TMC-66 is a novel benzo[a]naphthacenequinone compound isolated from Streptomyces sp. A5008 that demonstrates highly selective, competitive inhibition of endothelin converting enzyme.
TMC-66 may serve as a lead for ECE inhibitor development; leaves open translation to human cardiovascular applications.
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 2.9 microM. Taxonomy of the producing strain is also described.
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Asai et al. (1999) studied this question.
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