Martel P, Houdebine L M, Teyssot B, Djiane J
Biol Cell. 1983;49(2):119-26. doi: 10.1111/j.1768-322x.1984.tb00229.x.
Three phorbol esters: phorbol-12,13-dibutyrate (PDB), 12-0-tetradecanoylphorbol-13-acetate (TPA) and phorbol-12,13-diacetate (PDA) were added at various concentrations (10(1)-10(4) ng/ml) to the culture medium of rabbit mammary explants. The three phorbol esters inhibited the mitogenic signals of insulin, EGF and prolactin. They also prevented the induction of casein synthesis and casein mRNA accumulation by prolactin. In all cases, the most potent inhibitor was PDB. PDB did not alter the binding of prolactin to its receptors. The three phorbol esters added to mammary cell membranes with prolactin prevented the generation of the hormonal relay which specifically stimulates casein gene transcription when added to isolated nuclei. These data suggest that phorbol esters act directly at the membrane level where they interrupt the transfer of the hormonal messages, through a mechanism which may not be related to their promoter potency.
佛波醇 -12,13 - 二丁酸酯（PDB）、12 - O - 十四烷酰佛波醇 -13 - 乙酸酯（TPA）和佛波醇 -12,13 - 二乙酸酯（PDA）以不同浓度（10¹ - 10⁴ ng/ml）添加到兔乳腺外植体的培养基中。这三种佛波酯抑制胰岛素、表皮生长因子（EGF）和催乳素的促有丝分裂信号。它们还阻止催乳素诱导酪蛋白合成和酪蛋白mRNA积累。在所有情况下，最有效的抑制剂是PDB。PDB不会改变催乳素与其受体的结合。将这三种佛波酯与催乳素一起添加到乳腺细胞膜中，可阻止激素信号传递的产生，而当将其添加到分离的细胞核中时，该信号传递会特异性刺激酪蛋白基因转录。这些数据表明，佛波酯直接作用于膜水平，通过一种可能与其启动子活性无关的机制中断激素信息的传递。
