Aug 1, 1990

Potent and specific inhibitors of protein kinase C of microbial origin

T Tamaoki, H Nakano


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 microM) without inhibiting other protein kinases. Microbial metabolites appear to be a promising source of inhibitors that target signal transduction pathways of eukaryotes.

Mentioned in this Paper

Plant alkaloid
Filamentous fungus
Signal Transduction Pathways
Indole Alkaloids
Cladosporium cladosporioides extract
Protein KINASE

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