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