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dc.contributor.authorLu, Cenbinen
dc.contributor.authorMaurer, Christine Ken
dc.contributor.authorKirsch, Benjaminen
dc.contributor.authorSteinbach, Ankeen
dc.contributor.authorHartmann, Rolf Wen
dc.date.accessioned2014-05-12T09:42:12Z
dc.date.available2014-05-12T09:42:12Z
dc.date.issued2014-01-20
dc.identifier.citationOvercoming the unexpected functional inversion of a PqsR antagonist in Pseudomonas aeruginosa: an in vivo potent antivirulence agent targeting pqs quorum sensing. 2014, 53 (4):1109-12 Angew. Chem. Int. Ed. Engl.en
dc.identifier.issn1521-3773
dc.identifier.pmid24338917
dc.identifier.doi10.1002/anie.201307547
dc.identifier.urihttp://hdl.handle.net/10033/316718
dc.description.abstractThe virulence regulator PqsR of Pseudomonas aeruginosa is considered as an attractive target for attenuating the bacterial pathogenicity without eliciting resistance. However, despite efforts and desires, no promising PqsR antagonist has been discovered thus far. Now, a surprising functionality change of a highly affine PqsR antagonist in P. aeruginosa is revealed, which is mediated by a bacterial signal molecule synthase and responsible for low cellular potency. Blockade of the susceptible position led to the discovery of the first antivirulence compound that is potent in vivo and targets PqsR, thus providing a proof of concept for this novel antivirulence therapy.
dc.language.isoenen
dc.rightsArchived with thanks to Angewandte Chemie (International ed. in English)en
dc.titleOvercoming the unexpected functional inversion of a PqsR antagonist in Pseudomonas aeruginosa: an in vivo potent antivirulence agent targeting pqs quorum sensing.en
dc.typeArticleen
dc.contributor.departmentDivision of Drug design and optimization. Helmholtz-Institute for Pharmaceutical Research Saarland & Pharmaceutical and Medicinal Chemistry, Saarland University.en
dc.identifier.journalAngewandte Chemie (International ed. in English)en
refterms.dateFOA2015-01-15T00:00:00Z
html.description.abstractThe virulence regulator PqsR of Pseudomonas aeruginosa is considered as an attractive target for attenuating the bacterial pathogenicity without eliciting resistance. However, despite efforts and desires, no promising PqsR antagonist has been discovered thus far. Now, a surprising functionality change of a highly affine PqsR antagonist in P. aeruginosa is revealed, which is mediated by a bacterial signal molecule synthase and responsible for low cellular potency. Blockade of the susceptible position led to the discovery of the first antivirulence compound that is potent in vivo and targets PqsR, thus providing a proof of concept for this novel antivirulence therapy.


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