Interaction of Estrogenic Chemicals and Phytoestrogens with Estrogen Receptor β.
Interaction of Estrogenic Chemicals and Phytoestrogens with Estrogen Receptor β.
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DOI：
10.1210/endo.139.10.6216
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发表时间：
1998-10
期刊：
影响因子：
4.8
通讯作者：
G. Kuiper;J. Lemmen;B. Carlsson;J. Corton;S. Safe;P. T. van der Saag;B. van der Burg;J. Gustafsson-J.-Gus
中科院分区：
文献类型：
--
作者：
G. Kuiper;J. Lemmen;B. Carlsson;J. Corton;S. Safe;P. T. van der Saag;B. van der Burg;J. Gustafsson-J.-Gus
大鼠、小鼠和人雌激素受体（ER）存在两种亚型，ERα和ERβ，其在C-末端配体结合结构域和N-末端反式激活结构域中不同。在这项研究中，我们研究了环境化学品和植物雌激素的雌激素活性与ERα或ERβ蛋白的竞争结合试验，并在瞬时基因表达试验中使用细胞，其中通过在雌激素依赖性报告质粒的存在下与重组人ERα或ERβ互补DNA（cDNA）共转染培养物产生急性雌激素反应。人ERα和ERβ蛋白的饱和配基结合分析显示，[3 H]-17β-雌二醇（E2）具有高亲和力的单一结合组分[解离常数（Kd）= 0.05 - 0.1 nm]。所有环境雌激素化学品[多氯羟基联苯、二氯二苯三氯乙烷（DDT）及其衍生物、烷基酚、双酚A、甲氧滴滴涕和十氯酮]都与E2竞争结合雌激素受体的两种亚型，并具有...
The rat, mouse and human estrogen receptor (ER) exists as two subtypes, ERα and ERβ, which differ in the C-terminal ligand-binding domain and in the N-terminal transactivation domain. In this study, we investigated the estrogenic activity of environmental chemicals and phytoestrogens in competition binding assays with ERα or ERβ protein, and in a transient gene expression assay using cells in which an acute estrogenic response is created by cotransfecting cultures with recombinant human ERα or ERβ complementary DNA (cDNA) in the presence of an estrogen-dependent reporter plasmid. Saturation ligand-binding analysis of human ERα and ERβ protein revealed a single binding component for[ 3H]-17β-estradiol (E2) with high affinity[ dissociation constant (Kd) = 0.05 - 0.1 nm]. All environmental estrogenic chemicals [polychlorinated hydroxybiphenyls, dichlorodiphenyltrichloroethane (DDT) and derivatives, alkylphenols, bisphenol A, methoxychlor and chlordecone] compete with E2 for binding to both ER subtypes with a...