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À propos de : Synthesis of Potent Inhibitors of Anthrax Toxin Based on Poly-l-Glutamic Acid        

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  • Synthesis of Potent Inhibitors of Anthrax Toxin Based on Poly-l-Glutamic Acid
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  • We report the synthesis of biodegradable polyvalent inhibitors of anthrax toxin based on poly-l-glutamic acid(PLGA). These biocompatible polyvalent inhibitors are at least 4 orders of magnitude more potent than thecorresponding monovalent peptides in vitro and are comparable in potency to polyacrylamide-based inhibitors ofanthrax toxin assembly. We have elucidated the influence of peptide density on inhibitory potency and demonstratedthat these inhibitory potencies are limited by kinetics, with even higher activities seen when the inhibitors arepreincubated with the heptameric receptor-binding subunit of anthrax toxin prior to exposure to cells. Thesepolyvalent inhibitors are also effective at neutralizing anthrax toxin in vivo and represent attractive leads fordesigning biocompatible anthrax therapeutics.
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