| Literature DB >> 17320146 |
Sherida L Johnson1, Li-Hsing Chen, Maurizio Pellecchia.
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.Entities:
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Year: 2007 PMID： 17320146 PMCID： PMC2020844 DOI： 10.1016/j.bioorg.2006.12.005
Source DB: PubMed Journal: Bioorg Chem ISSN： 0045-2068 Impact factor: 5.275