title: Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK).
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.
authors.affiliation: Metabolic & Cardiovascular Diesases Research, Novartis Institute for Biomedical Research, Summit, NJ 07901, USA.
authors.forename: T D
authors.initials: TD
authors.lastname: Aicher
authors.forename: R E
authors.initials: RE
authors.lastname: Damon
authors.forename: J
authors.initials: J
authors.lastname: Koletar
authors.forename: C C
authors.initials: CC
authors.lastname: Vinluan
authors.forename: L J
authors.initials: LJ
authors.lastname: Brand
authors.forename: J
authors.initials: J
authors.lastname: Gao
authors.forename: S S
authors.initials: SS
authors.lastname: Shetty
authors.forename: E L
authors.initials: EL
authors.lastname: Kaplan
authors.forename: W R
authors.initials: WR
authors.lastname: Mann
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001786:Blood Glucose / Q000187:drug effects; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy / Q000378:metabolism; D004195:Disease Models, Animal; D004224:Diterpenes / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D051379:Mice; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases; D017346:Protein Serine-Threonine Kinases; D000081382:Pyruvate Dehydrogenase Acetyl-Transferring Kinase; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D001786:Blood Glucose; D004224:Diterpenes; D047428:Protein Kinase Inhibitors; D000081382:Pyruvate Dehydrogenase Acetyl-Transferring Kinase; D014315:Triterpenes; D011494:Protein Kinases; D017346:Protein Serine-Threonine Kinases