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    Effect of a small molecule lipid II binder on bacterial cell wall stress

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    Author
    Malin, J.
    Shetty, A.C.
    Daugherty, S.C.
    Date
    2017
    Journal
    Infection and Drug Resistance
    Publisher
    Dove Medical Press Ltd.
    Type
    Article
    
    Metadata
    Show full item record
    See at
    https://www.doi.org/10.2147/IDR.S126254
    Abstract
    We have recently identified small molecule compounds that act as binders of Lipid II, an essential precursor of bacterial cell wall biosynthesis. Lipid II comprised a hydrophilic head group that includes a peptidoglycan subunit composed of N-acetylglucosamine (GlcNAc) and N-acetylmuramic acid (MurNAc) coupled to a short pentapeptide moiety. This headgroup is coupled to a long bactoprenol chain via a pyrophosphate group. Here, we report on the cell wall activity relationship of dimethyl-3-methyl(phenyl)amino-ethenylcyclohexylidene-propenyl-3-ethyl-1,3-benzothiazolium iodide (compound 5107930) obtained by functional and genetic analyses. Our results indicate that compounds bind to Lipid II and cause specific upregulation of the vancomycin-resistance associated gene vraX. vraX is implicated in the cell wall stress stimulon that confers glycopeptide resistance. Our small molecule Lipid II inhibitor retained activity against strains of Staphylococcus aureus mutated in genes encoding the cell wall stress stimulon. This suggests the feasibility of developing this new scaffold as a therapeutic agent in view of increasing glycopeptide resistance. Copyright 2017 Malin et al.
    Keyword
    Antibiotics
    Bacterial membrane
    Defensin
    Lipid II
    Vancomycin
    Identifier to cite or link to this item
    https://www.scopus.com/inward/record.uri?eid=2-s2.0-85014511294&doi=10.2147%2fIDR.S126254&partnerID=40&md5=6a852b5c1f1f3747618d80576f9e94dd; http://hdl.handle.net/10713/9996
    ae974a485f413a2113503eed53cd6c53
    10.2147/IDR.S126254
    Scopus Count
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    UMB Open Access Articles 2017

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