A-102395, a new inhibitor of bacterial translocase I, produced by Amycolatopsis sp. SANK 60206.
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 new nucleoside inhibitor for translocase I, A-102395, isolated from the culture broth of the strain Amycolatopsis sp. SANK 60206. A-102395 is a new derivative of capuramycin that has the benzene with a uniquely substituted chain instead of an aminocaprolactam. A-102395 is a potent inhibitor of bacterial translocase I with IC50 value of 11 nM, but possesses no antimicrobial activity against various strains tested.
Murakami
Ryo
R
Exploratory Research Laboratories II, Daiichi-Sankyo Co., Ltd, Edogawa-ku, Tokyo, 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
D000617:Aminoglycosides / Q000737:chemistry / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003470:Culture Media / Q000737:chemistry; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005285:Fermentation; D006094:Gram-Positive Bacteria / Q000145:classification / Q000378:metabolism*; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D008968:Molecular Conformation; D013056:Spectrophotometry, Ultraviolet; D017855:Transferases (Other Substituted Phosphate Groups) / Q000037:antagonists & inhibitors*
C527229:A-102395; D000617:Aminoglycosides; D003470:Culture Media; D004791:Enzyme Inhibitors; C049983:capuramycin; D017855:Transferases (Other Substituted Phosphate Groups); C100130:phospho-N-acetylmuramoyl pentapeptide transferase