Covalent Lectin Inhibition and Application in Bacterial Biofilm Imaging

Angew Chem Int Ed Engl. 2017 Dec 22;56(52):16559-16564. doi: 10.1002/anie.201709368. Epub 2017 Nov 28.

Abstract

Biofilm formation by pathogenic bacteria is a hallmark of chronic infections. In many cases, lectins play key roles in establishing biofilms. The pathogen Pseudomonas aeruginosa often exhibiting various drug resistances employs its lectins LecA and LecB as virulence factors and biofilm building blocks. Therefore, inhibition of the function of these proteins is thought to have potential in developing "pathoblockers" preventing biofilm formation and virulence. A covalent lectin inhibitor specific to a carbohydrate binding site is described for the first time. Its application in the LecA-specific in vitro imaging of biofilms formed by P. aeruginosa is also reported.

Keywords: Pseudomonas aeruginosa; biofilms; carbohydrates; glycomimetics; lectins.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adhesins, Bacterial / chemistry
  • Adhesins, Bacterial / metabolism
  • Binding Sites
  • Biofilms / drug effects
  • Biofilms / growth & development
  • Carbohydrates / chemistry
  • Crystallography, X-Ray
  • Drug Design
  • Epoxy Compounds / chemistry
  • Epoxy Compounds / metabolism
  • Epoxy Compounds / pharmacology
  • Lectins / antagonists & inhibitors
  • Lectins / metabolism*
  • Pseudomonas aeruginosa / physiology*
  • Virulence Factors / antagonists & inhibitors
  • Virulence Factors / metabolism

Substances

  • Adhesins, Bacterial
  • Carbohydrates
  • Epoxy Compounds
  • LecA protein, bacteria
  • Lectins
  • Virulence Factors