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;