Novel synthetic analogs of the Pseudomonas autoinducer.
Release of virulence factors in Pseudomonas aeruginosa is regulated by two N-acylhomoserine lactones, PAI-1 and PAI-2, that activate the respective transcription factors LasR and RhlR. With the goal of developing novel therapeutic agents, we synthesized constrained analogs of PAI-1 and evaluated them in P. aeruginosa. Two of the novel analogs bound to LasR and showed agonist activity in LasR stimulation of a lasI-lacZ reporter construct.
Kline
T
T
PathoGenesis Corporation, Seattle, WA 98119, USA.
Bowman
J
J
Iglewski
B H
BH
de Kievit
T
T
Kakai
Y
Y
Passador
L
L
D001426:Bacterial Proteins; D004268:DNA-Binding Proteins / Q000378:metabolism; D017930:Genes, Reporter; D011550:Pseudomonas aeruginosa / Q000737:chemistry* / Q000472:pathogenicity; D015534:Trans-Activators / Q000378:metabolism; D014774:Virulence
D001426:Bacterial Proteins; D004268:DNA-Binding Proteins; C080365:LasR protein, Pseudomonas aeruginosa; D015534:Trans-Activators