α-N-Linked glycopeptides: conformational analysis and bioactivity as lectin ligands

Org Biomol Chem. 2012 Aug 14;10(30):5916-23. doi: 10.1039/c2ob07135e. Epub 2012 Mar 22.

Abstract

Natural N-glycosylation involves a β-anomeric linkage connecting the sugar to one asparagine residue of the protein. We herein report NMR- and modelling-based data on glycomimetics containing α-glycosidic linkages. The bioactivity of α-Gal-containing glycopeptides has been documented by revealing binding to two plant lectins, i.e. a potent β-trefoil toxin (Viscum album agglutinin) and β-sandwich lectin (Erythrina corallodendron agglutinin), by NMR protocols. Docking provided insights into the 3D structures of the resulting complexes. These results provide the basis to introduce α-substituted neoglycopeptides to the toolbox of scaffold for the design of potent lectin inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Erythrina / chemistry
  • Glycopeptides / chemistry*
  • Glycopeptides / metabolism*
  • Ligands
  • Models, Molecular
  • Nuclear Magnetic Resonance, Biomolecular
  • Plant Lectins / chemistry
  • Plant Lectins / metabolism*
  • Protein Conformation
  • Viscum album / chemistry

Substances

  • Glycopeptides
  • Ligands
  • Plant Lectins