β-Cyclodextrin derivatives that inhibit anthrax lethal toxin

Vladimir A. Karginov, Adiamseged Yohannes, Tanisha M. Robinson, Nour Eddine Fahmi, Kenneth Alibek, Sidney M. Hecht

Research output: Contribution to journalArticlepeer-review

41 Scopus citations

Abstract

Recently, we demonstrated that simultaneous blocking of bacterial growth by antibiotics and inhibition of anthrax toxin action with antibodies against protective antigen were beneficial for the treatment of anthrax. The present study examined the hypothesis that blocking the pore formed by protective antigen can inhibit the action of anthrax toxin. The potential inhibitors were chosen by a structure-based design using β-cyclodextrin as the starting molecule. Several β-cyclodextrin derivatives were evaluated for their ability to protect RAW 264.7 cells from the action of anthrax lethal toxin. Per-substituted aminoalkyl derivatives displayed inhibitory activity and were protective against anthrax lethal toxin action at low micromolar concentrations. These results provide the basis for a structure-based drug discovery program, with the goal of identifying new drug candidates for anthrax treatment.

Original languageEnglish (US)
Pages (from-to)33-40
Number of pages8
JournalBioorganic and Medicinal Chemistry
Volume14
Issue number1
DOIs
StatePublished - Jan 1 2006
Externally publishedYes

Keywords

  • Anthrax treatment
  • Lethal toxin inhibitors
  • β-Cyclodextrin derivatives

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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