diabetic patients suffer from Type 2 diabetes mellitus (T2DM). The world's economy coughs out billions of dollars annually to diagnose, treat and manage patients with diabetes. It has been shown that the naturally occurring gut hormones incretins, glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) can preserve the morphology and function of pancreatic beta cell. In addition, GIP and GLP-1 act on insulin receptors to facilitate insulin-receptor binding, resulting in optimal glucose metabolism. This review examines the medicinal chemistry and roles of incretins, specifically, GLP-1 and drugs which can mimic its actions and prevent its enzymatic degradation. The review discussed GLP-1 agonists such as exenatide, liraglutide, taspoglutide and albiglutide. The paper also identified and reviewed a number of inhibitors, which can block dipeptidyl peptidase 4 (DPP-4), the enzyme responsible for the rapid degradation of GLP-1. These DPP-4 inhibitors include sitagliptin, saxagliptin, vildagliptin and many others which are still in the experimental phase. FAU - Lotfy, Mohamed AU - Lotfy M AD - Department of Biology, Faculty of Science, UAE University. FAU - Singh, Jaipaul AU - Singh J FAU - Kalasz, Huba AU - Kalasz H FAU - Tekes, Kornelia AU - Tekes K FAU - Adeghate, Ernest AU - Adeghate E LA - eng PT - Journal Article DEP - 20110909 PL - United Arab Emirates TA - Open Med Chem J JT - The open medicinal chemistry journal JID - 101507899 PMC - PMC3174521 OTO - NOTNLM OT - DPP-4 inhibitors OT - Incretins OT - medicinal chemistry. OT - type 2 diabetes EDAT- 2011/10/04 06:00 MHDA- 2011/10/04 06:01 PMCR- 2011/09/09 CRDT- 2011/10/04 06:00 PHST- 2011/02/12 00:00 [received] PHST- 2011/03/27 00:00 [revised] PHST- 2011/03/30 00:00 [accepted] PHST- 2011/10/04 06:00 [entrez] PHST- 2011/10/04 06:00 [pubmed] PHST- 2011/10/04 06:01 [medline] PHST- 2011/09/09 00:00 [pmc-release] AID - TOMCJ-5-82 [pii] AID - 10.2174/1874104501105010082 [doi] PST - ppublish SO - Open Med Chem J. 2011;5(Suppl 2):82-92. doi: 10.2174/1874104501105010082. Epub 2011 Sep 9.