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Potent and Specific Inhibitors of Protein Kinase C of Microbial Origin

Bio/Technology volume 8, pages 732735 (1990) | Download Citation

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Abstract

Potent and specific inhibitors of protein kinase C have been found in streptomyces and fungi: Staurosporine, an alkaloid from Streptomyces sp., is the most potent inhibitor of protein kinases with an IC50 in the nanomolar range. UCN-01 (7-hydroxy staurosporine), isolated from Streptomyces sp., is a selective inhibitor of protein kinase C with antitumor activity. Calphostin, isolated from the fungus Cladosporium cladosporioides, specifically inhibits protein kinase C (IC50 = 0.05 μM) without inhibiting other protein kinases. Microbial metabolites appear to be a promising source of inhibitors that target signal transduction pathways of eukaryotes.

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  1. Kyowa Hakko Co. Ltd., Tokyo Research Laboratories, 3-6-6, Asahimachi, Machida-shi, Tokyo 194, Japan

    • Tatsuya Tamaoki
    •  & Hirofumi Nakano

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DOI

https://doi.org/10.1038/nbt0890-732