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Chemical probes for competitive profiling of the quorum sensing signal synthase PqsD of Pseudomonas aeruginosa

Chemical probes for competitive profiling of the quorum sensing signal synthase PqsD of Pseudomonas aeruginosa

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PROTHIWA, Michaela, Dávid SZAMOSVÁRI, Sandra GLASMACHER, Thomas BÖTTCHER, 2016. Chemical probes for competitive profiling of the quorum sensing signal synthase PqsD of Pseudomonas aeruginosa. In: Beilstein Journal of Organic Chemistry. 12, pp. 2784-2792. eISSN 1860-5397

@article{Prothiwa2016-12-20Chemi-37888, title={Chemical probes for competitive profiling of the quorum sensing signal synthase PqsD of Pseudomonas aeruginosa}, year={2016}, doi={10.3762/bjoc.12.277}, volume={12}, journal={Beilstein Journal of Organic Chemistry}, pages={2784--2792}, author={Prothiwa, Michaela and Szamosvári, Dávid and Glasmacher, Sandra and Böttcher, Thomas} }

<rdf:RDF xmlns:rdf="http://www.w3.org/1999/02/22-rdf-syntax-ns#" xmlns:bibo="http://purl.org/ontology/bibo/" xmlns:dc="http://purl.org/dc/elements/1.1/" xmlns:dcterms="http://purl.org/dc/terms/" xmlns:xsd="http://www.w3.org/2001/XMLSchema#" > <rdf:Description rdf:about="https://kops.uni-konstanz.de/rdf/resource/123456789/37888"> <dcterms:title>Chemical probes for competitive profiling of the quorum sensing signal synthase PqsD of Pseudomonas aeruginosa</dcterms:title> <dc:contributor>Glasmacher, Sandra</dc:contributor> <dc:creator>Böttcher, Thomas</dc:creator> <dc:creator>Glasmacher, Sandra</dc:creator> <dc:date rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2017-03-07T13:10:45Z</dc:date> <bibo:uri rdf:resource="https://kops.uni-konstanz.de/handle/123456789/37888"/> <dc:creator>Prothiwa, Michaela</dc:creator> <dcterms:rights rdf:resource="http://nbn-resolving.de/urn:nbn:de:bsz:352-20150914100631302-4485392-8"/> <dc:creator>Szamosvári, Dávid</dc:creator> <dc:contributor>Szamosvári, Dávid</dc:contributor> <dc:contributor>Prothiwa, Michaela</dc:contributor> <dcterms:abstract xml:lang="eng">The human pathogen Pseudomonas aeruginosa uses the pqs quorum sensing system to coordinate the production of its broad spectrum of virulence factors to facilitate colonization and infection of its host. Hereby, the enzyme PqsD is a virulence related quorum sensing signal synthase that catalyzes the central step in the biosynthesis of the Pseudomonas quinolone signals HHQ and PQS. We developed a library of cysteine reactive chemical probes with an alkyne handle for fluorescence tagging and report the selective and highly sensitive in vitro labelling of the active site cysteine of this important enzyme. Interestingly, only one type of probe, with a reactive α-chloroacetamide was capable of covalently reacting with the active site. We demonstrated the potential of our probes in a competitive labelling platform where we screened a library of synthetic HHQ and PQS analogues with heteroatom replacements and found several inhibitors of probe binding that may represent promising scaffolds for the development of customized PqsD inhibitors as well as a chemical toolbox to investigate the activity and active site specificity of the enzyme.</dcterms:abstract> <dc:contributor>Böttcher, Thomas</dc:contributor> <dcterms:available rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2017-03-07T13:10:45Z</dcterms:available> <dc:language>eng</dc:language> <dcterms:issued>2016-12-20</dcterms:issued> </rdf:Description> </rdf:RDF>

Dateiabrufe seit 07.03.2017 (Informationen über die Zugriffsstatistik)

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