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Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK)

1999; Elsevier BV; Volume: 9; Issue: 15 Linguagem: Inglês

10.1016/s0960-894x(99)00380-7

1464-3405

Thomas D. Aicher, Robert E. Damon, Judit Koletar, Christine C. Vinluan, Leonard Brand, Jiaping Gao, Suraj S. Shetty, Emma L. Kaplan, W. Mann,

Enzyme Catalysis and Immobilization

Several oximes of triterpenes with a 17-β 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 μmol/kg. However, the mechanism of the blood glucose lowering effect is likely unrelated to PDK inhibition.