Binding of 2-hydroxyestradiol and 4-hydroxyestradiol to the estrogen receptor of MCF-7 cells in cytosolic extracts and in nuclei of intact cells.

N Schütze, G Vollmer, W Wünsche, A Grote, B Feit, R Knuppen
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引用次数: 12

Abstract

The catechol estrogens (CE), 2-hydroxyestradiol (2-OH-E2) and 4-hydroxyestradiol (4-OH-E2) were analyzed for their binding affinity to the estrogen receptor of MCF-7 cells. Applying a competitive binding assay to cytosols prepared from MCF-7 breast cancer cells, we measured a relative binding affinity of 23% (2-OH-E2) and 26% (4-OH-E2) compared to E2. Nuclear binding assays with the same cell line demonstrated a high specific binding with Kd's of 0.31 nM (2-OH-E2) and 0.21 nM (4-OH-E2). The relative binding affinity measured was 25% and 42% for 2-OH-E2 and 4-OH-E2, respectively. Based on this nuclear binding it can be concluded that the estrogen receptor occupied by CE is bound within the nucleus and might therefore be transcriptionally active.

2-羟基雌二醇和4-羟基雌二醇与MCF-7细胞雌激素受体在细胞质提取物和完整细胞细胞核中的结合。
分析了儿茶酚类雌激素(CE)、2-羟基雌二醇(2-OH-E2)和4-羟基雌二醇(4-OH-E2)与MCF-7细胞雌激素受体的结合亲和力。通过对MCF-7乳腺癌细胞制备的细胞溶胶进行竞争性结合实验,我们测量了与E2相比,MCF-7的相对结合亲和力分别为23% (2-OH-E2)和26% (4-OH-E2)。与同一细胞系的核结合实验表明,Kd值分别为0.31 nM (2-OH-E2)和0.21 nM (4-OH-E2)。测定的2-OH-E2和4-OH-E2的相对结合亲和力分别为25%和42%。基于这种核结合,可以得出结论,CE占据的雌激素受体在细胞核内结合,因此可能具有转录活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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