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PVI, a potent polyvalent inhibitor of Anthrax Toxin

A molecule consisting of multiple copies a nonnatural peptide (Ac-HTSTYWWLDGAPK-NH2), covalently linked to a flexible polyacrylamine backbone, inhibited assembly of the anthrax  toxin complex in vitro and blocked toxin action in cell culture and in an animal intoxication model.

Mourez M., et al, Designing a polyvalent inhibitor of anthrax toxin. Nature Biotechnology 19, 958~961 (2001)

Activity of PVI:

Inhibiting binding of [35S]-LFN tp PA63 on CHO cells with an IC50= 20 nM;

 

Inhibiting the toxicity of a mixture of PA and LFNDTA with an IC50= 6 nM;

 

Inhibiting action of anthrax toxin in a rat intoxication modelwith delaying symptoms
at 12 nmol PVI as well as eliminating toxicity at 75 nmol PVI.

Activity of P1:

Inhibiting binding of [35S]-LFN tp PA63 on CHO cells with an IC50= 150 µM;

 

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