Positional Cyclization Scanning: A New Method to Evaluate the Bioactive Conformation of Glucagon

  • Jung-Mo Ahn
  • Dev Trivedi
  • Peter M. Gitu
  • Matthew Medeiros
  • Jennifer R. Swift
  • Victor J. Hruby
Part of the American Peptide Symposia book series (APSY, volume 7)

Abstract

Glucagon is a polypeptide hormone, which consists of 29 amino acid residues. Secreted from pancreas, it has an importance role in glucose homeostasis. The conformation of glucagon has been examined by various biophysical methods including X-ray crystallography [1] and 2D-NMR spectroscopy [2]. Although an amphiphilic helical conformation was observed at the C-terminal region of glucagon by both methods, the rest of the molecule displayed different conformations depending on the method used to examine them. The glucagon receptor is a G protein-coupled receptor (GPCR) which resides on the membrane surface, and unfortunately, it is still extremely difficult to examine a bioactive conformation of a ligand when it binds to its receptor. Therefore, in an attempt to obtain information about the bioactive conformation of glucagon, a new approach, “positional cyclization scanning”, was developed to determine secondary structures in the bioactive conformation.

Keywords

Polypeptide Disulfide Glucagon Lactam 

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Copyright information

© Springer Science+Business Media Dordrecht 2001

Authors and Affiliations

  • Jung-Mo Ahn
    • 1
  • Dev Trivedi
    • 1
  • Peter M. Gitu
    • 1
  • Matthew Medeiros
    • 1
  • Jennifer R. Swift
    • 1
  • Victor J. Hruby
    • 1
  1. 1.Department of ChemistryUniversity of ArizonaTucsonUSA

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