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Cell Chem Biol ; 26(9): 1274-1282.e4, 2019 09 19.
Artículo en Inglés | MEDLINE | ID: mdl-31279606

RESUMEN

Common approaches to antibiotic discovery include small-molecule screens for growth inhibition in target pathogens and screens for inhibitors of purified enzymes. These approaches have a shared intent of seeking to directly target a vital Achilles heel in a pathogen of interest. Here, we report the first screen against a sporulation pathway in a non-pathogenic bacterium as a means of discovering novel antibiotics-this effort has resulted in two important discoveries. First, we show that the sporulation program of Streptomyces venezuelae is exquisitely sensitive to numerous forms of DNA damage. Second, we have identified a DNA gyrase inhibitor. This molecule, EN-7, is active against pathogenic species that are resistant to ciprofloxacin and other clinically important antibiotics. We suggest that this strategy could be applied to other morphogenetic pathways in prokaryotes or eukaryotes as a means of identifying novel chemical matter having scientific and clinical utility.


Asunto(s)
Girasa de ADN/efectos de los fármacos , Descubrimiento de Drogas/métodos , Inhibidores de Topoisomerasa II/aislamiento & purificación , Antibacterianos/farmacología , Girasa de ADN/metabolismo , Pruebas de Sensibilidad Microbiana , Esporas Bacterianas/efectos de los fármacos , Streptomyces/efectos de los fármacos , Streptomyces/metabolismo , Inhibidores de Topoisomerasa II/metabolismo , Inhibidores de Topoisomerasa II/farmacología
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