ICI 182,780

Cat. No. 1047

ICI 182,780 C32H47F5O3S [129453-61-8]

Price and Availability

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Special Conditions

No more than 1 g per customer per year to be sold.

Chemical Name: 7α,17β-[9-[(4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol

Biological Activity

A high affinity estrogen receptor antagonist (IC50 = 0.29 nM), devoid of any partial agonism both in vitro and in vivo. Also high affinity agonist at the membrane estrogen receptor GPER.

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

Technical Data

Soluble to 50 mM in ethanol and to 100 mM in DMSO
>99 %
Store at RT

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Howell et al (2000) ICI 182,780 (FaslodexTM): Development of a novel, "pure" antiestrogen. Cancer 89 817. PMID: 10951345.

de Cupis et al (1995) Comparison between novel steroid-like and conventional nonsteroidal antioestrogens in inhibiting oestradiol and IGF-I induced proliferation of human breast cancer-derived cells. Br.J.Pharmacol. 116 2391. PMID: 8581274.

Wakeling et al (1991) A potent specific pure antiestrogen with clinical potential. Cancer Res. 51 3867. PMID: 1855205.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for ICI 182,780 include:

Maselli et al (2016) Low expression of estrogen receptor β in T lymphocytes and high serum levels of anti-estrogen receptor α antibodies impact disease activity in female patients with systemic lupus erythematosus. Front Vet Sci 7 3. PMID: 26759713.

Albanito et al (2015) Effects of Atrazine on Estrogen Receptor α- and G Protein-Coupled Receptor 30-Mediated Signaling and Proliferation in Cancer Cells and Cancer-Associated Fibroblasts. Environ Health Perspect 123 493. PMID: 25616260.

Bean et al (2015) The PI3K/mTOR dual inhibitor P7170 demonstrates potent activity against endocrine-sensitive and endocrine-resistant ER+ breast cancer. Oncotarget 149 69. PMID: 25491778.

Castro et al (2015) Differential expression of upstream stimulatory factor (USF) 2 variants in eutopic endometria from women with endometriosis: estradiol regulation. Biol Res 48 56. PMID: 26453052.

Harvey et al (2015) Methoxychlor and its metabolite HPTE inhibit cAMP production and expression of estrogen receptors α and β in the rat granulosa cell in vitro. Reprod Toxicol 51 72. PMID: 25549949.

Hole et al (2015) New cell culture model for aromatase inhibitor-resistant breast cancer shows sensitivity to fulvestrant treatment and cross-resistance between letrozole and exemestane. BMC Cancer 46 1481. PMID: 25625755.

Hu et al (2015) NF-κB signaling is required for XBP1 (unspliced and spliced)-mediated effects on antiestrogen responsiveness and cell fate decisions in breast cancer. Oncogenesis 35 379. PMID: 25368386.

Kastrati et al (2015) PHLDA1 expression is controlled by an estrogen receptor-NFκB-miR-181 regulatory loop and is essential for formation of ER+ mammospheres. Oncogene 34 2309. PMID: 24954507.

Kim et al (2015) Estrogen promotes luteolysis by redistributing prostaglandin F2α receptors within primate luteal cells. Reproduction 149 453. PMID: 25687410.

Larsen et al (2015) Aurora kinase B is important for antiestrogen resistant cell growth and a potential biomarker for tamoxifen resistant breast cancer. Aging Cell 15 239. PMID: 25885472.

Luzhna et al (2015) Altered radiation responses of breast cancer cells resistant to hormonal therapy. Mol Cell Biol 6 1678. PMID: 25682200.

Miyoshi et al (2015) Nodes-and-connections RNAi knockdown screening: identification of a signaling molecule network involved in fulvestrant action and breast cancer prognosis. Biol Sex Differ 4 e172. PMID: 26479444.

Myers et al (2015) Estrogenic and anti-estrogenic activity of off-the-shelf hair and skin care products. BMC Cancer 25 271. PMID: 24849798.

Segovia-Mendoza et al (2015) Antihormonal agents as a strategy to improve the effect of chemo-radiation in cervical cancer: in vitro and in vivo study. J Biol Chem 15 21. PMID: 25622528.

Shappell et al (2015) The Effects of Steroid Implant and Dietary Soybean Hulls on Estrogenic Activity of Sera of Steers Grazing Toxic Endophyte-Infected Tall Fescue Pasture. Cancer Lett 2 30. PMID: 26664959.

Simões et al (2015) Anti-estrogen Resistance in Human Breast Tumors Is Driven by JAG1-NOTCH4-Dependent Cancer Stem Cell Activity. Cell Cycle 12 1968. PMID: 26387946.

Tomita et al (2015) A cluster of noncoding RNAs activates the ESR1 locus during breast cancer adaptation. Nat Commun 6 6966. PMID: 25923108.

Tozzi et al (2015) Endogenous 17β-estradiol is required for activity-dependent long-term potentiation in the striatum: interaction with the dopaminergic system. Front Cell Neurosci 9 192. PMID: 26074768.

Wang et al (2015) Differential effects of estrogen and estrogen receptor antagonist, ICI 182 780, on the expression of calbindin-D9k in rat pituitary prolactinoma GH3 cells. Cancer Cell Int 7 8498. PMID: 25674214.

Xiong et al (2015) Opposite effects of two estrogen receptors on tau phosphorylation through disparate effects on the miR-218/PTPA pathway. Breast Cancer Res Treat 14 867. PMID: 26111662.

Xu et al (2015) A short report: PAMM, a novel antioxidant protein, induced by oxidative stress. Redox Biol 6 446. PMID: 26402163.

Zhou et al (2015) Estrogen mediated expression of nucleophosmin 1 in human endometrial carcinoma clinical stages through estrogen receptor-α signaling. Endocrinology 14 540. PMID: 25663821.

Adomas et al (2014) Breast tumor specific mutation in GATA3 affects physiological mechanisms regulating transcription factor turnover. BMC Cancer 14 278. PMID: 24758297.

Alao et al (2014) Selective inhibition of RET mediated cell proliferation in vitro by the kinase inhibitor SPP86. BMC Cancer 14 853. PMID: 25409876.

Choi et al (2014) Suppression of autophagic activation in the mouse uterus by estrogen and progesterone. Cell Rep 221 39. PMID: 24443716.

Colciago et al (2014) In vitro chronic administration of ERbeta selective ligands and prostate cancer cell growth: hypotheses on the selective role of 3beta-adiol in AR-positive RV1 cells. Biomed Res Int 2014 801473. PMID: 24877132.

Cook and Clarke (2014) Estrogen receptor-α signaling and localization regulates autophagy and unfolded protein response activation in ER+ breast cancer. Steroids 1. PMID: 26005699.

Fan et al (2014) A molecular model for the mechanism of acquired tamoxifen resistance in breast cancer. Eur J Cancer 50 2866. PMID: 25204804.

Fan et al (2014) Inhibition of c-Src blocks oestrogen-induced apoptosis and restores oestrogen-stimulated growth in long-term oestrogen-deprived breast cancer cells. Eur J Cancer 50 457. PMID: 24183378.

Giretti et al (2014) Effects of Estetrol on Migration and Invasion in T47-D Breast Cancer Cells through the Actin Cytoskeleton. Front Endocrinol (Lausanne) 5 80. PMID: 24904530.

Gottardo et al (2014) Antiapoptotic factor humanin is expressed in normal and tumoral pituitary cells and protects them from TNF-α-induced apoptosis. PLoS One 9 e111548. PMID: 25360890.

Haagenson et al (2014) Functional analysis of MKP-1 and MKP-2 in breast cancer tamoxifen sensitivity. Oncotarget 5 1101. PMID: 24658355.

Hill and Muldrew (2014) Oestrogen upregulates the sarcoplasmic reticulum Ca(2+) ATPase pump in coronary arteries. Clin Exp Pharmacol Physiol 41 430. PMID: 24684418.

Liang et al (2014) Egr1 protein acts downstream of estrogen-leukemia inhibitory factor (LIF)-STAT3 pathway and plays a role during implantation through targeting Wnt4. J Biol Chem 289 23534. PMID: 25012664.

Nag and Mokha (2014) Activation of a Gq-coupled membrane estrogen receptor rapidly attenuates α2-adrenoceptor-induced antinociception via an ERK I/II-dependent, non-genomic mechanism in the female rat. Am J Physiol Regul Integr Comp Physiol 267 122. PMID: 24613724.

Oróstica et al (2014) Estradiol increases cAMP in the oviductal secretory cells through a nongenomic mechanism. Reproduction 148 285. PMID: 25038866.

Seo et al (2014) Comprehensive analysis of prostaglandin metabolic enzyme expression during pregnancy and the characterization of AKR1B1 as a prostaglandin F synthase at the maternal-conceptus interface in pigs. Breast Cancer Res 90 99. PMID: 24695626.

Speroni et al (2014) Hormonal regulation of epithelial organization in a three-dimensional breast tissue culture model. PLoS One 20 42. PMID: 23675751.

Yi et al (2014) Anti-tumor efficacy of fulvestrant in estrogen receptor positive gastric cancer. Sci Rep 4 7592. PMID: 25534230.

Aida-Yasuoka et al (2013) Estradiol promotes the development of a fibrotic phenotype and is increased in the serum of patients with systemic sclerosis. J Neurosci 15 R10. PMID: 23305385.

Aupperlee et al (2013) Amphiregulin mediates progesterone-induced mammary ductal development during puberty. J Neurosci 15 R44. PMID: 23705924.

Greaves et al (2013) ERβ-dependent effects on uterine endothelial cells are cell specific and mediated via Sp1. Hum Reprod 28 2490. PMID: 23756706.

Johansson et al (2013) Retinoic acid receptor alpha is associated with tamoxifen resistance in breast cancer. Nat Commun 4 2175. PMID: 23868472.

Kim et al (2013) The effect of estrogen compounds on human embryoid bodies. Proc Natl Acad Sci U S A 20 661. PMID: 23184660.

Morandi et al (2013) GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors. Cancer Res 73 3783. PMID: 23650283.

Ruiz et al (2013) Induction of hepatic multidrug resistance-associated protein 3 by ethynylestradiol is independent of cholestasis and mediated by estrogen receptor. Proc Natl Acad Sci U S A 41 275. PMID: 23077105.

Sievers et al (2013) Differential action of monohydroxylated polycyclic aromatic hydrocarbons with estrogen receptors α and β. Proc Natl Acad Sci U S A 132 359. PMID: 22989670.

Teng et al (2013) Endocrine disruptors fludioxonil and fenhexamid stimulate miR-21 expression in breast cancer cells. Toxicol Sci 131 71. PMID: 23052036.

Zhang et al (2013) Fulvestrant regulates epidermal growth factor (EGF) family ligands to activate EGF receptor (EGFR) signaling in breast cancer cells. Environ Health Perspect 139 351. PMID: 23686416.

Antoon et al (2012) Inhibition of p38-MAPK alters SRC coactivation and estrogen receptor phosphorylation. Cancer Biol Ther 13 1026. PMID: 22825349.

Babu et al (2012) Genistein prevents hyperglycemia-induced monocyte adhesion to human aortic endothelial cells through preservation of the cAMP signaling pathway and ameliorates vascular inflammation in obese diabetic mice. J Nutr 142 724. PMID: 22399524.

Bobustuc et al (2012) MGMT inhibition restores ERα functional sensitivity to antiestrogen therapy. Mol Med 18 913. PMID: 22549111.

Cao et al (2012) Estrogen receptor β activation is antinociceptive in a model of visceral pain in the rat. J Pain 13 685. PMID: 22698981.

Collins-Burow et al (2012) Antiestrogenic activity of flavonoid phytochemicals mediated via the c-Jun N-terminal protein kinase pathway. Cell-type specific regulation of estrogen receptor alpha. J Steroid Biochem Mol Biol 132 186. PMID: 22634477.

Cook et al (2012) Glucose-regulated protein 78 controls cross-talk between apoptosis and autophagy to determine antiestrogen responsiveness. Int J Mol Sci 72 3337. PMID: 22752300.

González-Arenas et al (2012) Estradiol increases cell growth in human astrocytoma cell lines through ERα activation and its interaction with SRC-1 and SRC-3 coactivators. Biochim Biophys Acta 1823 379. PMID: 22142990.

Guido et al (2012) Estrogen receptor β (ERβ) produces autophagy and necroptosis in human seminoma cell line through the binding of the Sp1 on the phosphatase and tensin homolog deleted from chromosome 10 (PTEN) promoter gene. Int J Clin Exp Pathol 11 2911. PMID: 22810004.

Leal et al (2012) p130Cas over-expression impairs mammary branching morphogenesis in response to estrogen and EGF. PLoS One 7 e49817. PMID: 23239970.

Lee et al (2012) Estrogen-like activity of aqueous extract from Agrimonia pilosa Ledeb. in MCF-7 cells. Endocrinology 12 260. PMID: 23259680.

Mahmoodzadeh et al (2012) 17β-Estradiol-induced interaction of ERα with NPPA regulates gene expression in cardiomyocytes. Cardiovasc Res 96 411. PMID: 22962310.

Niu et al (2012) Effects of gonadal hormones on the peripheral cannabinoid receptor 1 (CB1R) system under a myositis condition in rats. J Cereb Blood Flow Metab 153 2283. PMID: 22940464.

Park et al (2012) Activation of Estrogen Receptor by Bavachin from Psoralea corylifolia. Proc Natl Acad Sci U S A 20 183. PMID: 24116293.

Peretz et al (2012) Bisphenol A inhibits follicle growth and induces atresia in cultured mouse antral follicles independently of the genomic estrogenic pathway. Biol Reprod 87 63. PMID: 22743301.

Richardson et al (2012) Estrogen prevents oxidative damage to the mitochondria in Friedreich's ataxia skin fibroblasts. Endocrinology 7 e34600. PMID: 22509330.

Rodriguez-Ubreva et al (2012) Pre-B cell to macrophage transdifferentiation without significant promoter DNA methylation changes. Nucleic Acids Res 40 1954. PMID: 22086955.

Ropero et al (2012) Insulinotropic effect of the non-steroidal compound STX in pancreatic β-cells. PLoS One 7 e34650. PMID: 22506040.

Shim and Lee (2012) Estrogen receptor is activated by korean red ginseng in vitro but not in vivo. J Ginseng Res 36 169. PMID: 23717117.

Vinnedge et al (2012) The DEK oncogene is a target of steroid hormone receptor signaling in breast cancer. Neuroscience 7 e46985. PMID: 23071688.

Wang and Kuehl-Kovarik (2012) Estradiol directly attenuates sodium currents and depolarizing afterpotentials in isolated gonadotropin-releasing hormone neurons. Brain Res 1436 81. PMID: 22209345.

Wen et al (2012) Modulation of ovine SBD-1 expression by 17beta-estradiol in ovine oviduct epithelial cells. BMC Vet Res 8 143. PMID: 22920556.

Youn et al (2012) Inhibition of XO or NOX attenuates diethylstilbestrol-induced endothelial nitric oxide deficiency without affecting its effects on LNCaP cell invasion and apoptosis. Clin Sci (Lond) 123 509. PMID: 22568671.

Zuloaga et al (2012) Estrogen receptor β dependent attenuation of cytokine-induced cyclooxygenase-2 by androgens in human brain vascular smooth muscle cells and rat mesenteric arteries. Exp Neurol 77 835. PMID: 22542504.

Ahn et al (2011) Expression and regulation of Enpp2 in rat uterus during the estrous cycle. Toxicol Sci 12 379. PMID: 22122904.

Baquié et al (2011) The liver receptor homolog-1 (LRH-1) is expressed in human islets and protects {β}-cells against stress-induced apoptosis. FEMS Immunol Med Microbiol 20 2823. PMID: 21536586.

Burns et al (2011) Selective mutations in estrogen receptor alpha D-domain alters nuclear translocation and non-estrogen response element gene regulatory mechanisms. J Biol Chem 286 12640. PMID: 21285458.

Corcoran et al (2011) The effect of 17β-estradiol on cholesterol content in human macrophages is influenced by the lipoprotein milieu. Clin Cancer Res 47 109. PMID: 21830321.

He et al (2011) Complete estrogen receptor blocker ICI182,780 promotes the proliferation of vascular smooth muscle cells. Acta Biochim Biophys Sin (Shanghai) 43 118. PMID: 21193431.

Hsu et al (2011) JNK suppression is essential for 17β-Estradiol inhibits prostaglandin E2-Induced uPA and MMP-9 expressions and cell migration in human LoVo colon cancer cells. J Vet Sci 18 61. PMID: 21859479.

Ivanova et al (2011) Tamoxifen increases nuclear respiratory factor 1 transcription by activating estrogen receptor beta and AP-1 recruitment to adjacent promoter binding sites. FASEB J 25 1402. PMID: 21233487.

Tyagi et al (2011) Daidzein prevents the increase in CD4+CD28null T cells and B lymphopoesis in ovariectomized mice: a key mechanism for anti-osteoclastogenic effect. PLoS One 6 e21216. PMID: 21731677.

Yu et al (2011) mTOR controls ovarian follicle growth by regulating granulosa cell proliferation. PLoS One 6 e21415. PMID: 21750711.

Zheng et al (2011) 17β-Estradiol enhances breast cancer cell motility and invasion via extra-nuclear activation of actin-binding protein ezrin. PLoS One 6 e22439. PMID: 21818323.

Allard and Colaiácovo (2010) Bisphenol A impairs the double-strand break repair machinery in the germline and causes chromosome abnormalities. Proc Natl Acad Sci U S A 107 20405. PMID: 21059909.

Bender et al (2010) Roles of 17β-estradiol involve regulation of reelin expression and synaptogenesis in the dentate gyrus. Cereb Cortex 20 2985. PMID: 20421250.

Cruz et al (2010) Proliferation of human mammary cancer cells exposed to 27-hydroxycholesterol. J Expo Sci Environ Epidemiol 1 531. PMID: 22993572.

Dalvai and Bystricky (2010) Cell cycle and anti-estrogen effects synergize to regulate cell proliferation and ER target gene expression. PLoS One 5 e11011. PMID: 20543978.

Foong et al (2010) 5-HT(1A), SST(1), and SST(2) receptors mediate inhibitory postsynaptic potentials in the submucous plexus of the guinea pig ileum. Receptors Clin Investig 298 G384. PMID: 20007849.

Guo et al (2010) Estrogen-receptor-mediated protection of cerebral endothelial cell viability and mitochondrial function after ischemic insult in vitro. PLoS One 30 545. PMID: 19861973.

Harte et al (2010) BRD7, a subunit of SWI/SNF complexes, binds directly to BRCA1 and regulates BRCA1-dependent transcription. Cancer Res 70 2538. PMID: 20215511.

LaPensee et al (2010) Bisphenol A and estradiol are equipotent in antagonizing cisplatin-induced cytotoxicity in breast cancer cells. Cancer Res 290 167. PMID: 19796866.

Lin et al (2010) B7-H1-dependent sex-related differences in tumor immunity and immunotherapy responses. J Immunol 185 2747. PMID: 20686128.

Madeo et al (2010) c-Jun activation is required for 4-hydroxytamoxifen-induced cell death in breast cancer cells. Oncogene 29 978. PMID: 19935718.

Mahmoodzadeh et al (2010) 17beta-Estradiol inhibits matrix metalloproteinase-2 transcription via MAP kinase in fibroblasts. Cardiovasc Res 85 719. PMID: 19861308.

Mao et al (2010) Progesterone increases systemic and local uterine proportions of CD4+CD25+ Treg cells during midterm pregnancy in mice. Endocrinology 151 5477. PMID: 20844003.

Murphy et al (2010) Estradiol suppresses NF-kappa B activation through coordinated regulation of let-7a and miR-125b in primary human macrophages. J Immunol 184 5029. PMID: 20351193.

Okada et al (2010) Estrogen stimulates proliferation and differentiation of neural stem/progenitor cells through different signal transduction pathways. Am J Physiol Heart Circ Physiol 11 4114. PMID: 21152324.

Peng et al (2010) Unexpected hormonal activity of a catechol equine estrogen metabolite reveals reversible glutathione conjugation. Chem Res Toxicol 23 1374. PMID: 20540524.

Pradhan et al (2010) Proinflammatory cytokines enhance estrogen-dependent expression of the multidrug transporter gene ABCG2 through estrogen receptor and NF{kappa}B cooperativity at adjacent response elements. J Biol Chem 285 31100. PMID: 20705611.

Rangasamy et al (2010) Estrogen suppresses MLK3-mediated apoptosis sensitivity in ER+ breast cancer cells. Cancer Res 70 1731. PMID: 20145118.

Rasmussen et al (2010) Prolactin and oestrogen synergistically regulate gene expression and proliferation of breast cancer cells. Endocr Relat Cancer 17 809. PMID: 20601496.

Sanchez et al (2010) Estrogen receptor-alpha promotes breast cancer cell motility and invasion via focal adhesion kinase and N-WASP. Mol Endocrinol 24 2114. PMID: 20880986.

Sherrill et al (2010) Developmental exposures of male rats to soy isoflavones impact Leydig cell differentiation. Biol Reprod 83 488. PMID: 20554919.

Son et al (2010) Androgen receptor-dependent transactivation of growth arrest-specific gene 6 mediates inhibitory effects of testosterone on vascular calcification. J Biol Chem 285 7537. PMID: 20048160.

Sunters et al (2010) Mechano-transduction in osteoblastic cells involves strain-regulated estrogen receptor alpha-mediated control of insulin-like growth factor (IGF) I receptor sensitivity to Ambient IGF, leading to phosphatidylinositol 3-kinase/AKT-dependent Wnt/LRP5 receptor-independent activation of beta-catenin signaling. J Biol Chem 285 8743. PMID: 20042609.

Suzuki et al (2010) Down-regulation of PROS1 gene expression by 17beta-estradiol via estrogen receptor alpha (ERalpha)-Sp1 interaction recruiting receptor-interacting protein 140 and the corepressor-HDAC3 complex. J Biol Chem 285 13444. PMID: 20200160.

Thuillier et al (2010) Interdependence of platelet-derived growth factor and estrogen-signaling pathways in inducing neonatal rat testicular gonocytes proliferation. Biol Reprod 82 825. PMID: 20089883.

Wang et al (2010) Estrogen receptor α (ERα) mediates 17β-estradiol (E2)-activated expression of HBO1. Proc Natl Acad Sci U S A 29 140. PMID: 21040551.

Zhang (2010) Hepatocyte growth factor system in the mouse uterus: variation across the estrous cycle and regulation by 17-β-estradiol and progesterone. Clin Cancer Res 82 1037. PMID: 20147731.

Bolanz et al (2009) Tamoxifen inhibits TRPV6 activity via estrogen receptor-independent pathways in TRPV6-expressing MCF-7 breast cancer cells. Mol Cancer Res 7 2000. PMID: 19996302.

Bondar et al (2009) Estradiol-induced estrogen receptor-α trafficking. Mol Cell Endocrinol 29 15323. PMID: 19955385.

Boue et al (2009) Identification of the potent phytoestrogen glycinol in elicited soybean (Glycine max). Endocrinology 150 2446. PMID: 19116342.

Chisamore et al (2009) Characterization of a novel small molecule subtype specific estrogen-related receptor alpha antagonist in MCF-7 breast cancer cells. PLoS One 4 e5624. PMID: 19462000.

Comitato et al (2009) A novel mechanism of natural vitamin E tocotrienol activity: involvement of ERbeta signal transduction. Am J Physiol Endocrinol Metab 297 E427. PMID: 19491296.

Flamini et al (2009) Differential actions of estrogen and SERMs in regulation of the actin cytoskeleton of endometrial cells. Mol Hum Reprod 15 675. PMID: 19541800.

Han et al (2009) The estrogen receptor alpha pathway induces oncogenic Wip1 phosphatase gene expression. Mol Cancer Res 7 713. PMID: 19435816.

Hartman et al (2009) Hes-6, an inhibitor of Hes-1, is regulated by 17β-estradiol and promotes breast cancer cell proliferation. Arthritis Res Ther 11 R79. PMID: 19891787.

Hsieh et al (2009) Mechanism of the salutary effects of estrogen on kupffer cell phagocytic capacity following trauma-hemorrhage: pivotal role of Akt activation. J Immunol 182 4406. PMID: 19299741.

Iorns et al (2009) CRK7 modifies the MAPK pathway and influences the response to endocrine therapy. Carcinogenesis 30 1696. PMID: 19651820.

Kramár et al (2009) Cytoskeletal changes underlie estrogen's acute effects on synaptic transmission and plasticity. Hum Mol Genet 29 12982. PMID: 19828812.

Lee et al (2009) K+-dependent Na+/Ca2+ exchanger 3 is involved in renal active calcium transport and is differentially expressed in the mouse kidney. Am J Physiol Renal Physiol 297 F371. PMID: 19474185.

Park et al (2009) 17Beta-estradiol at low concentrations acts through distinct pathways in normal versus benign prostatic hyperplasia-derived prostate stromal cells. Endocrinology 150 4594. PMID: 19608654.

Quiles et al (2009) Mutational analysis of progesterone receptor functional domains in stable cell lines delineates sets of genes regulated by different mechanisms. Mol Endocrinol 23 809. PMID: 19299443.

Schaub and Wood (2009) Blockade of estrogen action upregulates estrogen receptor-alpha mRNA in the fetal brain. Neonatology 96 115. PMID: 19279395.

Schreihofer and Redmond (2009) Soy phytoestrogens are neuroprotective against stroke-like injury in vitro. Neuroscience 158 602. PMID: 18976694.

Tan et al (2009) Autocrine regulation of cell proliferation by estrogen receptor-alpha in estrogen receptor-alpha-positive breast cancer cell lines. BMC Cancer 9 31. PMID: 19171042.

Vedin et al (2009) The oxysterol receptor LXR inhibits proliferation of human breast cancer cells. Cancer Res 30 575. PMID: 19168586.

Albanito et al (2008) G-protein-coupled receptor 30 and estrogen receptor-alpha are involved in the proliferative effects induced by atrazine in ovarian cancer cells. Environ Health Perspect 116 1648. PMID: 19079715.

Chen et al (2008) Estrogen prevents intestinal inflammation after trauma-hemorrhage via downregulation of angiotensin II and angiotensin II subtype I receptor. J Mol Endocrinol 295 G1131. PMID: 18832446.

Galluzzo et al (2008) The nutritional flavanone naringenin triggers antiestrogenic effects by regulating estrogen receptor alpha-palmitoylation. Endocrinology 149 2567. PMID: 18239068.

Iorns et al (2008) Identification of CDK10 as an important determinant of resistance to endocrine therapy for breast cancer. Cancer Cell 13 91. PMID: 18242510.

Liu et al (2008) Estrogen-enhanced gene expression of lipoprotein lipase in heart is antagonized by progesterone. Endocrinology 149 711. PMID: 17974624.

Matsubara et al (2008) Estrogen determines sex differences in airway responsiveness after allergen exposure. Reprod Sci 38 501. PMID: 18063836.

Oh et al (2008) Tyrosine phosphorylation of the nuclear receptor coactivator AIB1/SRC-3 is enhanced by Abl kinase and is required for its activity in cancer cells. Mol Cell Biol 28 6580. PMID: 18765637.

Pan et al (2008) Differential expression of microRNAs in myometrium and leiomyomas and regulation by ovarian steroids. J Biol Chem 12 227. PMID: 18182067.

Sirianni et al (2008) The novel estrogen receptor, G protein-coupled receptor 30, mediates the proliferative effects induced by 17β-estradiol on mouse spermatogonial GC-1 cell line. Int J Oncol 149 5043. PMID: 18566133.

Subtil-Rodríguez et al (2008) Progesterone induction of the 11beta-hydroxysteroid dehydrogenase type 2 promoter in breast cancer cells involves coordinated recruitment of STAT5A and progesterone receptor to a distal enhancer and polymerase tracking. Mol Cell Biol 28 3830. PMID: 18378698.

Teng et al (2008) Roles of estrogen receptor alpha and beta in modulating urothelial cell proliferation. Endocr Relat Cancer 15 351. PMID: 18310301.

Toloubeydokhti et al (2008) The expression and ovarian steroid regulation of endometrial micro-RNAs. J Exp Clin Cancer Res 15 993. PMID: 19088369.

Tsutsumi et al (2008) Differential regulation of the inducible nitric oxide synthase gene by estrogen receptors 1 and 2. Tissue Eng Part C Methods 199 267. PMID: 18753331.

Wang et al (2008) Hormonal regulation of BCRP expression in human placental BeWo cells. Pharm Res 25 444. PMID: 17823853.

Yuan et al (2008) Effects of estradiol and progesterone on the proinflammatory cytokine production by mononuclear cells from patients with chronic hepatitis C. World J Gastroenterol 14 2200. PMID: 18407594.

Akingbemi et al (2007) Exposure to phytoestrogens in the perinatal period affects androgen secretion by testicular Leydig cells in the adult rat. Endocrinology 148 4475. PMID: 17569756.

Albanito et al (2007) G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17beta-estradiol and selective GPR30 ligand G-1 in ovarian cancer cells. Cancer Res 67 1859. PMID: 17308128.

Bains et al (2007) Neuroprotection by estrogen against MPP+-induced dopamine neuron death is mediated by ERα in primary cultures of mouse mesencephalon. Biol Reprod 204 767. PMID: 17320868.

Chang et al (2007) Activation of estrogen receptor-mediated gene transcription by the equine estrogen metabolite, 4-methoxyequilenin, in human breast cancer cells. Endocrinology 148 4793. PMID: 17584965.

Cullen et al (2007) Resveratrol inhibits expression and binding activity of the monocyte chemotactic protein-1 receptor, CCR2, on THP-1 monocytes. Atherosclerosis 195 e125. PMID: 17499741.

Deschênes et al (2007) Regulation of GREB1 transcription by estrogen receptor α through a multipartite enhancer spread over 20 kb of upstream flanking sequences. BMC Complement Altern Med 282 17335. PMID: 17463000.

Kramer et al (2007) 17β-Estradiol utilizes the estrogen receptor to regulate CD16 expression in monocytes. Stroke 279 16. PMID: 17923257.

Peterson et al (2007) The silencing mediator of retinoic acid and thyroid hormone receptor (SMRT) corepressor is required for full estrogen receptor alpha transcriptional activity. Mol Cell Biol 27 5933. PMID: 17591692.

Rayner et al (2007) NM23-H2, an estrogen receptor β-associated protein, shows diminished expression with progression of atherosclerosis. Reprod Sci 292 R743. PMID: 17272673.

Schaub et al (2007) Blockade of estrogen receptors decreases CNS and pituitary prostaglandin synthase expression in fetal sheep. FASEB J 87 121. PMID: 17934250.

Trauernicht et al (2007) Modulation of estrogen receptor α protein level and survival function by DBC-1. Br J Pharmacol 21 1526. PMID: 17473282.

Velarde et al (2007) Kruppel-like factor 9 is a negative regulator of ligand-dependent estrogen receptor alpha signaling in Ishikawa endometrial adenocarcinoma cells. Mol Endocrinol 21 2988. PMID: 17717078.

Wittmann et al (2007) Definition of functionally important mechanistic differences among selective estrogen receptor down-regulators. Cancer Res 67 9549. PMID: 17909066.

Zhu and Pollard (2007) Estradiol-17beta regulates mouse uterine epithelial cell proliferation through insulin-like growth factor 1 signaling. Proc Natl Acad Sci U S A 104 15847. PMID: 17895382.

Alonso-Magdalena et al (2006) The estrogenic effect of bisphenol A disrupts pancreatic β-cell function in vivo and induces insulin resistance. Am J Physiol Gastrointest Liver Physiol 114 106. PMID: 16393666.

Buterin et al (2006) Convergent transcriptional profiles induced by endogenous estrogen and distinct xenoestrogens in breast cancer cells. Carcinogenesis 27 1567. PMID: 16474171.

Chen et al (2006) Activation of insulin-like growth factor I receptor-mediated pathway by ginsenoside Rg1. Br J Pharmacol 147 542. PMID: 16415910.

Dahm et al (2006) Estrogens, selective estrogen receptor modulators, and a selective estrogen receptor down-regulator inhibit endothelial production of tissue factor pathway inhibitor 1. BMC Cardiovasc Disord 6 40. PMID: 17029634.

Dalenc et al (2006) Farnesyl-transferase inhibitor R115,777 enhances tamoxifen inhibition of MCF-7 cell growth through estrogen receptor dependent and independent pathways. Breast Cancer Res 7 R1159. PMID: 16457696.

Journé et al (2006) Additive growth inhibitory effects of ibandronate and antiestrogens in estrogen receptor-positive breast cancer cell lines. Cancer Res 8 R2. PMID: 16417650.

Kilker and Planas-Silva (2006) Cyclin D1 is necessary for tamoxifen-induced cell cycle progression in human breast cancer cells. Breast Cancer Res 66 11478. PMID: 17145896.

Kim et al (2006) Antiestrogens and the formation of DNA damage in rats: a comparison. Infect Immun 19 852. PMID: 16780365.

Manavathi et al (2006) An inherent role of microtubule network in the action of nuclear receptor. J Endocrinol 103 15981. PMID: 17043237.

Ohshiro et al (2006) Biological role of estrogen receptor β in salivary gland adenocarcinoma cells. Exp Ther Med 12 5994. PMID: 17062671.

Shih et al (2006) 17β-Estradiol inhibits subarachnoid hemorrhage-induced inducible nitric oxide synthase gene expression by interfering with the nuclear factor κ B transactivation. Proc Natl Acad Sci U S A 37 3025. PMID: 17053178.

Vivacqua et al (2006) 17beta-estradiol, genistein, and 4-hydroxytamoxifen induce the proliferation of thyroid cancer cells through the g protein-coupled receptor GPR30. Mol Pharmacol 70 1414. PMID: 16835357.

Wang et al (2006) Disruption of estrogen receptor DNA-binding domain and related intramolecular communication restores tamoxifen sensitivity in resistant breast cancer. BMC Immunol 10 487. PMID: 17157789.

Widyarini et al (2006) Estrogen receptor signaling protects against immune suppression by UV radiation exposure. Neuroendocrinology 103 12837. PMID: 16908847.

Wieland et al (2006) Efficient intracellular multiplication of Legionella pneumophila in human monocytes requires functional host cell L-type calcium channels. Am J Physiol Gastrointest Liver Physiol 47 296. PMID: 16831218.

Xia et al (2006) A model of acquired autoresistance to a potent ErbB2 tyrosine kinase inhibitor and a therapeutic strategy to prevent its onset in breast cancer. Br J Cancer 103 7795. PMID: 16682622.

Abe and Terasawa (2005) Firing pattern and rapid modulation of activity by estrogen in primate luteinizing hormone releasing hormone-1 neurons. Endocrinology 146 4312. PMID: 15976055.

Acconcia et al (2005) Palmitoylation-dependent estrogen receptor alpha membrane localization: regulation by 17beta-estradiol. Mol Biol Cell 16 231. PMID: 15496458.

Candolfi et al (2005) Progesterone antagonizes the permissive action of estradiol on tumor necrosis factor-α-induced apoptosis of anterior pituitary cells. Proc Natl Acad Sci U S A 146 736. PMID: 15528300.

Crane-Godreau and Wira (2005) Effects of estradiol on lipopolysaccharide and Pam3Cys stimulation of CCL20/macrophage inflammatory protein 3 α and tumor necrosis factor α production by uterine epithelial cells in culture. Breast Cancer Res Treat 73 4231. PMID: 15972514.

Edmunds et al (2005) The effects of dietary phytoestrogens on aromatase activity in human endometrial stromal cells. Environ Health Perspect 45 709. PMID: 16285913.

Gingerich and Krukoff (2005) Estrogen modulates endothelial and neuronal nitric oxide synthase expression via an estrogen receptor beta-dependent mechanism in hypothalamic slice cultures. Endocrinology 146 2933. PMID: 15790731.

Hershberger et al (2005) Regulation of endogenous gene expression in human non-small cell lung cancer cells by estrogen receptor ligands. Cancer Cell 65 1598. PMID: 15735050.

Islander et al (2005) Estren promotes androgen phenotypes in primary lymphoid organs and submandibular glands. Reprod Nutr Dev 6 16. PMID: 16011795.

Labhart et al (2005) Identification of target genes in breast cancer cells directly regulated by the SRC-3/AIB1 coactivator. Proc Natl Acad Sci U S A 102 1339. PMID: 15677324.

Lee et al (2005) Estrogen receptor alpha pathway is involved in the regulation of Calbindin-D9k in the uterus of immature rats. Toxicol Sci 84 270. PMID: 15635152.

Park et al (2005) Formation of an IKKalpha-dependent transcription complex is required for estrogen receptor-mediated gene activation. Mol Cell 18 71. PMID: 15808510.

Stirone et al (2005) Estrogen increases mitochondrial efficiency and reduces oxidative stress in cerebral blood vessels. Mol Pharmacol 68 959. PMID: 15994367.

Zivadinovic and Watson (2005) Membrane estrogen receptor-alpha levels predict estrogen-induced ERK1/2 activation in MCF-7 cells. Breast Cancer Res 7 R130. PMID: 15642162.

Bulayeva and Watson (2004) Xenoestrogen-induced ERK-1 and ERK-2 activation via multiple membrane-initiated signaling pathways. Environ Health Perspect 112 1481. PMID: 15531431.

Dominguez et al (2004) Morphological effects of estrogen on cholinergic neurons in vitro involves activation of extracellular signal-regulated kinases. Carcinogenesis 24 982. PMID: 14749443.

Hartman et al (2004) HES-1 inhibits 17β-estradiol and heregulin-β1-mediated upregulation of E2F-1. J Cell Mol Med 23 8826. PMID: 15467735.

Journe et al (2004) Steroid-free medium discloses oestrogenic effects of the bisphosphonate clodronate on breast cancer cells. Breast Cancer Res 91 1703. PMID: 15477866.

Kouzmenko et al (2004) Wnt/β-catenin and estrogen signaling converge in vivo. Am J Respir Cell Mol Biol 279 40255. PMID: 15304487.

Levine (2004) Tamoxifen and the Rafoxifene analog LY117018: their effects on arachidonic acid release from cells in culture and on prostaglandin I2 production by rat liver cells. Proc Natl Acad Sci U S A 4 49. PMID: 15310397.

Maggiolini et al (2004) The G protein-coupled receptor GPR30 mediates c-fos up-regulation by 17beta-estradiol and phytoestrogens in breast cancer cells. J Biol Chem 279 27008. PMID: 15090535.

Morelli et al (2004) Nuclear insulin receptor substrate 1 interacts with estrogen receptor alpha at ERE promoters. Oncogene 23 7517. PMID: 15318176.

Ramsey et al (2004) Estrogen receptor beta isoforms exhibit differences in ligand-activated transcriptional activity in an estrogen response element sequence-dependent manner. Endocrinology 145 149. PMID: 14500565.

Wynne et al (2004) Age-related reduction in estrogen receptor-mediated mechanisms of vascular relaxation in female spontaneously hypertensive rats. Hypertension 43 405. PMID: 14699001.

Yang et al (2004) Human epidermal growth factor receptor 2 status modulates subcellular localization of and interaction with estrogen receptor α in breast cancer cells. Oncogene 10 3621. PMID: 15173068.

Bevan et al (2003) Environmental estrogens alter early development in Xenopus laevis. J Endocrinol 111 488. PMID: 12676604.

Finlay et al (2003) Regulation of PDGF production and ERK activation by estrogen is associated with TSC2 gene expression. Am J Physiol Cell Physiol 285 C409. PMID: 12700139.

Kimmins et al (2003) The effects of estrogen, its antagonist ICI 182, 780, and interferon-tau on the expression of estrogen receptors and integrin alphaV beta 3 on cycle day 16 in bovine endometrium. Reprod Biol Endocrinol 1 38. PMID: 12756058.

Paez-Pereda et al (2003) Involvement of bone morphogenetic protein 4 (BMP-4) in pituitary prolactinoma pathogenesis through a Smad/estrogen receptor crosstalk. BMC Cancer 100 1034. PMID: 12552124.

Schroeder et al (2003) Inhibition of prolactin (PRL)-induced proliferative signals in breast cancer cells by a molecular mimic of phosphorylated PRL, S179D-PRL. Biomol Ther (Seoul) 144 5300. PMID: 12970160.

Bucci et al (2002) 17-β-oestradiol-induced vasorelaxation in vitro is mediated by eNOS through hsp90 and akt/pkb dependent mechanism. Drug Metab Dispos 135 1695. PMID: 11934809.

Grimaldi et al (2002) Estrogen alters thresholds for B cell apoptosis and activation. J Clin Invest 109 1625. PMID: 12070310.

Hermenegildo et al (2002) Estradiol reduces F2α-isoprostane production in cultured human endothelial cells. Biol Reprod 283 H2644. PMID: 12388318.

Mukherjee et al (2002) Testosterone attenuates expression of vascular cell adhesion molecule-1 by conversion to estradiol by aromatase in endothelial cells: implications in atherosclerosis. Mol Endocrinol 99 4055. PMID: 11904449.

Wellejus and Loft (2002) Receptor-mediated ethinylestradiol-induced oxidative DNA damage in rat testicular cells. Proc Natl Acad Sci U S A 16 195. PMID: 11818367.

Goetz et al (1999) Estradiol induces the calcium-dependent translocation of endothelial nitric oxide synthase. J Neurosci 96 2788. PMID: 10077589.

Moosmann and Behl (1999) The antioxidant neuroprotective effects of estrogens and phenolic compounds are independent from their estrogenic properties. Chem Res Toxicol 96 8867. PMID: 10430862.

Paige et al (1999) Estrogen receptor (ER) modulators each induce distinct conformational changes in ER α and ER β. J Biomed Sci 96 3999. PMID: 10097152.

Alonso-Magdalena et al Pancreatic insulin content regulation by the estrogen receptor ER alpha. PLoS One 3 e2069. PMID: 18446233.

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