Katsuoka Y, Hoshino H, Shiramizu M, Sakabe K, Seiki K
Urology. 1986 Sep;28(3):228-31. doi: 10.1016/0090-4295(86)90048-8.
For basic studies of receptor dynamics in androgen-responsive tissues and cells, the autoradiographic and cytochemical procedures were applied to cultured tumor cells (DU-145 and PC-3). Uptake and retention of 3H-R1881, a potent synthetic androgen, were observed in DU-145 cells. The radioactive labelling was intense, and solely confined to the nuclei of DU-145 cells. Radioactivity over PC-3 cells was minimal. For assessing binding specificity, DU-145 cells were incubated with 3H-R1881 in the presence or absence of either unlabelled R1881, testosterone, progesterone, estradiol-17 beta, or corticosterone. The displacement of 3H-R1881 with R1881 and testosterone was significant, while no displacement was observed with other steroids. Nuclear localization of cytochemical staining of the dihydrotestosterone-peroxidase conjugate was evident in DU-145 cells. Our results indicate that androgen receptor may reside primarily in target cell nuclei of androgen-responsive tissues and tumors.
为了对雄激素反应性组织和细胞中的受体动力学进行基础研究,将放射自显影和细胞化学方法应用于培养的肿瘤细胞(DU-145和PC-3)。在DU-145细胞中观察到强效合成雄激素3H-R1881的摄取和保留。放射性标记强烈,且仅局限于DU-145细胞的细胞核。PC-3细胞上的放射性极少。为了评估结合特异性,将DU-145细胞与3H-R1881在有无未标记的R1881、睾酮、孕酮、雌二醇-17β或皮质酮的情况下孵育。R1881和睾酮对3H-R1881的置换作用显著,而其他类固醇未观察到置换作用。在DU-145细胞中,二氢睾酮-过氧化物酶结合物的细胞化学染色在细胞核中的定位很明显。我们的结果表明,雄激素受体可能主要存在于雄激素反应性组织和肿瘤的靶细胞核中。