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

Aicher, T D; Damon, R E; Koletar, J; Vinluan, C C; Brand, L J; Gao, J; Shetty, S S; Kaplan, E L; Mann, W R.

Bioorg Med Chem Lett ; 9(15): 2223-8, 1999 Aug 02.

Article in English | MEDLINE | ID: mdl-10465550

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.

Subject(s)

Diterpenes/chemical synthesis , Protein Kinase Inhibitors , Protein Kinases , Triterpenes/chemical synthesis , Administration, Oral , Animals , Blood Glucose/drug effects , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Experimental/metabolism , Disease Models, Animal , Diterpenes/pharmacology , Diterpenes/therapeutic use , Mice , Protein Serine-Threonine Kinases , Pyruvate Dehydrogenase Acetyl-Transferring Kinase , Rats , Rats, Sprague-Dawley , Structure-Activity Relationship , Triterpenes/pharmacology , Triterpenes/therapeutic use

ABSTRACT

Subject(s)

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