Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists

Xin Zhang, Matthew J. Belousoff, Peishen Zhao, Albert J. Kooistra, Tin T. Truong, Sheng Yu Ang, Christina Rye Underwood, Thomas Egebjerg, Petr Šenel, Gregory D. Stewart, Yi Lynn Liang, Alisa Glukhova, Hari Venugopal, Arthur Christopoulos, Sebastian G.B. Furness, Laurence J. Miller, Steffen Reedtz-Runge, Christopher J. Langmead, David E. Gloriam, Radostin DanevPatrick M. Sexton, Denise Wootten

Research output: Contribution to journalArticlepeer-review

4 Scopus citations

Abstract

Zhang et al. show that the non-peptide GLP-1R agonist PF 06882961, but not CHU-128, was able to closely mimic the in vitro pharmacological fingerprint of GLP-1. These pharmacological activities could be rationalized from high-resolution structures that provide a novel template for the design of new agonists targeting the GLP-1R.

Original languageEnglish (US)
Pages (from-to)485-500.e7
JournalMolecular Cell
Volume80
Issue number3
DOIs
StatePublished - Nov 5 2020

Keywords

  • G-protein-coupled receptor
  • GLP-1
  • cryoelectron microscopy
  • glucagon-like peptide-1 receptor
  • non-peptide agonists

ASJC Scopus subject areas

  • Molecular Biology
  • Cell Biology

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