Characterization of the “Estrogenicity” of tamoxifen and raloxifene in HepG2 cells: Regulation of gene expression from an ERE controlled reporter vector versus regulation of the endogenous SHBG and PS2 genes
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Cited by (33)
Multigenerational effects of the anticancer drug tamoxifen and its metabolite 4-hydroxy-tamoxifen on Daphnia pulex
2016, Science of the Total EnvironmentPET imaging of oestrogen receptors in patients with breast cancer
2013, The Lancet OncologyThe aryl hydrocarbon receptor ligands 2,3,7,8-tetrachlorodibenzo-p-dioxin and 3-methylcholanthrene regulate distinct genetic networks
2012, Molecular and Cellular EndocrinologyCitation Excerpt :In order to systematically compare the effects of TCDD and 3-MC on ER signaling, we conducted a whole genome analysis of the transcriptional effects of TCDD and 3-MC, and compared it to the transcriptional response after treatment with diethylstilbestrol (DES), a well-characterized ER ligand. We analyzed gene expression profiles in HepG2 cells, a human hepatocellular carcinoma cell line, stably expressing ERα at moderate levels (HepG2-ERα, Barkhem et al., 1997). We chose this cell line because it endogenously expresses the AhR signaling machinery and exhibits high metabolic capacity towards 3-MC (Swedenborg et al., 2008) and other substances (Bursztyka et al., 2008).
An oestrogen receptor β-selective agonist exerts anti-neoplastic effects in experimental intrahepatic cholangiocarcinoma
2012, Digestive and Liver DiseaseAberrant estrogen regulation of PEMT results in choline deficiency-associated liver dysfunction
2011, Journal of Biological ChemistryCitation Excerpt :Using transcript-specific primer-probe sets and cDNA standards, we quantified the absolute level of expression of each transcript with and without treatment with the estrogen analog moxestrol. This synthetic estrogen was used because it is not subject to cytochrome P450 metabolism expected in primary hepatocytes (34, 35). Although transcript A was most abundant in unstimulated cells (∼7.5 × 105 copies/150 ng of cDNA), it was not induced at any time point tested (Fig. 2, A and D).
Interplay between Estrogen Response Element Sequence and Ligands Controls in Vivo Binding of Estrogen Receptor to Regulated Genes
2004, Journal of Biological ChemistryCitation Excerpt :OHT was a less effective activator of the cellular PI-9 gene (Fig. 2) than of the transfected PI-9 promoter (see Fig. 1B). 17β-Estradiol and Moxestrol Induce Similar Binding of ER to the PI-9 ERU and to the pS2 ERE—The prototypical estrogen, 17β-estradiol, is rapidly metabolized in HepG2 cells and other p450-containing liver cells (36, 42). Studies of hepatic gene regulation lasting more than a few hours therefore require the use of unacceptably high micromolar concentrations of E2 (42).