A potent α/β-peptide analogue of GLP-1 with prolonged action in vivo. Academic Article uri icon

Overview

abstract

  • Glucagon-like peptide-1 (GLP-1) is a natural agonist for GLP-1R, a G protein-coupled receptor (GPCR) on the surface of pancreatic β cells. GLP-1R agoinsts are attractive for treatment of type 2 diabetes, but GLP-1 itself is rapidly degraded by peptidases in vivo. We describe a design strategy for retaining GLP-1-like activity while engendering prolonged activity in vivo, based on strategic replacement of native α residues with conformationally constrained β-amino acid residues. This backbone-modification approach may be useful for developing stabilized analogues of other peptide hormones.

publication date

  • September 5, 2014

Research

keywords

  • Glucagon-Like Peptide 1
  • Receptors, Glucagon

Identity

PubMed Central ID

  • PMC4183665

Scopus Document Identifier

  • 84919945753

Digital Object Identifier (DOI)

  • 10.1021/ja507168t

PubMed ID

  • 25191938

Additional Document Info

volume

  • 136

issue

  • 37