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  • Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK).

Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK).

Bioorganic & medicinal chemistry letters (1999-08-28)
T D Aicher, R E Damon, J Koletar, C C Vinluan, L J Brand, J Gao, S S Shetty, E L Kaplan, W R Mann
ABSTRACT

Several oximes of triterpenes with a 17-beta hydroxyl and abietane derivatives are inhibitors of pyruvate dehydrogenase kinase (PDK) activity. The oxime 12 and dehydroabietyl amine 2 exhibit a blood glucose lowering effect in the diabetic ob/ob mouse after a single oral dose of 100 micromol/kg. However, the mechanism of the blood glucose lowering effect is likely unrelated to PDK inhibition.

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Pyruvate Dehydrogenase from porcine heart, buffered aqueous glycerol solution, 0.1-1.0 units/mg protein (Lowry)
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