ArticleBioconjugate chemistry
Synthesis of potent inhibitors of anthrax toxin based on poly-L-glutamic acid.
Article in Bioconjugate chemistry. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- Synthesis of multivalent polymer-aptamer conjugates with enhanced inhibitory potency.International journal of nanomedicine · 2018Article
- Polymeric drugs: Advances in the development of pharmacologically active polymers.Journal of controlled release : official journal of the Controlled Release Society · 2015Review
- Cationic PAMAM dendrimers as pore-blocking binary toxin inhibitors.Biomacromolecules · 2014Article
- Obstructing toxin pathways by targeted pore blockage.Chemical reviews · 2012Review
- Structure-based design of a heptavalent anthrax toxin inhibitor.Biomacromolecules · 2011Article
- Synthesis of Homopolymers and Copolymers Containing an Active Ester of Acrylic Acid by RAFT: Scaffolds for Controlling Polyvalent Ligand Display.Journal of polymer science. Part A, Polymer chemistry · 2008Article
- Stable and potent polyvalent anthrax toxin inhibitors: raft-inspired domain formation in liposomes that contain PEGylated lipids.Chemistry (Weinheim an der Bergstrasse, Germany) · 2008Article
- Multivalent Inhibitors of Channel-Forming Bacterial Toxins.Current topics in microbiology and immunologyReview
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
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 the corresponding monovalent peptides in vitro and are comparable in potency to polyacrylamide-based inhibitors of anthrax toxin assembly. We have elucidated the influence of peptide density on inhibitory potency and demonstrated that these inhibitory potencies are limited by kinetics, with even higher activities seen when the inhibitors are preincubated with the heptameric receptor-binding subunit of anthrax toxin prior to exposure to cells. These polyvalent inhibitors are also effective at neutralizing anthrax toxin in vivo and represent attractive leads for designing biocompatible anthrax therapeutics.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.