Glucagon-like peptide-1 (GLP-1) analogs: recent advances, new possibilities, and therapeutic implications

J Med Chem. 2015 Feb 12;58(3):1020-37. doi: 10.1021/jm500810s. Epub 2014 Nov 13.


Glucagon-like peptide-1 (GLP-1) is an incretin that plays important physiological roles in glucose homeostasis. Produced from intestine upon food intake, it stimulates insulin secretion and keeps pancreatic β-cells healthy and proliferating. Because of these beneficial effects, it has attracted a great deal of attention in the past decade, and an entirely new line of diabetic therapeutics has emerged based on the peptide. In addition to the therapeutic applications, GLP-1 analogs have demonstrated a potential in molecular imaging of pancreatic β-cells; this may be useful in early detection of the disease and evaluation of therapeutic interventions, including islet transplantation. In this Perspective, we focus on GLP-1 analogs for their studies on improvement of biological activities, enhancement of metabolic stability, investigation of receptor interaction, and visualization of the pancreatic islets.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Diabetes Mellitus / drug therapy
  • Diabetes Mellitus / metabolism
  • Glucagon-Like Peptide 1* / metabolism
  • Glucagon-Like Peptide 1* / therapeutic use
  • Humans
  • Insulin-Secreting Cells / metabolism
  • Molecular Imaging


  • Glucagon-Like Peptide 1