NUCLEAR BINDING AND RETENTION OF RECEPTOR ESTROGEN COMPLEX - RELATION TO AGONISTIC AND ANTAGONISTIC PROPERTIES OF ESTRIOL
NUCLEAR BINDING AND RETENTION OF RECEPTOR ESTROGEN COMPLEX - RELATION TO AGONISTIC AND ANTAGONISTIC PROPERTIES OF ESTRIOL
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DOI：
10.1210/endo-100-1-91
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发表时间：
1977-01-01
期刊：
影响因子：
4.8
通讯作者：
PECK, EJ
中科院分区：
文献类型：
--
作者：
CLARK, JH;PASZKO, Z;PECK, EJ
[在大鼠中]检查了受体雌激素复合物的核保留或驻留与雌三醇的激动和拮抗特性之间的关系。用雌二醇（E2）、雌三醇（E3）或两种激素（E2和E3）治疗后24和48 h，测量细胞质雌激素受体（Rc）和子宫重量。在任何时间，所有组的Rc水平均升高。由于Rc水平在每种情况下均高于对照组，因此Rc似乎不是雌三醇拮抗作用的限制因素。这些类固醇的核受体雌激素复合物（RnE）的易位和保留的影响进行了检查。按上述方法注射大鼠，并在注射后1、3和6 h通过[3H]雌二醇交换测定RnE。所有处理均引起受体向核室的等量易位。到6 h，E2处理动物中存在的Rn量显著高于对照组，而E2 + E3动物中的Rn量居中。E3单独未能引起显着的核保留的Rn。这些保留模式与上述重量和细胞质受体反应相关，并表明RnE3复合物的短核驻留时间与E3的拮抗作用有关。为了测试这一点，这些雌激素通过石蜡颗粒给药，以维持每种激素的血液水平。Rn水平在植入后24和48 h升高，治疗组之间无显著差异。生长反应无差异。在所有3例病例中，子宫重量均受到高度刺激（高于对照组300%）。由于RnE3复合物的核滞留时间短，E3可能作为雌激素拮抗剂注射时作为一个团。当E3持续存在且RnE3升高并维持时，E3是一种没有拮抗特性的强效雌激素。
The relationship between nuclear retention or residency of receptor estrogen complexes and the agonistic and antagonistic properties of estriol was examined [in rats]. Cytoplasmic estrogen receptor (Rc) and uterine weight were measured 24 and 48 h after treatment with estradiol (E2), estriol (E3) or both hormones (E2 and E3). Levels of Rc were elevated in all groups at either time. Since levels of Rc were above control in each case, Rc does not appear to be the limiting factor in the antagonistic effect of estriol. The effect of these steroids on translocation and retention of nuclear receptor estrogen complexes (RnE) was examined. Rats were injected as above and RnE measured by [3H]estradiol exchange 1, 3 and 6 h after injection. All treatments cause equal translocation of receptor to the nuclear compartment. By 6 h the quantity of Rn present in E2 treated animals was significantly above controls, while that in E2 + E3 animals was intermediate. E3 alone failed to cause significant nuclear retention of Rn. These patterns of retention correlate with the weight and cytoplasmic receptor responses above and suggest that the short nuclear residency time of RnE3 complexes relates to the antagonism of E3. To test this, these estrogens were administered via paraffin pellets to maintain blood levels of each hormone. Levels of Rn were elevated 24 and 48 h after implant with no significant differences between treatment groups. There were no differences in the growth response. Uterine weights were highly stimulated in all 3 cases (300% above control). E3 probably acts as an estrogen antagonist when injected as a bolus because of the short nuclear retention time of RnE3 complexes. When E3 is present continuously and RnE3 is elevated and maintained, E3 is a potent estrogen without antagonistic properties.