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ID: ALA3868607

Journal: Bioorg Med Chem

Title: Development of a novel series of non-natural triaryl agonists and antagonists of the Pseudomonas aeruginosa LasR quorum sensing receptor.

Authors: Capilato JN, Philippi SV, Reardon T, McConnell A, Oliver DC, Warren A, Adams JS, Wu C, Perez LJ.

Abstract: Bacterial chemical communication, through a process called quorum sensing (QS), plays a central role in infection in numerous bacterial pathogens. Quorum sensing in Pseudomonas aeruginosa employs a series of small molecule receptors including the master QS regulator, LasR. In this study we investigate a non-natural triaryl series of LasR ligands using a combination of structure activity relationship studies and computational modeling. These studies have enabled the identification of key structural requirements for ligand binding and have revealed a new strategy for inducing the therapeutically relevant antagonism of LasR.

CiteXplore: 27825554

DOI: 10.1016/j.bmc.2016.10.021