Náray A
Biochim Biophys Acta. 1983 Apr 20;756(3):328-34. doi: 10.1016/0304-4165(83)90341-0.
The effect of sodium molybdate on the stability and activation of the glucocorticoid receptor from chick and rat thymus were investigated. Molybdate, at a concentration range of 1-10 mM, blocked denaturation of the cytosol receptor by elevated (25 and 37 degrees C) temperatures. This effect could be observed only with the aggregated (low-salt) form of the receptor. Molybdate also inhibited transformation of the receptor-hormone complex to the DNA-binding state which occurs either with incubation at 25 degrees C or with salt treatment. The inhibitory effect of molybdate could be observed only on the non-activated receptor; nuclear-and DNA-binding of the activated receptor was not significantly changed by molybdate. Both effects were concentration-dependent. Molybdate had no effect on the activation of the partially purified glucocorticoid receptor. Molybdate effect was also examined using intact lymphocytes. Sodium molybdate had no effect either on the steroid binding of whole cells or on the nuclear transfer of the hormone-receptor complex. While the mechanism of molybdate action remains unknown the results of experiments on purified receptor suggest that molybdate does not act directly on the receptor molecule; rather through some cytosol factor(s). However, these effects could only be seen in cell-free experiments, and not during the conditions of the living cell.
研究了钼酸钠对鸡和大鼠胸腺糖皮质激素受体稳定性及活化的影响。钼酸钠浓度在1 - 10 mM范围内,可阻止在升高温度(25和37摄氏度)下胞质受体的变性。仅在受体的聚集(低盐)形式中可观察到这种效应。钼酸钠还抑制受体 - 激素复合物向DNA结合状态的转变,这种转变在25摄氏度孵育或盐处理时会发生。钼酸钠的抑制作用仅在未活化的受体上可观察到;钼酸钠对活化受体的核结合和DNA结合没有显著影响。这两种效应均呈浓度依赖性。钼酸钠对部分纯化的糖皮质激素受体的活化没有影响。还使用完整淋巴细胞检测了钼酸钠的作用。钼酸钠对全细胞的类固醇结合或激素 - 受体复合物的核转运均无影响。虽然钼酸钠的作用机制尚不清楚,但对纯化受体的实验结果表明,钼酸钠并非直接作用于受体分子;而是通过某些胞质因子起作用。然而,这些效应仅在无细胞实验中可见,在活细胞条件下则不然。