EC Number   |
Inhibitors |
Structure |
|---|
   2.3.1.B38 | (furan-3-yl)(2-nitrophenyl)methanol |
PqsBC inhibitor reduces the production of the MvfR natural ligands in wild-type strain PA14 down to 34% at its highest concentration |
   |
| 2.3.1.B38 | 2-aminoacetophenone |
pathway-inherent competitive inhibitor. EC50 of 46 microM in the in vitro assay |
|
| 2.3.1.B38 | ethyl 3-benzyl-1-[2-(4-fluoroanilino)-2-oxoethyl]-2,4-dioxo-1,3,4,5,6,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-7(2H)-carboxylate |
PqsBC inhibitor reduces the production of the MvfR natural ligands in wild-type strain PA14 down to 35% at its highest concentration |
|
| 2.3.1.B38 | more |
2-heptyl-4(1H)-quinolone and 2-heptyl-3-hydroxy-4(1H)-quinolone as well as ,4-dihydroxyquinoline at concentrations up to 50 microM do not affect PqsBC activity |
|
| 2.3.1.B38 | more |
Pseudomonas aeruginosa is a Gram-negative bacterium, which causes opportunistic infections in immuno-compromised individuals. Due to its multiple resistances toward antibiotics, the development of new drugs is required. Interfering with quorum sensing (QS), a cell-to-cell communication system, has shown to be highly efficient in reducing Pseudomonas aeruginosa pathogenicity. One of its QS systems employs Pseudomonas quinolone signal (PQS) and 4-hydroxy-2-heptylquinoline (HHQ) as signal molecules. Both activate the transcriptional regulator MvfR (Multiple Virulence Factor Regulator), also called PqsR, driving the production of QS molecules as well as toxins and biofilm formation. Effects of QS inhibitors (QSIs), such as MvfR antagonists and PqsBC inhibitors, on the biosynthesis of the MvfR-regulated small molecules 2'-aminoacetophenone (2-AA), dihydroxyquinoline (DHQ), 4-hydroxy-2-heptylquinoline (HHQ), Pseudomonas quinolone signal (PQS), and 4-hydroxy-2-heptylquinoline-N-oxide (HQNO). The employed synthetic MvfR antagonist fully inhibits pqs small molecule formation showing expected sigmoidal dose-response curves for 2-AA, HQNO, HHQ, and PQS |
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