Discovery of PqsE Thioesterase Inhibitors for Pseudomonas aeruginosa Using DNA-Encoded Small Molecule Library Screening

Pseudomonas aeruginosa is a leading cause of hospital-acquired infections in the United States. PqsE, a thioesterase enzyme, is vital for virulence of P. aeruginosa, making PqsE an attractive target for inhibition. Neither the substrate nor the product of PqsE catalysis has been identified. A librar...

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Veröffentlicht in:	ACS chemical biology 2020-02, Vol.15 (2), p.446-456
Hauptverfasser:	Valastyan, Julie S, Tota, Michael R, Taylor, Isabelle R, Stergioula, Vasiliki, Hone, Graham A. B, Smith, Chari D, Henke, Brad R, Carson, Kenneth G, Bassler, Bonnie L
Format:	Artikel
Sprache:	eng
Schlagworte:	Bacterial Proteins - antagonists & inhibitors Benzamides - chemical synthesis Benzamides - pharmacology DNA - chemistry Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Microbial Sensitivity Tests Molecular Structure Phthalic Acids - chemical synthesis Phthalic Acids - pharmacology Pseudomonas aeruginosa - drug effects Pseudomonas aeruginosa - enzymology Small Molecule Libraries - chemical synthesis Small Molecule Libraries - pharmacology Structure-Activity Relationship Thiolester Hydrolases - antagonists & inhibitors
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