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Identification of the Hypertension Drug Guanfacine as an Antivirulence Agent in Pseudomonas aeruginosa.
Okada, Bethany K; Li, Anran; Seyedsayamdost, Mohammad R.
Afiliación
  • Okada BK; Department of Chemistry, Princeton University, Princeton, NJ, 08544, USA.
  • Li A; Department of Molecular Biology, Princeton University, Princeton, NJ, 08544, USA.
  • Seyedsayamdost MR; Department of Chemistry, Princeton University, Princeton, NJ, 08544, USA.
Chembiochem ; 20(15): 2005-2011, 2019 08 01.
Article en En | MEDLINE | ID: mdl-30927315
An alternative solution to the cyclical development of new antibiotics is the concept of disarming pathogens without affecting their growth, thereby eliminating the selective pressures that lead to resistant phenotypes. Here, we have employed our previously developed HiTES methodology to identify one such compound against the ESKAPE pathogen Pseudomonas aeruginosa. Rather than induce silent biosynthetic gene clusters, we used HiTES to suppress actively expressed virulence genes. By screening a library of 770 FDA-approved drugs, we identified guanfacine, a clinical hypertension drug, as an antivirulence agent in P. aeruginosa. Follow-up studies showed that guanfacine reduces biofilm formation and pyocycanin production without altering growth. Moreover, we identified a homologue of QseC, a sensor His kinase used by multiple pathogens to turn on virulence, as a target of guanfacine. Our studies suggest that guanfacine might be an attractive antivirulence lead in P. aeruginosa and provide a template for uncovering such molecules by screening for downregulators of actively expressed biosynthetic genes.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pseudomonas aeruginosa / Guanfacina / Factores de Virulencia / Antibacterianos / Antihipertensivos Tipo de estudio: Diagnostic_studies / Observational_studies / Prognostic_studies Límite: Humans Idioma: En Revista: Chembiochem Asunto de la revista: BIOQUIMICA Año: 2019 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Alemania

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pseudomonas aeruginosa / Guanfacina / Factores de Virulencia / Antibacterianos / Antihipertensivos Tipo de estudio: Diagnostic_studies / Observational_studies / Prognostic_studies Límite: Humans Idioma: En Revista: Chembiochem Asunto de la revista: BIOQUIMICA Año: 2019 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Alemania