Abstract
Bacterial phospho-N-acetylmuramyl-pentapeptide translocase (translocase I: EC 2.7.8.13) is a key enzyme in peptidoglycan biosynthesis, and a known target of antibiotics. Here we report a novel nucleoside inhibitor against translocase I, A-94964, isolated from the culture broth of the strain Streptomyces sp. SANK 60404. A-94964 inhibited bacterial translocase I with IC50 value of 1.1 microg/ml, and showed antimicrobial activities against Staphylococcus aureus and Enterococcus faecalis with MIC of 100 and 50 microg/ml, respectively. A-94964 did not show cytotoxicity against mammalian cell lines.
MeSH terms
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Anti-Bacterial Agents / isolation & purification*
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Anti-Bacterial Agents / pharmacology
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Bacteria / enzymology*
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Disaccharides / isolation & purification*
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Disaccharides / pharmacology
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Enzyme Inhibitors / isolation & purification*
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Enzyme Inhibitors / pharmacology
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HeLa Cells
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Humans
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Pyrimidine Nucleotides / isolation & purification*
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Pyrimidine Nucleotides / pharmacology
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Streptomyces / classification*
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Streptomyces / metabolism
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Transferases (Other Substituted Phosphate Groups) / antagonists & inhibitors*
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Tunicamycin / pharmacology
Substances
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A 94964
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Anti-Bacterial Agents
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Disaccharides
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Enzyme Inhibitors
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Pyrimidine Nucleotides
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Tunicamycin
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Transferases (Other Substituted Phosphate Groups)
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phospho-N-acetylmuramoyl pentapeptide transferase