Targeting Quorum Sensing : High-Throughput Screening to Identify Novel LsrK Inhibitors

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http://hdl.handle.net/10138/304313

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Gatta , V , Ilina , P , Porter , A , McElroy , S & Tammela , P 2019 , ' Targeting Quorum Sensing : High-Throughput Screening to Identify Novel LsrK Inhibitors ' , International Journal of Molecular Sciences , vol. 20 , no. 12 , 3112 . https://doi.org/10.3390/ijms20123112

Title: Targeting Quorum Sensing : High-Throughput Screening to Identify Novel LsrK Inhibitors
Author: Gatta, Viviana; Ilina, Polina; Porter, Alison; McElroy, Stuart; Tammela, Päivi
Contributor: University of Helsinki, Bioactivity Screening Group
University of Helsinki, Bioactivity Screening Group
University of Helsinki, Division of Pharmaceutical Biosciences
Date: 2019-06-02
Language: eng
Number of pages: 17
Belongs to series: International Journal of Molecular Sciences
ISSN: 1422-0067
URI: http://hdl.handle.net/10138/304313
Abstract: Since quorum sensing (QS) is linked to the establishment of bacterial infection, its inactivation represents one of the newest strategies to fight bacterial pathogens. LsrK is a kinase playing a key role in the processing of autoinducer-2 (AI-2), a quorum-sensing mediator in gut enteric bacteria. Inhibition of LsrK might thus impair the quorum-sensing cascade and consequently reduce bacterial pathogenicity. Aiming for the development of a target-based assay for the discovery of LsrK inhibitors, we evaluated different assay set-ups based on ATP detection and optimized an automation-compatible method for the high-throughput screening of chemical libraries. The assay was then used to perform the screening of a 2000-compound library, which provided 12 active compounds with an IC50
Subject: ACID
AI-2
ANTIOXIDANT
CELASTROL
DRUGS
IDENTIFICATION
IN-VIVO
SYSTEMS
VIRULENCE
antivirulence agent
bacterial communication
harpagoside
rosolic acid
virulence
116 Chemical sciences
1182 Biochemistry, cell and molecular biology
317 Pharmacy
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