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Novel synthetic analogs of the Pseudomonas autoinducer
T Kline1, J Bowman, B H Iglewski
1PathoGenesis Corporation, Seattle, WA 98119, USA.
Bioorganic & Medicinal Chemistry Letters
|January 5, 2000
Abstract:
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.