The development of non-peptide glucagon-like peptide-1 receptor agonist for the treatment of type 2 diabetes

Arch Pharm Res. 2011 Jul;34(7):1041-3. doi: 10.1007/s12272-011-0721-z.

Abstract

Glucagon-like peptide-1 (GLP-1) is the main member of the incretin family and stimulates insulin secretion by binding with its specific receptor on pancreatic β-cells. In addition, GLP-1 exerts broad beneficial effects on the glucose regulation by suppressing food intake and delaying stomach emptying. Now, long acting GLP-1 analogs including exenatide and liraglutide have been approved for the treatment of diabetes mellitus type 2, however long-term injection can limit their use for these chronic patients. In this report, the authors provide a review on the development of non-peptide GLP-1 receptor agonists and introduce a novel agonist DA-15864.

Publication types

  • Review

MeSH terms

  • Animals
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Drug Design
  • Glucagon-Like Peptide 1 / analogs & derivatives
  • Glucagon-Like Peptide 1 / metabolism
  • Glucagon-Like Peptide 1 / pharmacology*
  • Glucagon-Like Peptide 1 / therapeutic use
  • Glucagon-Like Peptide-1 Receptor
  • Humans
  • Hypoglycemic Agents / pharmacology*
  • Hypoglycemic Agents / therapeutic use
  • Insulin / biosynthesis
  • Insulin-Secreting Cells / drug effects*
  • Insulin-Secreting Cells / physiology
  • Molecular Targeted Therapy*
  • Rats
  • Receptors, Glucagon / agonists*
  • Receptors, Glucagon / metabolism

Substances

  • GLP1R protein, human
  • Glp1r protein, rat
  • Glucagon-Like Peptide-1 Receptor
  • Hypoglycemic Agents
  • Insulin
  • Receptors, Glucagon
  • Glucagon-Like Peptide 1