A β-peptide agonist of the GLP-1 receptor, a class B GPCR

Org Lett. 2013 Oct 18;15(20):5318-21. doi: 10.1021/ol402568j. Epub 2013 Oct 2.

Abstract

Previous work has shown that certain β(3)-peptides can effectively mimic the side chain display of an α-helix and inhibit interactions between proteins, both in vitro and in cultured cells. Here we describe a β(3)-peptide analog of GLP-1, CC-3(Act), that interacts with the GLP-1R extracellular domain (nGLP-1R) in vitro in a manner that competes with exendin-4 and induces GLP-1R-dependent cAMP signaling in cultured CHO-K1 cells expressing GLP-1R.

Publication types

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

MeSH terms

  • Animals
  • CHO Cells
  • Cricetulus
  • Dose-Response Relationship, Drug
  • Glucagon-Like Peptide 1 / analogs & derivatives*
  • Glucagon-Like Peptide 1 / pharmacology
  • Glucagon-Like Peptide-1 Receptor
  • Humans
  • Ligands
  • Models, Molecular
  • Receptors, Glucagon / agonists*
  • Structure-Activity Relationship

Substances

  • GLP1R protein, human
  • Glucagon-Like Peptide-1 Receptor
  • Ligands
  • Receptors, Glucagon
  • Glucagon-Like Peptide 1