Conformational restriction of peptidyl immunogens with covalent replacements for the hydrogen bond

Vaccine. 1988 Apr;6(2):99-103. doi: 10.1016/s0264-410x(88)80007-0.

Abstract

A new strategy for designing synthetic vaccines is presented. In this approach synthetic peptides are conformationally restricted by replacing putative hydrogen bonds with covalent mimics. The chemistry for substituting a hydrazone-ethane link (N-N = CH-CH2-CH2) for an (i + 4)----i hydrogen bond in a pentapeptide with alpha-helical potential is reported. Chemically shaping peptides to mimic the three-dimensional surfaces of proteins may enhance their immunogenicity. To test this strategy, a potential synthetic vaccine for malaria, Cys-(Asn-Pro-Asn-Ala)3-NH2, was conformationally restricted by replacing putative hydrogen bonds between asparagine side chains with a covalent replacement, an ethylene bridge, to give first generation chemically shaped immunogens. Antibodies to one of the shaped malarial peptides show a strong reaction with living Plasmodium falciparum sporozoites, a form of malaria which infects hundreds of millions of people yearly.

Publication types

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

MeSH terms

  • Animals
  • Antigens / immunology*
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / immunology
  • Plasmodium falciparum / immunology
  • Protein Conformation
  • Vaccines, Synthetic / immunology*
  • Vaccines, Synthetic / isolation & purification

Substances

  • Antigens
  • Oligopeptides
  • Vaccines, Synthetic