Marr W, White J O, Elder M G, Lim L
Biochem J. 1980 Jul 15;190(1):17-25. doi: 10.1042/bj1900017.
Oestrogen receptors were measured in the cytosolic and purified nuclear fractions of rat liver. Both cytosolic and nuclear receptors bind oestrogen with high affinity (Kd = 1.47 and 2.28 nM respectively) and specificity similar to that of receptors in order oestrogen-target tissues such as the uterus. During the 4-day oestrous cycle the receptor content and distribution between cytosol and nucleus did not vary; in particular, the content of nuclear receptor did not appear to fluctuate in concert with known cyclic changes in the concentration of plasma oestrogen. Injection of 50 micrograms of oestradiol-17 beta or 10 micrograms of ethynyloestradiol resulted in a 4--6-fold increase in the nuclear receptor content, with a concomitant decrease in the unoccupied-receptor content of cytosol 1 h after injection. The nuclear receptors present after injection bind oestrogens with similar affinity (Kd = 2.78 nM) and specificity to receptors present in uninjected animals. The administration of lower doses of either oestrogen was less effective in producing increases in nuclear receptor content. Hence there is apparently substantial translocation of receptor to the nucleus in response to hyperphysiological doses of oestrogen, but not to the physiological changes in plasma oestrogen concentrations during the oestrous cycle. The response to exogenous oestrogens is discussed in relation to the clinical use of synthetic oestrogens and progestogens.
在大鼠肝脏的胞质和纯化的核级分中测量雌激素受体。胞质和核受体均以高亲和力（分别为Kd = 1.47和2.28 nM）结合雌激素，其特异性与子宫等雌激素靶组织中的受体相似。在4天的发情周期中，受体含量以及在胞质和细胞核之间的分布没有变化；特别是，核受体的含量似乎并未随着血浆雌激素浓度已知的周期性变化而波动。注射50微克的17β-雌二醇或10微克的乙炔雌二醇导致核受体含量增加4至6倍，注射后1小时胞质中空位受体含量随之降低。注射后出现的核受体以与未注射动物中存在的受体相似的亲和力（Kd = 2.78 nM）和特异性结合雌激素。给予较低剂量的任何一种雌激素在增加核受体含量方面效果较差。因此，显然在超生理剂量的雌激素作用下，受体大量转运至细胞核，但在发情周期中对血浆雌激素浓度的生理变化无反应。结合合成雌激素和孕激素的临床应用讨论了对外源雌激素的反应。
