| Autor: |
Charlotte E. Mardle, Layla R. Goddard, Bailei C. Spelman, Helen S. Atkins, Louise E. Butt, Paul A. Cox, Darren M. Gowers, Helen A. Vincent, Anastasia J. Callaghan |
| Jazyk: |
angličtina |
| Rok vydání: |
2020 |
| Předmět: |
|
| Zdroj: |
Biochemistry and Biophysics Reports, Vol 23, Iss , Pp 100773- (2020) |
| Druh dokumentu: |
article |
| ISSN: |
2405-5808 |
| DOI: |
10.1016/j.bbrep.2020.100773 |
| Popis: |
Increasing resistance of bacteria to antibiotics is a serious global challenge and there is a need to unlock the potential of novel antibacterial targets. One such target is the essential prokaryotic endoribonuclease RNase E. Using a combination of in silico high-throughput screening and in vitro validation we have identified three novel small molecule inhibitors of RNase E that are active against RNase E from Escherichia coli, Francisella tularensis and Acinetobacter baumannii. Two of the inhibitors are non-natural small molecules that could be suitable as lead compounds for the development of broad-spectrum antibiotics targeting RNase E. The third small molecule inhibitor is glucosamine-6-phosphate, a precursor of bacterial cell envelope peptidoglycans and lipopolysaccharides, hinting at a novel metabolite-mediated mechanism of regulation of RNase E. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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