Activation of protein kinase C by non-phorbol tumor promoter, mezerein.
Mezerein, classified as a second-stage tumor promoter, has no diacylglycerol-like structure in its molecule, but can activate protein kinase C both in vitro and in vivo. This non-phorbol diterpene competitively inhibits the specific binding of a radioactive tumor-promoting phorbol ester to the enzyme. It is suggestive that tumor-promoting phorbol esters and mezerein cause analogous changes in the membrane to activate protein kinase C, and utilize this protein kinase as a common receptive protein for tumor promotion.
D000818:Animals; D001921:Brain / Q000201:enzymology*; D002273:Carcinogens / Q000494:pharmacology*; D004224:Diterpenes; D004789:Enzyme Activation / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D015240:Phorbol 12,13-Dibutyrate; D010703:Phorbol Esters / Q000378:metabolism; D010743:Phospholipids / Q000494:pharmacology; D011485:Protein Binding; D011493:Protein Kinase C; D011494:Protein Kinases / Q000378:metabolism*; D051381:Rats; D013329:Structure-Activity Relationship; D013729:Terpenes / Q000494:pharmacology*; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology
D002273:Carcinogens; D004224:Diterpenes; D010703:Phorbol Esters; D010743:Phospholipids; D013729:Terpenes; C011309:mezerein; D015240:Phorbol 12,13-Dibutyrate; D011494:Protein Kinases; D011493:Protein Kinase C; D013755:Tetradecanoylphorbol Acetate