A high-throughput screening approach to anthrax lethal factor inhibition |
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Authors: | Johnson Sherida L Chen Li-Hsing Pellecchia Maurizio |
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Institution: | Burnham Institute for Medical Research, La Jolla, CA 92037, USA. |
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Abstract: | 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 identification of new scaffolds that inhibit LF and the Botulinum Neurotoxin Type A in the low micromolar range, while sparing the human metallo-proteases MMP-2 and MMP-9. Therefore, these scaffolds could be further exploited for the development of potent and selective anti-toxin agents. |
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Keywords: | Anthrax Lethal factor High-throughput screening Botulinum Neurotoxin |
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