Inhibition of anthrax lethal factor: lability of hydroxamate as a chelating group
نویسندگان
چکیده
منابع مشابه
A high-throughput screening approach to anthrax lethal factor inhibition.
A high-throughput screening approach was used to identify new inhibitors of the metallo-protease lethal factor from Bacillus anthracis. A library of approximately 14,000 compounds was screened using a fluorescence-based in vitro assay and hits were further characterized enzymatically via measurements of IC50 and Ki values against a small panel of metallo-proteases. This study led to the identif...
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Bacillus anthracis lethal toxin (LT) produces symptoms of anthrax in mice and induces rapid lysis of macrophages derived from certain inbred strains. LT is comprised of a receptor binding component, protective antigen (PA), which delivers the enzymatic component, lethal factor (LF), into cells. We found that mouse macrophages were protected from toxin by the antitumor drug cis-diammineplatinum ...
متن کاملEfficient synthetic inhibitors of anthrax lethal factor.
Inhalation anthrax is a deadly disease for which there is currently no effective treatment. Bacillus anthracis lethal factor (LF) metalloproteinase is an integral component of the tripartite anthrax lethal toxin that is essential for the onset and progression of anthrax. We report here on a fragment-based approach that allowed us to develop inhibitors of LF. The small-molecule inhibitors we hav...
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BACKGROUND Anthrax is a human disease that results from infection by the bacteria, Bacillus anthracis and has recently been used as a bioterrorist agent. Historically, this disease was associated with Bacillus spore exposure from wool or animal carcasses. While current vaccine approaches (targeted against the protective antigen) are effective for prophylaxis, multiple doses must be injected. Co...
متن کاملExamination of anthrax lethal factor inhibition by siderophores, small hydroxamates, and protamine.
BACKGROUND AND PURPOSE Based on their ability to chelate metals, hydroxamate molecules and siderophores have been successfully used as metalloenzyme inhibitors. As the anthrax toxin lethal factor (LF) is a zinc (Zn)-metallopeptidase, an investigation of the ability of some small non-siderophore hydroxamate compounds, 5 hydroxamate-containing siderophores, and 1 catecholate siderophore was under...
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ژورنال
عنوان ژورنال: Applied Microbiology and Biotechnology
سال: 2012
ISSN: 0175-7598,1432-0614
DOI: 10.1007/s00253-012-3893-7