14122-46-4Relevant articles and documents
β-Cyclodextrin derivatives that inhibit anthrax lethal toxin
Karginov, Vladimir A.,Yohannes, Adiamseged,Robinson, Tanisha M.,Fahmi, Nour Eddine,Alibek, Kenneth,Hecht, Sidney M.
, p. 33 - 40 (2006)
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.
Search for cyclodextrin-based inhibitors of anthrax toxins: Synthesis, structural features, and relative activities
Karginov, Vladimir A.,Nestorovich, Ekaterina M.,Yohannes, Adiamseged,Robinson, Tanisha M.,Fahmi, Nour Eddine,Schmidtmann, Frank,Hecht, Sidney M.,Bezrukov, Sergey M.
, p. 3740 - 3753 (2007/10/03)
Recently, using structure-inspired drug design, we demonstrated that aminoalkyl derivatives of β-cyclodextrin inhibited anthrax lethal toxin action by blocking the transmembrane pore formed by the protective antigen (PA) subunit of the toxin. In the prese
