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Development of Glucagon-like Peptide-1 Analogs and GLP-1 Receptor Agonists

  

  • Received:2011-01-26 Revised:2011-05-18 Published:2012-02-15 Online:2012-02-15

Abstract: Glucagon-like peptide-1(GLP-1) is a hormone secreted from enteroendocrine L cells of the intestine. Upon binding to its receptor, it results in many effects such as increasing insulin biosynthesis and secretion from β cells; suppressing glucagon secretion from α cells; enhancing islet neogenesis and proliferation of β cells; decreasing apoptosis of β cells; enhancing body sensibility to insulin and so on. However, GLP-1 is rapidly degraded by DPP IV enzyme and clearance in renal; the in vivo half-life is less than 2 min which limited the clinical utility of GLP-1 in type 2 diabetes. Many efforts were focused on finding the novel GLP-1 receptor agonist or GLP-1 analogs retaining the biological effects of GLP-1. This review summarized the physiological properties of GLP-1 and the ongoing development of GLP-1-based therapies for treatment of diabetes.

Key words: Type 2 diabetes, Glucagon-like peptide-1, GLP-1 receptor, Incretin, long-acting GLP-1R agonist