Molybdate inhibition of glucocorticoid receptor inactivation and transformation.
Molybdate inhibition of glucocorticoid receptor inactivation and transformation.
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钼酸盐抑制糖皮质激素受体失活和转化。
DOI：
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发表时间：
1979
影响因子：
4.8
通讯作者：
W. Pratt
中科院分区：
文献类型：
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作者：
K. Leach;M. Dahmer;N. Hammond;J. J. Sando;W. Pratt
当胞浆在25摄氏度加热时，糖皮质激素受体的失活被钼酸盐可逆地阻断，并被其他一些磷酸酶抑制剂如氟化物和葡萄糖1-磷酸减缓。钼酸盐还可以防止因0℃的盐暴露或硫酸铵沉淀而导致的非结合受体失活，这三种抑制剂都可以防止Sephadex G-50凝胶过滤引起的非结合受体失活。钼酸盐和钨酸盐都能阻断糖皮质激素受体复合体向DNA结合态的依赖温度的转变，而氟化物和葡萄糖1-磷酸对此没有影响。在0摄氏度时，盐、硫酸铵沉淀或凝胶过滤引起的转变也会被钼酸盐和钨酸盐阻止。钨酸盐与钼酸盐的不同之处在于，它对受体失活几乎没有影响。氟化物和1-磷酸葡萄糖不抑制转化。这些观察结果支持钼酸盐和钨酸盐通过与糖皮质激素受体本身的可逆联系而相互作用的假设。我们认为，它们可能通过与受体上的磷酸部分形成复合体来发挥作用。
The inactivation of glucocorticoid receptors that occurs when cytosol is heated at 25 degrees C is blocked reversibly by molybdate and slowed by some other phosphatase inhibitors such as fluoride and glucose 1-phosphate. Molybdate is also capable of preventing nonenzymatic inactivation of unbound receptors caused by exposure to salt or precipitation with ammonium sulfate at 0 degrees C. Inactivation of unbound receptors caused by Sephadex G-50 gel filtration is prevented by all three inhibitors. Both molybdate and tungstate block temperature-dependent transformation of glucocorticoid.receptor complexes to the DNA-binding state, where fluoride and glucose 1-phosphate have no effect. Transformation brought about at 0 degrees C by salt, ammonium sulfate precipitation, or gel filtration is also blocked by both molybdate and tungstate. Tungstate differs from molybdate in that it has little or no effect on receptor inactivation. Fluoride and glucose 1-phosphate do not inhibit transformation. These observations support the proposal that molybdate and tungstate are interacting through a reversible association with the glucocorticoid receptor itself. We propose that they may act by forming a complex with a phosphate moiety on the receptor.