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

Viviana Gatta, Polina Ilina, Alison Porter, Stuart McElroy, Päivi Tammela

Forskningsoutput: TidskriftsbidragArtikelVetenskapligPeer review

Sammanfattning

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

Originalspråkengelska
Artikelnummer3112
TidskriftInternational Journal of Molecular Sciences
Volym20
Utgåva12
Antal sidor17
ISSN1422-0067
DOI
StatusPublicerad - 2 jun 2019
MoE-publikationstypA1 Tidskriftsartikel-refererad

Vetenskapsgrenar

  • 116 Kemi
  • 1182 Biokemi, cell- och molekylärbiologi
  • 317 Farmaci

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