期刊
SCIENCE
卷 321, 期 5896, 页码 1673-1675出版社
AMER ASSOC ADVANCEMENT SCIENCE
DOI: 10.1126/science.1159961
关键词
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资金
- L. Clay and East Hill Management (Boston, MA, USA)
- Wellcome Trust under the Seeding Drug Discovery Initiative
- UK Biotechnology and Biological Sciences Research Council
- UK Department of Trade and Industry
- [AppGen55]
FtsZ is an essential bacterial guanosine triphosphatase and homolog of mammalian beta-tubulin that polymerizes and assembles into a ring to initiate cell division. We have created a class of small synthetic antibacterials, exemplified by PC190723, which inhibits FtsZ and prevents cell division. PC190723 has potent and selective in vitro bactericidal activity against staphylococci, including methicillin- and multi- drug- resistant Staphylococcus aureus. The putative inhibitor- binding site of PC190723 was mapped to a region of FtsZ that is analogous to the Taxol- binding site of tubulin. PC190723 was efficacious in an in vivo model of infection, curing mice infected with a lethal dose of S. aureus. The data validate FtsZ as a target for antibacterial intervention and identify PC190723 as suitable for optimization into a new anti- staphylococcal therapy.
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