TMC-66, a New Endothelin Converting Enzyme Inhibitor Produced by Streptomyces sp. A5008

A new endothelin converting enzyme (ECE) inhibitor, TMC-66 was isolated from the fermentation broth of Streptomyces sp. A5008. The structure of TMC-66 was elucidated by spectroscopic analyses to be a new member of benzo[a]naphthacenequinone class of antibiotics. TMC-66 had a highly selective inhibit...

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Bibliographic Details
Published in:Journal of antibiotics 1999/07/25, Vol.52(7), pp.607-612
Main Authors: ASAI, YASUYUKI, NONAKA, NOBUAKI, SUZUKI, SHIN-ICHI, NISHIO, MAKI, TAKAHASHI, KOHEI, SHIMA, HIDEAKI, OHMORI, KENJI, OHNUKI, TETSUO, KOMATSUBARA, SABURO
Format: Article
Language:English
Subjects:
Animals
antibiotics
Antibiotics (antibacterial agents, antifungal agents)
Antibiotics, microbial producers, chemotherapic agents, antiseptics, disinfecting agents
Applied microbiology
Aspartic Acid Endopeptidases - antagonists & inhibitors
Biological and medical sciences
Chemical Phenomena
Chemistry, Physical
endothelin converting enzyme
endothelin converting enzyme inhibitors
Endothelin-Converting Enzymes
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Fermentation
Fundamental and applied biological sciences. Psychology
Lung - drug effects
Lung - enzymology
Metalloendopeptidases
Microbiology
Naphthacenes - chemistry
Naphthacenes - pharmacology
Protease Inhibitors - pharmacology
Rats
Streptomyces
Streptomyces - classification
Streptomyces - metabolism
TMC-66
Trypsin Inhibitors - pharmacology
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Description
Summary:A new endothelin converting enzyme (ECE) inhibitor, TMC-66 was isolated from the fermentation broth of Streptomyces sp. A5008. The structure of TMC-66 was elucidated by spectroscopic analyses to be a new member of benzo[a]naphthacenequinone class of antibiotics. TMC-66 had a highly selective inhibitory activity for ECE with an IC50 value of 2.9μM. Taxonomy of the producing strain is also described.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.52.607