WARF: P130310US02

Non-Natural Peptides for Treating Diabetes


Samuel Gellman, Lisa Johnson, Alan Attie, Alan Saghatelian, Mark Keller

The Wisconsin Alumni Research Foundation (WARF) is seeking commercial partners interested in developing peptide analogs of GLP-1 with prolonged effects in vivo.
OVERVIEWDiabetes mellitus continues to be a chronic public health issue despite the availability of injectable insulin since the 1920s. Finding alternative treatments is the subject of intense research. In recent years, efforts have focused on a potent anti-hyperglycemic hormone called glucagon-like peptide-1 (GLP-1).

GLP-1 is the natural agonist (activator) of a receptor found on the surface of pancreatic beta cells. Activation of this receptor promotes insulin release and survival of the beta cells. Such properties are attractive for treating type 2 diabetes. Unfortunately, GLP-1 is rapidly degraded by peptidase enzymes in the body. In fact, its half-life is less than two minutes.

There is interest in creating synthetic GLP-1 peptide analogs that resist degradation.
THE INVENTIONUW–Madison researchers have developed a new approach for designing GLP-1 receptor agonists that could be used to treat diabetes. The agonists retain GLP-1-like function but have prolonged activity in vivo.

The method includes strategically replacing native α-amino acid residues with conformationally constrained β-amino acid resides. The new α/β peptides mimic GLP-1 in terms of interacting with pancreatic beta cells and regulating blood glucose levels. The peptides are less susceptible to enzyme degradation due in part to the multiple β residue replacements.
  • Two GLP-1 receptor agonists have been approved for treating type 2 diabetes: exenatide (first patent expires in 2016) and liraglutide (patent expires in 2017).
  • Non-natural peptides for potentially treating diabetes and hyperglycemia
  • Longer half-life in vivo than natural GLP-1
  • Glucose-lowering effects may compete with drugs currently on the market.
STAGE OF DEVELOPMENTThe researchers have assessed protease resistance in vitro, the effects of the peptide on glucose-dependent insulin secretion in cell culture, and performed a glucose tolerance test in mice.
Contact Information
For current licensing status, please contact Rafael Diaz at or 608-960-9847.
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