Hashimoto Y, Shudo K
Institute of Applied Microbiology, University of Tokyo.
Jpn J Cancer Res. 1991 Jun;82(6):665-75. doi: 10.1111/j.1349-7006.1991.tb01902.x.
Suspension-cultured HeLa cells possess a cytosolic-nuclear tumor promoter-specific binding protein (CN-TPBP) which lacks protein kinase C activity. This CN-TPBP existed in cytosol of HeLa cells, but translocated into nuclear fraction of the cells after treatment of the cells with 12-O-tetradecanoylphorbol 13-acetate (TPA). The translocation of CN-TPBP induced by TPA became apparent within 10 min after the treatment with TPA, and was completed within 3 h. CN-TPBP bound TPA with the association constant of 1.4 x 10(10) M-1, and also bound teleocidin B, debromoaplysiatoxin, and thapsigargin in a mutually competitive manner. The binding affinity order of synthetic analogs of teleocidin B correlated with the adhesion-inducing potency order of the compounds toward human leukemia cell line HL-60. The apparent molecular weight of CN-TPBP under non-denaturing conditions was estimated to be 66-68 kDa. CN-TPBP forms a complex with the 90 kDa heat shock protein, and the complex was stabilized by the presence of molybdate. These characteristics of CN-TPBP are similar to those of the nuclear receptors of glucocorticoid and dioxin. These findings suggested that CN-TPBP acts as a nuclear receptor for tumor promoters, and that tumor promoters may exert their biological effects by binding to CN-TPBP.
悬浮培养的HeLa细胞拥有一种缺乏蛋白激酶C活性的胞质-核肿瘤启动子特异性结合蛋白(CN-TPBP)。这种CN-TPBP存在于HeLa细胞的胞质中,但在用12-O-十四烷酰佛波醇13-乙酸酯(TPA)处理细胞后会转移到细胞核部分。TPA诱导的CN-TPBP转移在TPA处理后10分钟内变得明显,并在3小时内完成。CN-TPBP与TPA结合,结合常数为1.4×10(10) M-1,并且还以相互竞争的方式结合teleocidin B、脱溴海兔毒素和毒胡萝卜素。teleocidin B的合成类似物的结合亲和力顺序与化合物对人白血病细胞系HL-60的粘附诱导能力顺序相关。在非变性条件下,CN-TPBP的表观分子量估计为66-68 kDa。CN-TPBP与90 kDa热休克蛋白形成复合物,并且该复合物在钼酸盐存在下得以稳定。CN-TPBP的这些特征与糖皮质激素和二恶英的核受体相似。这些发现表明CN-TPBP作为肿瘤启动子的核受体发挥作用,并且肿瘤启动子可能通过与CN-TPBP结合来发挥其生物学效应。