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Glycomimetic, Orally Bioavailable LecB Inhibitors Block Biofilm Formation of Pseudomonas aeruginosa

Glycomimetic, Orally Bioavailable LecB Inhibitors Block Biofilm Formation of Pseudomonas aeruginosa

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SOMMER, Roman, Stefanie WAGNER, Katharina ROX, Annabelle VARROT, Dirk HAUCK, Eike-Christian WAMHOFF, Janine SCHREIBER, Thomas RYCKMANS, Thomas BRUNNER, Alexander TITZ, 2018. Glycomimetic, Orally Bioavailable LecB Inhibitors Block Biofilm Formation of Pseudomonas aeruginosa. In: Journal of the American Chemical Society. 140(7), pp. 2537-2545. ISSN 0002-7863. eISSN 1520-5126. Available under: doi: 10.1021/jacs.7b11133

@article{Sommer2018Glyco-41985, title={Glycomimetic, Orally Bioavailable LecB Inhibitors Block Biofilm Formation of Pseudomonas aeruginosa}, year={2018}, doi={10.1021/jacs.7b11133}, number={7}, volume={140}, issn={0002-7863}, journal={Journal of the American Chemical Society}, pages={2537--2545}, author={Sommer, Roman and Wagner, Stefanie and Rox, Katharina and Varrot, Annabelle and Hauck, Dirk and Wamhoff, Eike-Christian and Schreiber, Janine and Ryckmans, Thomas and Brunner, Thomas and Titz, Alexander} }

<rdf:RDF xmlns:dcterms="http://purl.org/dc/terms/" xmlns:dc="http://purl.org/dc/elements/1.1/" xmlns:rdf="http://www.w3.org/1999/02/22-rdf-syntax-ns#" xmlns:bibo="http://purl.org/ontology/bibo/" xmlns:dspace="http://digital-repositories.org/ontologies/dspace/0.1.0#" xmlns:foaf="http://xmlns.com/foaf/0.1/" xmlns:void="http://rdfs.org/ns/void#" xmlns:xsd="http://www.w3.org/2001/XMLSchema#" > <rdf:Description rdf:about="https://kops.uni-konstanz.de/rdf/resource/123456789/41985"> <dc:contributor>Sommer, Roman</dc:contributor> <dc:contributor>Brunner, Thomas</dc:contributor> <dspace:isPartOfCollection rdf:resource="https://kops.uni-konstanz.de/rdf/resource/123456789/28"/> <dc:contributor>Schreiber, Janine</dc:contributor> <dc:creator>Sommer, Roman</dc:creator> <dc:creator>Varrot, Annabelle</dc:creator> <dc:creator>Wamhoff, Eike-Christian</dc:creator> <dc:contributor>Wamhoff, Eike-Christian</dc:contributor> <bibo:uri rdf:resource="https://kops.uni-konstanz.de/handle/123456789/41985"/> <dc:creator>Schreiber, Janine</dc:creator> <dcterms:issued>2018</dcterms:issued> <dc:contributor>Varrot, Annabelle</dc:contributor> <foaf:homepage rdf:resource="http://localhost:8080/jspui"/> <dc:contributor>Wagner, Stefanie</dc:contributor> <dcterms:available rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2018-04-10T08:09:38Z</dcterms:available> <dcterms:title>Glycomimetic, Orally Bioavailable LecB Inhibitors Block Biofilm Formation of Pseudomonas aeruginosa</dcterms:title> <dc:creator>Brunner, Thomas</dc:creator> <dc:contributor>Titz, Alexander</dc:contributor> <dc:date rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2018-04-10T08:09:38Z</dc:date> <dc:contributor>Ryckmans, Thomas</dc:contributor> <dc:language>eng</dc:language> <dc:creator>Ryckmans, Thomas</dc:creator> <dc:contributor>Hauck, Dirk</dc:contributor> <dc:creator>Rox, Katharina</dc:creator> <dc:creator>Hauck, Dirk</dc:creator> <dcterms:isPartOf rdf:resource="https://kops.uni-konstanz.de/rdf/resource/123456789/28"/> <dc:contributor>Rox, Katharina</dc:contributor> <dc:creator>Titz, Alexander</dc:creator> <dcterms:abstract xml:lang="eng">The opportunistic Gram-negative bacterium Pseudomonas aeruginosa is a leading pathogen for infections of immuno-compromised patients and those suffering from cystic fibrosis. Its ability to switch from planktonic life to aggregates, forming the so-called biofilms, is a front-line mechanism of antimicrobial resistance. The bacterial carbohydrate-binding protein LecB is an integral component and necessary for biofilm formation. Here, we report a new class of drug-like low molecular weight inhibitors of the lectin LecB with nanomolar affinities and excellent receptor binding kinetics and thermodynamics. This class of glycomimetic inhibitors efficiently blocked biofilm formation of P. aeruginosa in vitro while the natural monovalent carbohydrate ligands failed. Furthermore, excellent selectivity and pharmacokinetic properties were achieved. Notably, two compounds showed good oral bioavailability, and high compound concentrations in plasma and urine were achieved in vivo.</dcterms:abstract> <void:sparqlEndpoint rdf:resource="http://localhost/fuseki/dspace/sparql"/> <dc:creator>Wagner, Stefanie</dc:creator> </rdf:Description> </rdf:RDF>

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