title: Synthetic quinolone signal analogues inhibiting the virulence factor elastase of Pseudomonas aeruginosa.
abstract: We explore the chemical space of Pseudomonas quinolone signal analogs as privileged structures and report the discovery of a thioquinolone as a potent inhibitor of the important virulence factor elastase of the human pathogen Pseudomonas aeruginosa. We provide evidence that the derivative binds to the active site zinc of elastase and additionally acts as a fluorescent zinc sensor.
authors.affiliation: Department of Chemistry, Konstanz Research School Chemical Biology, University of Konstanz, 78457 Konstanz, Germany. Thomas.Boettcher@uni-konstanz.de.
authors.forename: Dávid
authors.initials: D
authors.lastname: Szamosvári
authors.affiliation: Department of Chemistry, Konstanz Research School Chemical Biology, University of Konstanz, 78457 Konstanz, Germany. Thomas.Boettcher@uni-konstanz.de.
authors.forename: Valentin F
authors.initials: VF
authors.lastname: Reichle
authors.affiliation: Department of Chemistry, Konstanz Research School Chemical Biology, University of Konstanz, 78457 Konstanz, Germany. Thomas.Boettcher@uni-konstanz.de.
authors.forename: Monica
authors.initials: M
authors.lastname: Jureschi
authors.affiliation: Department of Chemistry, Konstanz Research School Chemical Biology, University of Konstanz, 78457 Konstanz, Germany. Thomas.Boettcher@uni-konstanz.de.
authors.forename: Thomas
authors.identifier: http://orcid.org/0000-0003-0235-4825
authors.initials: T
authors.lastname: Böttcher
mesh_terms: D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011550:Pseudomonas aeruginosa / Q000201:enzymology*; D015363:Quinolones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D037521:Virulence Factors / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D015363:Quinolones; D037521:Virulence Factors; D010196:Pancreatic Elastase