Publikation: Competitive Live-Cell Profiling Strategy for Discovering Inhibitors of the Quinolone Biosynthesis of Pseudomonas aeruginosa
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2018
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Journal of the American Chemical Society : JACS. 2018, 140(43), pp. 14019-14023. ISSN 0002-7863. eISSN 1520-5126. Available under: doi: 10.1021/jacs.8b07629
Zusammenfassung
Quinolones of the human pathogen Pseudomonas aeruginosa serve as antibacterial weapons and quorum sensing signals and coordinate the production of important virulence factors. A central enzyme for the biosynthesis of these quinolones is the synthetase PqsD. We developed an activity-based probe strategy that allows to screen for PqsD inhibitors in a cellular model system of live cells of Escherichia coli overexpressing PqsD. This strategy allowed us to determine IC50 values for PqsD inhibition directly in live cells. Our most potent inhibitors were derived from the anthranilic acid core of the native substrate and resulted in single-digit micromolar IC50 values. The effectiveness of our approach was ultimately demonstrated in P. aeruginosa by the complete shutdown of the production of quinolone quorum sensing signals and quinolone N-oxides and a considerable inhibition of the production of phenazine virulence factors.
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PROTHIWA, Michaela, Felix ENGLMAIER, Thomas BÖTTCHER, 2018. Competitive Live-Cell Profiling Strategy for Discovering Inhibitors of the Quinolone Biosynthesis of Pseudomonas aeruginosa. In: Journal of the American Chemical Society : JACS. 2018, 140(43), pp. 14019-14023. ISSN 0002-7863. eISSN 1520-5126. Available under: doi: 10.1021/jacs.8b07629BibTex
@article{Prothiwa2018-10-18Compe-43674,
year={2018},
doi={10.1021/jacs.8b07629},
title={Competitive Live-Cell Profiling Strategy for Discovering Inhibitors of the Quinolone Biosynthesis of Pseudomonas aeruginosa},
number={43},
volume={140},
issn={0002-7863},
journal={Journal of the American Chemical Society : JACS},
pages={14019--14023},
author={Prothiwa, Michaela and Englmaier, Felix and Böttcher, Thomas}
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