A Journal of Postdoctoral Research.
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    ISSN : 2328-9791
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Design and Synthesis of Small Molecule Inhibitors against the Protective Antigen of Baci
Melanie Lödige, PhD
University of Pennsylvania

Perelman School of Medicine, 415 Curie Blvd, Philadelphia,PA 19104, USA


Bacillus anthracis carries a special type of bacterial toxin and is considered to be a potential biological weapon. The highly lethal spores of B. anthracis cause severe diseases such as cutaneous, gastrointestinal, and inhalation anthrax. The multicomponent binarytoxin (AB-type) of B. anthracis consists of two separate components: component A with enzymatic activity (edema factor and lethal factor) and component B (protective antigen, PA - the binding portion). Component B is essential for the formation of transmembrane channels (PApores) that translocate component A from endosomes to the cytoplasm, thereby causing lethal effects in the target cells. We have designed and synthesized small molecule inhibitors belonging to a novel class of aminoquinolinium substances that block the entry of the enzymatic components through the PA pore. 


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