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Science. 2008 Sep 19;321(5896):1673-5. doi: 10.1126/science.1159961.

An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.

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1
Prolysis, Begbroke Science Park, Oxfordshire OX5 1PF, UK.

Abstract

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.

PMID:
18801997
DOI:
10.1126/science.1159961
[Indexed for MEDLINE]
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