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Attenuating Staphylococcus aureus virulence gene regulation: a medicinal chemistry perspective.

Abstract：

:Virulence gene expression in Staphylococcus aureus is tightly regulated by intricate networks of transcriptional regulators and two-component signal transduction systems. There is now an emerging body of evidence to suggest that the blockade of S. aureus virulence gene expression significantly attenuates infection in experimental models. In this Perspective, we will provide insights into medicinal chemistry strategies for the development of chemical reagents that have the capacity to inhibit staphylococcal virulence expression. These reagents can be broadly grouped into four categories: (1) competitive inhibitors of the accessory gene regulator (agr) quorum sensing system, (2) inhibitors of AgrA-DNA interactions, (3) RNAIII transcription inhibitors, and (4) inhibitors of the SarA family of transcriptional regulators. We discuss the potential of specific examples of antivirulence agents for the management and treatment of staphylococcal infections.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Gordon CP,Williams P,Chan WC

doi

10.1021/jm3014635

subject

Has Abstract

pub_date

2013-02-28 00:00:00

pages

1389-404

issue

4

eissn

0022-2623

issn

1520-4804

journal_volume

56

pub_type

杂志文章

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