Glycoconjugate Journal

, Volume 21, Issue 8–9, pp 471–478 | Cite as

Multimeric glycotherapeutics: New paradigm

  • Nicolai V. Bovin
  • Alexander B. Tuzikov
  • Alexander A. Chinarev
  • Alexandra S. Gambaryan
Article

Abstract

The general principle of anti-adhesion therapy is the inhibition of microorganism adhesion to the host cell with the help of a soluble receptor analog. Despite an evident attractiveness of the concept and its long existence, the therapeutics of the ‘post-antibiotic era’ have not yet appeared. This can be explained by the contradictoriness of requirements for anti-adhesion drugs: to be efficient a drug must be multivalent, i.e. large molecule, but to obtain FDA approval it should be a small molecule. A way to overcome this contradiction is self-assembly of glycopeptides. The carbohydrate part of glycopeptide is responsible for binding with the lectin of microorganisms, whereas a simple peptide part is responsible for an association to the so-called tectomers. Depending on the structure, tectomers are formed either spontaneously or upon promotion of a microorganism. In particular, sialopeptide, which is capable of converting to a tectomer only in the presence of the influenza virus, has been obtained. Thus, the new strategy of anti-adhesion therapy can be formulated as follows: (1) identification of oligosaccharide-receptor for a particular virus (bacteria); (2) optimization of the peptide part; (3) conventional trials. The expected advantages of this strategy are the following: (i) no polymer; (ii) a virion completely covered with a tectomer, i.e. blocking is both complete and irreversible; (iii) rapid and rational lead identification and optimization; (iv) minimum side effects; (v) potential for microorganism resistance to natural receptor is lower than in the case of mimetics. Published in 2004.

anti-adhesion therapy bacteria glycopeptides influenza oligosaccharides self-assembly virus 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

Copyright information

© Springer Science+Business Media, Inc. 2004

Authors and Affiliations

  • Nicolai V. Bovin
    • 1
  • Alexander B. Tuzikov
    • 1
  • Alexander A. Chinarev
    • 1
  • Alexandra S. Gambaryan
    • 2
  1. 1.Shemyakin-Ovchinnikov Institute of Bioorganic ChemistryRussia
  2. 2.Chumakov Institute of Poliomyelitis and Viral EncephalitidesRussia

Personalised recommendations