Synthetic ligands that activate and inhibit a quorum-sensing regulator in Pseudomonas aeruginosa

被引：61
|
作者：
Mattmann, Margrith E. [1 ]
Geske, Grant D. [1 ]
Worzalla, Gregory A. [1 ,2 ]
Chandler, Josephine R. [3 ]
Sappington, Kaia J. [3 ]
Greenberg, E. Peter [3 ]
Blackwell, Helen E. [1 ]
机构：
[1] Univ Wisconsin, Dept Chem, Madison, WI 53706 USA
[2] Univ Wisconsin, Dept Bacteriol, Madison, WI 53706 USA
[3] Univ Washington, Sch Med, Dept Microbiol, Seattle, WA 98195 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 10期
关键词：
D O I：
10.1016/j.bmcl.2007.11.095
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The transcription factor QscR is a regulator of quorum sensing in Pseudomonas aeruginosa and plays a role in controlling virulence in this prevalent opportunistic pathogen. This study outlines the discovery of a set of synthetic N-acylated homoserine lactones that are capable of either activating or strongly inhibiting QscR in a cell-based reporter gene assay. We demonstrate that the synthetic antagonists inhibit ligand-dependent QscR binding to DNA. Several of these ligands can selectively modulate QscR instead of LasR, or modulate the activity of both receptors, and represent new chemical tools to study the hierarchy of quorum-sensing signaling in P. aeruginosa. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3072 / 3075
页数：4
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