This study investigated the effects of E2, diethylstilbestrol (DES), antiestrogens, the phytoestrogen resveratrol, and the xenoestrogens octylphenol (OP), nonylphenol (NP), endosulfan, kepone, 2,3,4,5-tetrachlorobiphenyl-4-ol (HO-PCB-Cl(4)), bisphenol-A (BPA), and 2,2-bis-(p-hydroxyphenyl)-1,1,1-trichloroethane (HPTE) on induction of luciferase activity in breast cancer cells transfected with a construct (pSp1(3)) containing three tandem GC-rich Sp binding sites linked to luciferase and wild-type or variant ERalpha. The results showed that induction of luciferase activity was highly structure-dependent in both MCF-7 and MDA-MB-231 cells. Moreover, RNA interference assays using small inhibitory RNAs for Sp1, Sp3 and Sp4 also demonstrated structure-dependent differences in activation of ERalpha/Sp1, ERalpha/Sp3 and ERalpha/Sp4. These results demonstrate for the first time that various structural classes of ER ligands differentially activate wild-type and variant ERalpha/Sp-dependent transactivation, selectively use different Sp proteins, and exhibit selective ER modulator (SERM)-like activity.

译文

:这项研究调查了E2,己烯雌酚(DES),抗雌激素,植物雌激素白藜芦醇和异雌激素辛基苯酚(OP),壬基苯酚(NP),硫丹,酮酮,2,3,4,5-四氯联苯-4-醇的作用(HO-PCB-Cl(4)),双酚A(BPA)和2,2-双-(对羟基苯基)-1,1,1-三氯乙烷(HPTE)对乳腺癌细胞中萤光素酶活性的诱导作用用含有三个串联荧光富集的Sp结合位点的荧光素酶和野生型或变体ERalpha的构建体(pSp1(3))转染。结果表明,萤光素酶活性的诱导在MCF-7和MDA-MB-231细胞中都高度依赖结构。此外,使用针对Sp1,Sp3和Sp4的小抑制性RNA进行的RNA干扰分析还证明了ERalpha / Sp1,ERalpha / Sp3和ERalpha / Sp4激活中的结构依赖性差异。这些结果首次证明,各种结构类别的ER配体差异性激活野生型和变体ERalpha / Sp依赖性反式激活,选择性地使用不同的Sp蛋白,并表现出选择性的ER调节剂(SERM)样活性。

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