Protein Information

Name estrogen receptors
Synonyms ER; ERA; ER alpha; ERalpha; ESR; ESR 1; ESR1; ESRA…

Compound Information

Name DDT
CAS 1,1′-(2,2,2-trichloroethylidene)bis[4-chlorobenzene]

Reference List

PubMed Abstract RScore(About this table)
16329587 Liu GH, Yang KD, Liu XP, Qin QF: [Effects of residues of organochlorine pesticides on reproductive endocrine in human]. Wei Sheng Yan Jiu. 2005 Sep;34(5):524-8.


However, the hormones, for example, LH in the women blood and P in the cords blood decreased respectively with the rising pesticides' levels and an obvious dose-effect relationship was found. (2) The expressional abundances of alpha-estrogen receptor (alpha-ER), beta-endorphin (beta-EP) and gonadotropin releasing hormone (GnRH) in the placentae and alpha-ER and beta-EP in the cord tissues went up respectively in dose-effect manner following the rising pesticides' burdens. (3) The times of the previous adverse pregnancy outcomes increased with the increase of the residues' burdens and there were significant differences between the control and various residue groups, but the times in the high-residue was smaller than that in the mid-residue group (P < 0.01).
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15483189 Sonneveld E, Jansen HJ, Riteco JA, Brouwer A, van der Burg B: Development of androgen- and estrogen-responsive bioassays, members of a panel of human cell line-based highly selective steroid-responsive bioassays. Toxicol Sci. 2005 Jan;83(1):136-48. Epub 2004 Oct 13.


We have established highly sensitive and specific androgen and estrogen reporter cell lines which we have named AR (androgen receptor) and ERalpha (estrogen receptor alpha) CALUX (Chemically Activated LUciferase eXpression), respectively.
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19766106 Rossi M, Dimida A, Ferrarini E, Silvano E, De Marco G, Agretti P, Aloisi G, Simoncini T, Di Bari L, Tonacchera M, Giorgi F, Maggio R: Presence of a putative steroidal allosteric site on glycoprotein hormone receptors. Eur J Pharmacol. 2009 Nov 25;623(1-3):155-9. Epub 2009 Sep 17.


The notion that all these compounds interfere with nuclear estrogen receptors, as either agonists (DDT and diethylstilbestrol) or antagonists (quercetin), prompted us to test the ability of the steroid hormone 17-beta-estradiol to inhibit the TSH receptor activity.
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15811583 Halldin K, Axelsson J, Brunstrom B: Effects of endocrine modulators on sexual differentiation and reproductive function in male Japanese quail. Brain Res Bull. 2005 Apr 15;65(3):211-8. Epub 2004 Dec 18.


Many of these compounds bind to estrogen receptors, thereby potentially disrupting estrogen-regulated functions.
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16705413 Noguerol TN, Boronat S, Casado M, Raldua D, Barcelo D, Pina B: Evaluating the interactions of vertebrate receptors with persistent pollutants and antifouling pesticides using recombinant yeast assays. Anal Bioanal Chem. 2006 Jul;385(6):1012-9. Epub 2006 May 17.


In this work we use two yeast systems to test the ability of different chemicals to bind and activate two vertebrate receptors which are intimately related to adverse biological effects of pollution in exposed fauna: the estrogen receptor (ER) and the aryl hydrocarbon receptor (AhR).
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15458791 Penza M, Bonetti E, Villa R, Ganzerla S, Bergonzi R, Biasiotto G, Caimi L, Apostoli P, Ciana P, Maggi A, Di Lorenzo D: Whole body action of xenoestrogens with different chemical structures in estrogen reporter male mice. Toxicology. 2004 Dec 1;205(1-2):65-73.


By a time dependent analysis of the transgenic reporter expression (luciferase), we showed that all these chemicals modulated the estrogen receptors (ERs) in the whole body, although with a different efficacy and depending upon the tissue analyzed.
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19478717 Roy JR, Chakraborty S, Chakraborty TR: Estrogen-like endocrine disrupting chemicals affecting puberty in humans--a review. Med Sci Monit. 2009 Jun;15(6):RA137-45.


The structural similarity of estrogen disruptors with estrogen allow them to bind and activate estrogen receptors and show a similar response even in the absence of estrogen that can lead to precocious puberty (PP).
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17984292 Kiyosawa N, Kwekel JC, Burgoon LD, Williams KJ, Tashiro C, Chittim B, Zacharewski TR: o,p'-DDT elicits PXR/CAR-, not ER-, mediated responses in the immature ovariectomized rat liver. Toxicol Sci. 2008 Feb;101(2):350-63. Epub 2007 Nov 5.


Few genes known to be estrogen receptor (ER) regulated were differentially expressed when compared to the hepatic gene expression profile elicited by ethynyl estradiol in immature ovariectomized C57BL/6 mice using the same study design and analysis methods.
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16199348 Murono EP, Derk RC: The reported active metabolite of methoxychlor, 2,2-bis (p-hydroxyphenyl)-1,1,1-trichloroethane, inhibits testosterone formation by cultured Leydig cells from neonatal rats. Reprod Toxicol. 2005 Nov-Dec;20(4):503-13.


In a recent study, HPTE was shown to inhibit both basal and hCG-stimulated testosterone production by cultured Leydig cells from immature and adult rats, and these effects were reported to be mediated through the estrogen receptor.
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16797915 Vanparys C, Maras M, Lenjou M, Robbens J, Van Bockstaele D, Blust R, De Coen W: Flow cytometric cell cycle analysis allows for rapid screening of estrogenicity in MCF-7 breast cancer cells. Toxicol In Vitro. 2006 Oct;20(7):1238-48. Epub 2006 May 16.


This flow cytometric proliferation assay confirms that the estrogenic activity of structurally analogous parabens is mediated by the estrogen receptor pathway and is proportional to the alkyl chain length.
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12948897 Kanno J, Onyon L, Peddada S, Ashby J, Jacob E, Owens W: The OECD program to validate the rat uterotrophic bioassay. Environ Health Perspect. 2003 Sep;111(12):1550-8.


Positive agonists of the estrogen receptor included the potent reference estrogen 17-ethinyl estradiol (EE), and the weak estrogen agonists bisphenol A, genistein, methoxychlor, nonylphenol, and o,p -DDT.
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17222880 Charles GD, Gennings C, Tornesi B, Kan HL, Zacharewski TR, Bhaskar Gollapudi B, Carney EW: Analysis of the interaction of phytoestrogens and synthetic chemicals: an in vitro/in vivo comparison. Toxicol Appl Pharmacol. 2007 Feb 1;218(3):280-8. Epub 2006 Dec 5.


Estrogenic activity was evaluated using an in vitro human estrogen receptor (ER) transcriptional activation assay and an in vivo immature rat uterotrophic assay.
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20093282 Chen M, Chiou P, Liao YH, Lin CM, Chen T: Development and characterization of five Rainbow Trout pituitary single-cell clone lines capable of producing pituitary hormones. J Endocrinol. 2010 Jan 21.


Reverse transcription (RT)-PCR analysis revealed that, in addition to expressing growth hormone (GH), prolactin (PRL) and estradiol receptor alpha (E2Ralpha) genes, each single-cell clone line also expressed other pituitary specific genes such as thyroid stimulating hormone (TSH), gonadotropin I (GTH-1), gonadotropin II (GTH-2), somatolactin (SL), proopiomelanocortin-B (POMC-B) and corticoidsteroid receptor (CR).
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18032409 Rasier G, Parent AS, Gerard A, Denooz R, Lebrethon MC, Charlier C, Bourguignon JP: Mechanisms of interaction of endocrine-disrupting chemicals with glutamate-evoked secretion of gonadotropin-releasing hormone. Toxicol Sci. 2008 Mar;102(1):33-41. Epub 2007 Nov 20.


A complete prevention of o,p'-DDT effects was caused by an estrogen receptor (ER) antagonist as well as an aryl hydrocarbon receptor (AHR) antagonist and inhibitors of protein kinases A and C and mitogen-activated kinases.
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17475301 Leanos-Castaneda O, van der Kraak G, Rodriguez-Canul R, Gold G: Endocrine disruption mechanism of o,p'-DDT in mature male tilapia (Oreochromis niloticus). Toxicol Appl Pharmacol. 2007 Jun 1;221(2):158-67. Epub 2007 Mar 23.


In particular, the possibility that o,p'-DDT effects were mediated directly via the estrogen receptor (ER).
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18835349 Minh SD, Below S, Muller C, Hildebrandt JP: Novel mammalian cell lines expressing reporter genes for the detection of environmental chemicals activating endogenous aryl hydrocarbon receptors (ArhR) or estrogen receptors (ER). Toxicol In Vitro. 2008 Dec;22(8):1935-47. Epub 2008 Sep 15.

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15084752 Gennings C, Carter WH Jr, Carney EW, Charles GD, Gollapudi BB, Carchman RA: A novel flexible approach for evaluating fixed ratio mixtures of full and partial agonists. Toxicol Sci. 2004 Jul;80(1):134-50. Epub 2004 Apr 14.


The methods are illustrated with a combination of six chemicals in an estrogen receptor-alpha (ER-alpha) reporter gene assay.
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17337754 Penza M, Montani C, Romani A, Vignolini P, Ciana P, Maggi A, Pampaloni B, Caimi L, Di Lorenzo D: Genistein accumulates in body depots and is mobilized during fasting, reaching estrogenic levels in serum that counter the hormonal actions of estradiol and organochlorines. Toxicol Sci. 2007 Jun;97(2):299-307. Epub 2007 Mar 3.


The observed effects may be relevant to a protective action of phytoestrogens against estrogen receptor-interacting pollutants as well as the dietary modulation of estradiol action.
1(0,0,0,1) Details
15603917 Frigo DE, Vigh KA, Struckhoff AP, Elliott S, Beckman BS, Burow ME, McLachlan JA: Xenobiotic-induced TNF-alpha expression and apoptosis through the p38 MAPK signaling pathway. Toxicol Lett. 2005 Feb 15;155(2):227-38.


Some xenobiotics, such as dichlorodiphenyltrichloroethane (DDT), bind to and activate estrogen receptors (ERs), eliciting estrogenic effects in both wildlife and humans.
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18678925 McGee TD, Edwards J, Roitberg AE: Preliminary molecular dynamic simulations of the estrogen receptor alpha ligand binding domain from antagonist to apo. Int J Environ Res Public Health. 2008 Jun;5(2):111-4.

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20074635 Freyberger A, Wilson V, Weimer M, Tan S, Tran HS, Ahr HJ: Assessment of a robust model protocol with accelerated throughput for a human recombinant full length estrogen receptor-alpha binding assay: Protocol optimization and intralaboratory assay performance as initial steps towards validation. Reprod Toxicol. 2010 Jan 13.

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16626760 Lemaire G, Mnif W, Mauvais P, Balaguer P, Rahmani R: Activation of alpha- and beta-estrogen receptors by persistent pesticides in reporter cell lines. Life Sci. 2006 Aug 15;79(12):1160-9. Epub 2006 Mar 27.

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15811587 Mussi P, Ciana P, Raviscioni M, Villa R, Regondi S, Agradi E, Maggi A, Di Lorenzo D: Activation of brain estrogen receptors in mice lactating from mothers exposed to DDT. Brain Res Bull. 2005 Apr 15;65(3):241-7. Epub 2004 Dec 18.

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17963131 Ansari RA, Gandy J: Determining the transrepression activity of xenoestrogen on nuclear factor-kappa B in Cos-1 cells by estrogen receptor-alpha. Int J Toxicol. 2007 Sep-Oct;26(5):441-9.

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17949972 Blum JL, James MO, Stuchal LD, Denslow ND: Stimulation of transactivation of the largemouth bass estrogen receptors alpha, beta-a, and beta-b by methoxychlor and its mono- and bis-demethylated metabolites in HepG2 cells. J Steroid Biochem Mol Biol. 2008 Jan;108(1-2):55-63. Epub 2007 Sep 7.

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18980187 Xu H, Kraus WL, Shuler ML: Development of a stable dual cell-line GFP expression system to study estrogenic endocrine disruptors. Biotechnol Bioeng. 2008 Dec 15;101(6):1276-87.


Here we constructed a dual cell-line green fluorescence protein (GFP) expression system to identify and study endocrine disrupting compounds with activities of estrogen receptor agonists or antagonists.
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18635653 Katsu Y, Kohno S, Hyodo S, Ijiri S, Adachi S, Hara A, Guillette LJ Jr, Iguchi T: Molecular cloning, characterization, and evolutionary analysis of estrogen receptors from phylogenetically ancient fish. Endocrinology. 2008 Dec;149(12):6300-10. Epub 2008 Jul 17.

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17258427 Fu KY, Chen CY, Chang WM: Application of a yeast estrogen screen in non-biomarker species Varicorhinus barbatulus fish with two estrogen receptor subtypes to assess xenoestrogens. Toxicol In Vitro. 2007 Jun;21(4):604-12. Epub 2006 Dec 19.

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18801367 Naidoo V, Katsu Y, Iguchi T: The influence of non-toxic concentrations of DDT and DDE on the old world vulture estrogen receptor alpha. Gen Comp Endocrinol. 2008 Nov-Dec;159(2-3):188-95. Epub 2008 Aug 28.

4(0,0,0,4) Details
18275596 Aube M, Larochelle C, Ayotte P: 1,1-dichloro-2,2-bis (p-chlorophenyl) ethylene (p,p'-DDE) disrupts the estrogen-androgen balance regulating the growth of hormone-dependent breast cancer cells. Breast Cancer Res. 2008;10(1):R16. Epub 2008 Feb 14.


We sought to examine the biological plausibility of this association by testing the effect of p,p'-DDE on the proliferation of CAMA-1 cells, a human breast cancer cell line that expresses the estrogen receptor alpha (ERalpha) and the androgen receptor (AR), in the presence of physiological concentrations of estrogens and androgens in the cell culture medium.
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20064516 Katsu Y, Taniguchi E, Urushitani H, Miyagawa S, Takase M, Kubokawa K, Tooi O, Oka T, Santo N, Myburgh J, Matsuno A, Iguchi T: Molecular cloning and characterization of ligand- and species-specificity of amphibian estrogen receptors. Gen Comp Endocrinol. 2010 Jan 12.

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18700809 Wang L, Zhou S, Lin K, Zhao M, Liu W, Gan J: Enantioselective estrogenicity of o,p'-dichlorodiphenyltrichloroethane in the MCF-7 human breast carcinoma cell line. Environ Toxicol Chem. 2009 Jan;28(1):1-8.


The maximal down-regulation of the transcription levels of estrogen receptor alpha (ERa) and ER3 by R-(-)-o,p'-DDT were 49 and 40% at the concentration of 10 (-6) mol/L, while those by S-(+)-o,p'-DDT were 24 and 26% at the concentration of 10 (-5) mol/L.
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18992306 Li J, Li N, Ma M, Giesy JP, Wang Z: In vitro profiling of the endocrine disrupting potency of organochlorine pesticides. Toxicol Lett. 2008 Dec 15;183(1-3):65-71. Epub 2008 Oct 17.


Aspects of neuro-endocrine system modulation include interactions such as agonism or antagonism of estrogen receptor (ER) binding.
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17088055 Thomas P, Dong J: Binding and activation of the seven-transmembrane estrogen receptor GPR30 by environmental estrogens: a potential novel mechanism of endocrine disruption. J Steroid Biochem Mol Biol. 2006 Dec;102(1-5):175-9. Epub 2006 Nov 7.

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19371625 Boehme K, Simon S, Mueller SO: Gene expression profiling in Ishikawa cells: a fingerprint for estrogen active compounds. Toxicol Appl Pharmacol. 2009 Apr 1;236(1):85-96. Epub 2009 Jan 23.


Several anthropogenous and naturally occurring substances, referred to as estrogen active compounds (EACs), are able to interfere with hormone and in particular estrogen receptor signaling.
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16337670 Hoekstra PF, Burnison BK, Garrison AW, Neheli T, Muir DC: Estrogenic activity of dicofol with the human estrogen receptor: Isomer- and enantiomer-specific implications. Chemosphere. 2006 Jun;64(1):174-7. Epub 2005 Dec 7.

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15541753 Villa R, Bonetti E, Penza ML, Iacobello C, Bugari G, Bailo M, Parolini O, Apostoli P, Caimi L, Ciana P, Maggi A, Di Lorenzo D: Target-specific action of organochlorine compounds in reproductive and nonreproductive tissues of estrogen-reporter male mice. Toxicol Appl Pharmacol. 2004 Dec 1;201(2):137-48.


The present work tests, in transgenic estrogen-reporter mice (ERE-tK-LUC), whether this increase is sufficient to modulate the estrogen receptors (ERs) in the whole body.
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15336722 Murono EP, Derk RC: The effects of the reported active metabolite of methoxychlor, 2,2-bis (p-hydroxyphenyl)-1,1,1-trichloroethane, on testosterone formation by cultured Leydig cells from young adult rats. Reprod Toxicol. 2004 Nov;19(1):135-46.


A recent study reported that HPTE inhibited both basal and hCG-stimulated testosterone formation by immature and adult cultured rat Leydig cells and that this effect was mediated through the estrogen receptor.
2(0,0,0,2) Details
17596564 Rasier G, Parent AS, Gerard A, Lebrethon MC, Bourguignon JP: Early maturation of gonadotropin-releasing hormone secretion and sexual precocity after exposure of infant female rats to estradiol or dichlorodiphenyltrichloroethane. Biol Reprod. 2007 Oct;77(4):734-42. Epub 2007 Jun 27.


These effects were prevented by antagonists of alpha-amino-3-hydroxy-5-methylisoxazole-4 propionic acid (AMPA)/kainate receptors and estrogen receptor.
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16183391 Heneweer M, Muusse M, van den Berg M, Sanderson JT: Additive estrogenic effects of mixtures of frequently used UV filters on pS2-gene transcription in MCF-7 cells. Toxicol Appl Pharmacol. 2005 Oct 15;208(2):170-7.


An estrogen receptor-mediated mechanism of action was expected for all UV filters.
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18921983 Celik L, Davey J, Lund D, Schiott B: Exploring interactions of endocrine-disrupting compounds with different conformations of the human estrogen receptor alpha ligand binding domain: a molecular docking study. Chem Res Toxicol. 2008 Nov;21(11):2195-206.

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18595403 Zhang Z, Hu J: Effects of p,p'-DDE exposure on gonadal development and gene expression in Japanese medaka (Oryzias latipes). J Environ Sci. 2008;20(3):347-52.


By quantitative real-time RT-PCR, it was found that gene expressions of vitellogenins (VTG-1, VTG-2), choriogenins (CHG-H, CHG-L), and estrogen receptor alpha (ER-alpha) in the liver of the fish were significantly up-regulated byp,p'-DDE exposure.
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17240461 Kristensen T, Edwards TM, Kohno S, Baatrup E, Guillette LJ Jr: Fecundity, 17beta-estradiol concentrations and expression of vitellogenin and estrogen receptor genes throughout the ovarian cycle in female Eastern mosquitofish from three lakes in Florida. Aquat Toxicol. 2007 Mar 10;81(3):245-55. Epub 2006 Dec 17.

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15026083 Fujimoto N, Kitamura S: Effects of environmental estrogenic chemicals on AP1 mediated transcription with estrogen receptors alpha and beta. J Steroid Biochem Mol Biol. 2004 Jan;88(1):53-9.

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19140503 Wozniak M, Murias M: [Xenoestrogens: endocrine disrupting compounds] . Ginekol Pol. 2008 Nov;79(11):785-90.


These chemicals can mimic the activity of endogenous estrogens, antagonize their interaction with estrogen receptors or disrupt the synthesis, metabolism and functions of endogenous female hormones.
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14604893 Frigo DE, Tang Y, Beckman BS, Scandurro AB, Alam J, Burow ME, McLachlan JA: Mechanism of AP-1-mediated gene expression by select organochlorines through the p38 MAPK pathway. Carcinogenesis. 2004 Feb;25(2):249-61. Epub 2003 Nov 6.


Our laboratory has studied cell signaling by environmental chemicals associated with the estrogen receptor (ER) and more recently via ER-independent mechanisms.
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15876529 Kuhl AJ, Manning S, Brouwer M: Brain aromatase in Japanese medaka (Oryzias latipes): Molecular characterization and role in xenoestrogen-induced sex reversal. J Steroid Biochem Mol Biol. 2005 Jun;96(1):67-77.


The promoter sequence revealed potential binding sites for the estrogen receptor and for transcription factors involved in primary neurogenesis and sex determination.
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