A-94964, a novel inhibitor of bacterial translocase I, produced by Streptomyces sp. SANK 60404. I. Taxonomy, isolation and biological activity.
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.
Murakami
Ryo
R
Exploratory Research Laboratories II, Daiichi-Sankyo Co., Ltd., 1-16-13 Kitakasai, Edogawa-ku, Tokyo 134-8630, Japan. murakami.ryo.bw@daiichisankyo.co.jp
Fujita
Yoko
Y
Kizuka
Masaaki
M
Kagawa
Tomoka
T
Muramatsu
Yasunori
Y
Miyakoshi
Shunichi
S
Takatsu
Toshio
T
Inukai
Masatoshi
M
D000900:Anti-Bacterial Agents / Q000302:isolation & purification* / Q000494:pharmacology; D001419:Bacteria / Q000201:enzymology*; D004187:Disaccharides / Q000302:isolation & purification* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000302:isolation & purification* / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D011742:Pyrimidine Nucleotides / Q000302:isolation & purification* / Q000494:pharmacology; D013302:Streptomyces / Q000145:classification* / Q000378:metabolism; D017855:Transferases (Other Substituted Phosphate Groups) / Q000037:antagonists & inhibitors*; D014415:Tunicamycin / Q000494:pharmacology
C535078:A 94964; D000900:Anti-Bacterial Agents; D004187:Disaccharides; D004791:Enzyme Inhibitors; D011742:Pyrimidine Nucleotides; D014415:Tunicamycin; D017855:Transferases (Other Substituted Phosphate Groups); C100130:phospho-N-acetylmuramoyl pentapeptide transferase