Centre INRS–Institut Armand-Frappier –

Design and synthesis of peptide inhibitors of PqsE as novel antibacterial therapeutics

Pseudomonas aeruginosa (Pa), a prevalent opportunistic human pathogen responsible for morbidity and mortality among individuals suffering from cystic fibrosis, is notorious for its high resistance to antibiotic treatments.

As recently demonstrated, cell-to-cell signaling regulated by the PqsE enzyme plays a central role in the control of the pathogenicity of Pa by modulating the expression of virulence-related functions. As such, PqsE represents a potential target for therapeutic intervention. The present proposal aimed to design specific inhibitors of this enzyme through a combinatorial chemistry approach and to evaluate their potential as new antibacterial agents.