Vinyl Sulfones: Inhibitors of SrtA, a Transpeptidase Required for Cell Wall Protein Anchoring and Virulence in Staphylococcus aureus

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• 作者：Brenda A. Frankel ; Matthew Bentley ; Ryan G. Kruger ; and Dewey G. McCafferty
• 刊名：Journal of the American Chemical Society
• 出版年：2004
• 出版时间：March 24, 2004
• 年：2004
• 卷：126
• 期：11
• 页码：3404 - 3405
• 全文大小：55K
• 年卷期：v.126,no.11(March 24, 2004)
• ISSN：1520-5126

文摘

Several small molecule vinyl sulfones were found to exhibit irreversible time-dependent inhibition of the Staphylococcus aureus sortase SrtA in vitro. A representative of these compounds was shown to impair the ability of S. aureus bacteria to bind fibronectin-coated surfaces through in vivo inhibition of SrtA-mediated linkage of fibronectin to the cell surface. These data highlight the potential use of small molecule vinyl sulfones as chemotherapeutics to prevent adhesion to and colonization of host tissues during S. aureus infection.