Shyamala G
Biochemistry. 1975 Jan 28;14(2):437-44. doi: 10.1021/bi00673a034.
The specific interaction of glucocorticoids with nuclei of mouse mammary tumor was studied in vitro by incubation of the tissue with [3H]dexamethasone at 25 degrees. It was demonstrated that the mammary tumors contain a limited number of specific nuclear binding sites which were saturated with low hormone concentrations (10-8 M)9 The concentrations of specific binding sites in the nuclei were related to the concentration of cytoplasmic binding sites of unincubated tissues and varied between individual tumors. The binding component in the nuclei appeared to be a protein and was easily solubilized with 0.4 M KCl containing buffers. The ability of various corticoids to block the nuclear localization of the steroid correlated well with their glucocorticoid potency. Estradiol and progesterone at concentrations of 10-6 M were also effective in competing for the glucocorticoid receptor binding sites. However, while the glucocorticoids such as hydrocortisone and corticosterone translocated to nuclear sites also specific for dexamethasone, estradiol and progesterone competed for the cytoplasmic binding sites and did not translocate to the nucleus. The possible significance of the interaction of various steroids with the glucocorticoid receptors in mammary tumors is discussed.
通过在25℃下将组织与[3H]地塞米松孵育,在体外研究了糖皮质激素与小鼠乳腺肿瘤细胞核的特异性相互作用。结果表明,乳腺肿瘤含有数量有限的特异性核结合位点,这些位点在低激素浓度(10-8M)时就会饱和。细胞核中特异性结合位点的浓度与未孵育组织细胞质结合位点的浓度相关,且在不同肿瘤个体之间有所变化。细胞核中的结合成分似乎是一种蛋白质,很容易用含0.4M氯化钾的缓冲液溶解。各种皮质激素阻断类固醇核定位的能力与其糖皮质激素效力密切相关。浓度为10-6M的雌二醇和孕酮在竞争糖皮质激素受体结合位点方面也有效。然而,虽然氢化可的松和皮质酮等糖皮质激素也会转运到对地塞米松特异的核位点,但雌二醇和孕酮竞争细胞质结合位点,并不转运到细胞核。文中讨论了各种类固醇与乳腺肿瘤中糖皮质激素受体相互作用的可能意义。