LRET-based HTS of a small-compound library for inhibitors of bacterial RNA polymerase.
Assay Drug Dev Technol
; 5(6): 759-68, 2007 Dec.
Article
em En
| MEDLINE
| ID: mdl-18052851
ABSTRACT
Resistance mechanisms against whole classes of antibiotics are currently developing faster than research generates new structurally different biologically active agents. The demand for new antimicrobial drugs has not been matched by the speed of discovery. The interface between sigma and core of bacterial RNA polymerase offers an attractive target for drug discovery, and we have previously described the development of a very robust high-throughput assay for this target based on luminescence resonance energy transfer. Here we describe a semiautomated screen of a commercially available library (Chembridge, San Diego, CA) that led to the identification of four small molecules, two of which have activity in preventing in vitro transcription and growth of Escherichia coli.
Buscar no Google
Base de dados:
MEDLINE
Assunto principal:
Bactérias
/
RNA Polimerases Dirigidas por DNA
/
Inibidores Enzimáticos
/
Antibacterianos
Limite:
Humans
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article