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抗雌激素ICI 182780会破坏雌激素受体的核质穿梭。

The antiestrogen ICI 182780 disrupts estrogen receptor nucleocytoplasmic shuttling.

作者信息

Dauvois S, White R, Parker M G

机构信息

Molecular Endocrinology Laboratory, Imperial Cancer Research Fund, Lincoln's Inn Fields, London, UK.

出版信息

J Cell Sci. 1993 Dec;106 ( Pt 4):1377-88. doi: 10.1242/jcs.106.4.1377.

DOI:10.1242/jcs.106.4.1377
PMID:8126115
Abstract

The mouse estrogen receptor was shown to be constantly shuttling between the nucleus and cytoplasm although under steady-state conditions it is detected predominantly in the cell nucleus in both the absence and presence of estradiol. Shuttling was demonstrated by monitoring the transfer of protein between nuclei in heterokaryons and by examining the subcellular distribution of mutant receptors. In the presence of the partial antiestrogen 4-hydroxytamoxifen the receptor was retained in the nucleus whereas it accumulated in the cytoplasm when cells were treated with the pure antiestrogen ICI 182780. The effect of the pure antiestrogen was to inhibit nucleocytoplasmic shuttling of the receptor by blocking its nuclear uptake. Thus although ligand binding is not required by the estrogen receptor to undergo nucleocytoplasmic shuttling, this process can be disrupted by the binding of a pure antiestrogen.

摘要

已表明,小鼠雌激素受体在细胞核与细胞质之间不断穿梭,尽管在稳态条件下,无论有无雌二醇,它主要在细胞核中被检测到。通过监测异核体中核间蛋白质的转移以及检查突变受体的亚细胞分布,证实了穿梭现象。在存在部分抗雌激素4-羟基他莫昔芬的情况下,受体保留在细胞核中,而当细胞用纯抗雌激素ICI 182780处理时,它则在细胞质中积累。纯抗雌激素的作用是通过阻断其核摄取来抑制受体的核质穿梭。因此,尽管雌激素受体进行核质穿梭不需要配体结合,但这个过程可以被纯抗雌激素的结合所破坏。

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The antiestrogen ICI 182780 disrupts estrogen receptor nucleocytoplasmic shuttling.抗雌激素ICI 182780会破坏雌激素受体的核质穿梭。
J Cell Sci. 1993 Dec;106 ( Pt 4):1377-88. doi: 10.1242/jcs.106.4.1377.
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Inhibition of estrogen receptor-DNA binding by the "pure" antiestrogen ICI 164,384 appears to be mediated by impaired receptor dimerization.“纯”抗雌激素ICI 164,384对雌激素受体与DNA结合的抑制作用似乎是由受体二聚化受损介导的。
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An estrogen receptor positive MCF-7 clone that is resistant to antiestrogens and estradiol.一种对抗雌激素和雌二醇具有抗性的雌激素受体阳性MCF-7克隆。
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Expression of human estrogen receptor using an efficient adenoviral gene delivery system is able to restore hormone-dependent features to estrogen receptor-negative breast carcinoma cells.使用高效腺病毒基因递送系统表达人雌激素受体能够使雌激素受体阴性乳腺癌细胞恢复激素依赖性特征。
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