Discovery of antagonists of PqsR, a key player in 2-alkyl-4-quinolone-dependent quorum sensing in Pseudomonas aeruginosa.
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Authors
Lu, CenbinKirsch, Benjamin
Zimmer, Christina
de Jong, Johannes C
Henn, Claudia
Maurer, Christine K
Müsken, Mathias
Häussler, Susanne
Steinbach, Anke
Hartmann, Rolf W
Issue Date
2012-03-23
Metadata
Show full item recordAbstract
The pqs quorum sensing communication system of Pseudomonas aeruginosa controls virulence factor production and is involved in biofilm formation, therefore playing an important role for pathogenicity. In order to attenuate P. aeruginosa pathogenicity, we followed a ligand-based drug design approach and synthesized a series of compounds targeting PqsR, the receptor of the pqs system. In vitro evaluation using a reporter gene assay in Escherichia coli led to the discovery of the first competitive PqsR antagonists, which are highly potent (K(d,app) of compound 20: 7 nM). These antagonists are able to reduce the production of the virulence factor pyocyanin in P. aeruginosa. Our finding offers insights into the ligand-receptor interaction of PqsR and provides a promising starting point for further drug design.Citation
Discovery of antagonists of PqsR, a key player in 2-alkyl-4-quinolone-dependent quorum sensing in Pseudomonas aeruginosa. 2012, 19 (3):381-90 Chem. Biol.Affiliation
Helmholtz Institute for Pharmaceutical Research Saarland, Campus C2.3, 66123 Saarbrücken, Germany.Journal
Chemistry & biologyPubMed ID
22444593Type
ArticleLanguage
enISSN
1879-1301ae974a485f413a2113503eed53cd6c53
10.1016/j.chembiol.2012.01.015
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