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Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK).
Authors: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
Affiliation:Metabolic & Cardiovascular Diesases Research, Novartis Institute for Biomedical Research, Summit, NJ 07901, USA.
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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