Crystal structure of the GLP-1 receptor bound to a peptide agonist

Nature. 2017 Jun 8;546(7657):254-258. doi: 10.1038/nature22800. Epub 2017 May 31.

Abstract

Glucagon-like peptide 1 (GLP-1) regulates glucose homeostasis through the control of insulin release from the pancreas. GLP-1 peptide agonists are efficacious drugs for the treatment of diabetes. To gain insight into the molecular mechanism of action of GLP-1 peptides, here we report the crystal structure of the full-length GLP-1 receptor bound to a truncated peptide agonist. The peptide agonist retains an α-helical conformation as it sits deep within the receptor-binding pocket. The arrangement of the transmembrane helices reveals hallmarks of an active conformation similar to that observed in class A receptors. Guided by this structural information, we design peptide agonists with potent in vivo activity in a mouse model of diabetes.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Binding Sites
  • Crystallography, X-Ray
  • Dose-Response Relationship, Drug
  • Glucagon-Like Peptide-1 Receptor / agonists*
  • Glucagon-Like Peptide-1 Receptor / chemistry*
  • Glucagon-Like Peptide-1 Receptor / metabolism
  • Humans
  • Male
  • Mice
  • Models, Molecular
  • Peptides / chemistry*
  • Peptides / metabolism
  • Peptides / pharmacology*
  • Protein Conformation
  • Rats
  • Receptors, Corticotropin-Releasing Hormone / chemistry
  • Receptors, Glucagon / chemistry

Substances

  • Glucagon-Like Peptide-1 Receptor
  • Peptides
  • Receptors, Corticotropin-Releasing Hormone
  • Receptors, Glucagon
  • CRF receptor type 1