Article
Development of a novel series of non-natural triaryl agonists and antagonists of the Pseudomonas aeruginosa LasR quorum sensing receptor
Bioorganic & Medicinal Chemistry
(2017)
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.
Keywords
- Anti-virulence,
- Pseudomonas aeruginosa,
- Structure–activity relationship,
- Computational modeling,
- Quorum sensing
Disciplines
Publication Date
January, 2017
DOI
10.1016/j.bmc.2016.10.021
Citation Information
Joseph N. Capilato, Shane V. Phillipi, Thomas Reardon, Ashleigh McConnell, et al.. "Development of a novel series of non-natural triaryl agonists and antagonists of the Pseudomonas aeruginosa LasR quorum sensing receptor" Bioorganic & Medicinal Chemistry Vol. 25 Iss. 1 (2017) p. 153 - 165 ISSN: 0968-0896 Available at: http://works.bepress.com/lark-perez/5/