N-Hydroxybenzimidazole inhibitors of ExsA MAR transcription factor in Pseudomonas aeruginosa: In vitro anti-virulence activity and metabolic stability
| Autor: | Mark Grier, Michael Draper, Caroline Dudley, Peter J. Donovan, Oak K. Kim, Kevin A. Klausner, Victoria J. Bartlett, S. Ken Tanaka, Michael N. Alekshun, Stuart B. Levy, Lynne Garrity-Ryan |
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| Rok vydání: | 2010 |
| Předmět: |
Clinical Biochemistry
Pharmaceutical Science Virulence medicine.disease_cause Biochemistry DNA-binding protein Type three secretion system Drug Discovery medicine Humans Molecular Biology Transcription factor biology Pseudomonas aeruginosa Chemistry Organic Chemistry biology.organism_classification In vitro Pseudomonadales Microsomes Liver Molecular Medicine Benzimidazoles Transcription Factors Pseudomonadaceae |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 20:3380-3383 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2010.04.014 |
| Popis: | ExsA is a multiple adaptational response (MAR) transcription factor, regulating the expression of a virulence determinant, the type III secretion system (T3SS) in Pseudomonas aeruginosa. Non-cytotoxic, non-antibacterial N-hydroxybenzimidazoles were identified as effective inhibitors of ExsA-DNA binding, and their potential utility as anti-virulence agents for P. aeruginosa was demonstrated in a whole cell assay. Select N-hydroxybenzimidazole inhibitors were stable in an in vitro human liver microsomal assay. |
| Databáze: | OpenAIRE |
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