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钼酸钠对绿猴子宫雌激素和孕激素受体稳定作用的可逆性

Reversibility of the stabilization effect of sodium molybdate on uterine estrogen and progesterone receptors of the vervet monkey.

作者信息

Klein T, Potgieter H C, Spies J H, van der Watt J J, Savage N

出版信息

J Recept Res. 1985;5(4):267-95. doi: 10.3109/10799898509041883.

DOI:10.3109/10799898509041883
PMID:4057178
Abstract

Sodium molybdate affected the stability of vervet monkey (Cercopithecus aethiops pygerythrus) uterine estrogen (ER) and progesterone (PR) receptors. Yields of receptors were invariably higher (20-40%) when cytosols were prepared in the presence of 10mM sodium molybdate. No changes were observed in the binding affinities for the natural ligands as reflected in dissociation constants. Receptor-ligand association at 0 degrees C and 20 degrees C was not affected in the presence or absence of molybdate. Stability studies at 37 degrees C indicated both receptors to be more resistant to inactivation in the presence of molybdate. Dissociation of ER and PR was biphasic, indicating the existence of slow (SDC), as well as fast dissociating (FDC) complexes. Rate constants of dissociation were significantly affected by the presence of sodium molybdate. Although no significant changes in the sedimentation coefficients were observed, marked differences in the actual gradient profiles could be illustrated in the presence or absence of sodium molybdate. Observed effects could only be partially reversed in sedimentation dialysis experiments. Proteolytic inhibitors phenylmethylsulfonylfluoride (PMSF) and leupeptin had no inhibitive effect on the molybdate stabilization of ER and PR.

摘要

钼酸钠影响了绿猴(赤猴指名亚种)子宫雌激素(ER)和孕激素(PR)受体的稳定性。当在10mM钼酸钠存在的情况下制备胞质溶胶时,受体产量总是更高(20 - 40%)。解离常数反映出对天然配体的结合亲和力没有变化。在0摄氏度和20摄氏度时,无论有无钼酸钠存在,受体 - 配体结合均不受影响。在37摄氏度下的稳定性研究表明,两种受体在有钼酸钠存在时对失活更具抗性。ER和PR的解离是双相的,表明存在缓慢解离(SDC)以及快速解离(FDC)复合物。解离速率常数受到钼酸钠存在的显著影响。尽管未观察到沉降系数有显著变化,但在有或无钼酸钠存在的情况下,实际梯度分布存在明显差异。在沉降透析实验中,观察到的效应只能部分逆转。蛋白水解抑制剂苯甲基磺酰氟(PMSF)和亮抑酶肽对ER和PR的钼酸盐稳定作用没有抑制作用。

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