Large cyclic peptides as cores of multivalent ligands: application to inhibitors of receptor binding by cholera toxin

J Org Chem. 2004 Oct 29;69(22):7737-40. doi: 10.1021/jo0489770.

Abstract

Large cyclic decapeptides (up to 50-atom ring) were synthesized efficiently on the solid phase with allyl-ester protection of the carboxyl terminus during elongation. Pentavalent ligands, in a "core-linker-finger" modular setup, were assembled by using these cyclic peptide cores to demonstrate large affinity gains for inhibition of surface receptor binding by the cholera toxin B pentamer. The results suggest that the peptide cores retain expanded conformation in solution so that shorter flexible linkers are needed for larger peptide cores to achieve the best inhibitory results.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Binding Sites
  • Cholera Toxin / antagonists & inhibitors*
  • Computer Simulation
  • Ligands
  • Models, Molecular
  • Molecular Structure
  • Peptides, Cyclic / chemical synthesis*
  • Peptides, Cyclic / pharmacology
  • Protein Binding
  • Receptors, Cell Surface / antagonists & inhibitors*
  • Receptors, Cell Surface / metabolism

Substances

  • Ligands
  • Peptides, Cyclic
  • Receptors, Cell Surface
  • Cholera Toxin