Novel synthetic analogs of the Pseudomonas autoinducer

Bioorg Med Chem Lett. 1999 Dec 20;9(24):3447-52. doi: 10.1016/s0960-894x(99)00626-5.

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Bacterial Proteins
  • DNA-Binding Proteins / metabolism
  • Genes, Reporter
  • Pseudomonas aeruginosa / chemistry*
  • Pseudomonas aeruginosa / pathogenicity
  • Trans-Activators / metabolism
  • Virulence

Substances

  • Bacterial Proteins
  • DNA-Binding Proteins
  • LasR protein, Pseudomonas aeruginosa
  • Trans-Activators