Miyake R, Tanaka Y, Tsuda T, Kaibuchi K, Kikkawa U, Nishizuka Y
Biochem Biophys Res Commun. 1984 Jun 15;121(2):649-56. doi: 10.1016/0006-291x(84)90231-6.
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.
狼毒大戟素被归类为第二阶段肿瘤促进剂,其分子中没有二酰基甘油样结构,但在体外和体内均可激活蛋白激酶C。这种非佛波醇二萜可竞争性抑制放射性肿瘤促进佛波酯与该酶的特异性结合。这表明肿瘤促进佛波酯和狼毒大戟素在膜上引起类似变化以激活蛋白激酶C,并将这种蛋白激酶用作肿瘤促进的共同受体蛋白。