ICI 182,780 (CAS 129453-61-8): R&D Systems
Catalog Number: 1047
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.
Technical Data
  • M.Wt:
    606.77
  • Formula:
    C32H47F5O3S
  • Solubility:
    Soluble to 50 mM in ethanol and to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at RT
  • CAS No:
    129453-61-8
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.
Additional Information
Licensing Caveats:
Sold with the permission of AstraZeneca UK Ltd.
Background References
  1. Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells.
    Thomas et al.
    Endocrinology, 2005;146:624
  2. Comparison between novel steroid-like and conventional nonsteroidal antioestrogens in inhibiting oestradiol and IGF-I induced proliferation of human breast cancer-derived cells.
    de Cupis et al.
    Br.J.Pharmacol., 1995;116:2391
  3. ICI 182,780 (FaslodexTM): Development of a novel, "pure" antiestrogen.
    Howell et al.
    Cancer, 2000;89:817
  4. A potent specific pure antiestrogen with clinical potential.
    Wakeling et al.
    Cancer Res., 1991;51:3867
Citations:

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

212 Citations: Showing 1 - 10
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  1. Pancreatic insulin content regulation by the estrogen receptor ER alpha.
    Authors: Alonso-Magdalena Et al.
    PLoS One ;3:e2069
  2. Structural and molecular mechanisms of cytokine-mediated endocrine resistance in human breast cancer cells.
    Authors: Stender
    Mol Cell 2017;65(6):1122
  3. Differential and directional estrogenic signaling pathways induced by enterolignans and their precursors.
    Authors: Zhu
    PLoS One 2017;12(2):e0171390
  4. 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.
    Authors: Maselli Et al.
    Front Vet Sci 2016;7:3
  5. Antiestrogen resistant cell lines expressing estrogen receptor α mutations upregulate the unfolded protein response and are killed by BHPI
    Authors: Mao Et al.
    Scientific Reports 2016;6:34753
  6. Endogenous 17β-estradiol is required for activity-dependent long-term potentiation in the striatum: interaction with the dopaminergic system.
    Authors: Tozzi Et al.
    Front Cell Neurosci 2015;9:192
  7. Differential effects of estrogen and estrogen receptor antagonist, ICI 182 780, on the expression of calbindin-D9k in rat pituitary prolactinoma GH3 cells.
    Authors: Wang Et al.
    Cancer Cell Int 2015;7:8498
  8. A cluster of noncoding RNAs activates the ESR1 locus during breast cancer adaptation.
    Authors: Tomita Et al.
    Nat Commun 2015;6:6966
  9. A short report: PAMM, a novel antioxidant protein, induced by oxidative stress.
    Authors: Xu Et al.
    Redox Biol 2015;6:446
  10. Altered radiation responses of breast cancer cells resistant to hormonal therapy.
    Authors: Luzhna Et al.
    Mol Cell Biol 2015;6:1678
  11. Methoxychlor and its metabolite HPTE inhibit cAMP production and expression of estrogen receptors α and β in the rat granulosa cell in vitro.
    Authors: Harvey Et al.
    Reprod Toxicol 2015;51:72
  12. Nodes-and-connections RNAi knockdown screening: identification of a signaling molecule network involved in fulvestrant action and breast cancer prognosis.
    Authors: Miyoshi Et al.
    Biol Sex Differ 2015;4:e172
  13. Differential expression of upstream stimulatory factor (USF) 2 variants in eutopic endometria from women with endometriosis: estradiol regulation.
    Authors: Castro Et al.
    Biol Res 2015;48:56
  14. New cell culture model for aromatase inhibitor-resistant breast cancer shows sensitivity to fulvestrant treatment and cross-resistance between letrozole and exemestane.
    Authors: Hole Et al.
    BMC Cancer 2015;46:1481
  15. NF-κB signaling is required for XBP1 (unspliced and spliced)-mediated effects on antiestrogen responsiveness and cell fate decisions in breast cancer.
    Authors: Hu Et al.
    Oncogenesis 2015;35:379
  16. PHLDA1 expression is controlled by an estrogen receptor-NFκB-miR-181 regulatory loop and is essential for formation of ER+ mammospheres.
    Authors: Kastrati Et al.
    Oncogene 2015;34:2309
  17. The Effects of Steroid Implant and Dietary Soybean Hulls on Estrogenic Activity of Sera of Steers Grazing Toxic Endophyte-Infected Tall Fescue Pasture.
    Authors: Shappell Et al.
    Cancer Lett 2015;2:30
  18. Estrogenic and anti-estrogenic activity of off-the-shelf hair and skin care products.
    Authors: Myers Et al.
    BMC Cancer 2015;25:271
  19. Aurora kinase B is important for antiestrogen resistant cell growth and a potential biomarker for tamoxifen resistant breast cancer.
    Authors: Larsen Et al.
    Aging Cell 2015;15:239
  20. Antihormonal agents as a strategy to improve the effect of chemo-radiation in cervical cancer: in vitro and in vivo study.
    Authors: Segovia-Mendoza Et al.
    J Biol Chem 2015;15:21
  21. Opposite effects of two estrogen receptors on tau phosphorylation through disparate effects on the miR-218/PTPA pathway.
    Authors: Xiong Et al.
    Breast Cancer Res Treat 2015;14:867
  22. Estrogen mediated expression of nucleophosmin 1 in human endometrial carcinoma clinical stages through estrogen receptor-α signaling.
    Authors: Zhou Et al.
    Endocrinology 2015;14:540
  23. The PI3K/mTOR dual inhibitor P7170 demonstrates potent activity against endocrine-sensitive and endocrine-resistant ER+ breast cancer.
    Authors: Bean Et al.
    Oncotarget 2015;149:69
  24. Estrogen promotes luteolysis by redistributing prostaglandin F2α receptors within primate luteal cells.
    Authors: Kim Et al.
    Reproduction 2015;149:453
  25. Anti-estrogen Resistance in Human Breast Tumors Is Driven by JAG1-NOTCH4-Dependent Cancer Stem Cell Activity.
    Authors: Simões Et al.
    Cell Cycle 2015;12:1968
  26. Effects of Atrazine on Estrogen Receptor α- and G Protein-Coupled Receptor 30-Mediated Signaling and Proliferation in Cancer Cells and Cancer-Associated Fibroblasts.
    Authors: Albanito Et al.
    Environ Health Perspect 2015;123:493
  27. Antiapoptotic factor humanin is expressed in normal and tumoral pituitary cells and protects them from TNF-α-induced apoptosis.
    Authors: Gottardo Et al.
    PLoS One 2014;9:e111548
  28. 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.
    Authors: Seo Et al.
    Breast Cancer Res 2014;90:99
  29. Effects of Estetrol on Migration and Invasion in T47-D Breast Cancer Cells through the Actin Cytoskeleton.
    Authors: Giretti Et al.
    Front Endocrinol (Lausanne) 2014;5:80
  30. Functional analysis of MKP-1 and MKP-2 in breast cancer tamoxifen sensitivity.
    Authors: Haagenson Et al.
    Oncotarget 2014;5:1101
  31. Inhibition of c-Src blocks oestrogen-induced apoptosis and restores oestrogen-stimulated growth in long-term oestrogen-deprived breast cancer cells.
    Authors: Fan Et al.
    Eur J Cancer 2014;50:457
  32. A molecular model for the mechanism of acquired tamoxifen resistance in breast cancer.
    Authors: Fan Et al.
    Eur J Cancer 2014;50:2866
  33. Anti-tumor efficacy of fulvestrant in estrogen receptor positive gastric cancer.
    Authors: Yi Et al.
    Sci Rep 2014;4:7592
  34. Oestrogen upregulates the sarcoplasmic reticulum Ca(2+) ATPase pump in coronary arteries.
    Authors: Hill and Muldrew
    Clin Exp Pharmacol Physiol 2014;41:430
  35. Egr1 protein acts downstream of estrogen-leukemia inhibitory factor (LIF)-STAT3 pathway and plays a role during implantation through targeting Wnt4.
    Authors: Liang Et al.
    J Biol Chem 2014;289:23534
  36. 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.
    Authors: Nag and Mokha
    Am J Physiol Regul Integr Comp Physiol 2014;267:122
  37. Suppression of autophagic activation in the mouse uterus by estrogen and progesterone.
    Authors: Choi Et al.
    Cell Rep 2014;221:39
  38. Hormonal regulation of epithelial organization in a three-dimensional breast tissue culture model.
    Authors: Speroni Et al.
    PLoS One 2014;20:42
  39. 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.
    Authors: Colciago Et al.
    Biomed Res Int 2014;2014:801473
  40. Selective inhibition of RET mediated cell proliferation in vitro by the kinase inhibitor SPP86.
    Authors: Alao Et al.
    BMC Cancer 2014;14:853
  41. Breast tumor specific mutation in GATA3 affects physiological mechanisms regulating transcription factor turnover.
    Authors: Adomas Et al.
    BMC Cancer 2014;14:278
  42. Estradiol increases cAMP in the oviductal secretory cells through a nongenomic mechanism.
    Authors: Oróstica Et al.
    Reproduction 2014;148:285
  43. Estrogen receptor-α signaling and localization regulates autophagy and unfolded protein response activation in ER+ breast cancer.
    Authors: Cook and Clarke
    Steroids 2014;1
  44. GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors.
    Authors: Morandi Et al.
    Cancer Res 2013;73:3783
  45. Retinoic acid receptor alpha is associated with tamoxifen resistance in breast cancer.
    Authors: Johansson Et al.
    Nat Commun 2013;4:2175
  46. Induction of hepatic multidrug resistance-associated protein 3 by ethynylestradiol is independent of cholestasis and mediated by estrogen receptor.
    Authors: Ruiz Et al.
    Proc Natl Acad Sci U S A 2013;41:275
  47. ERβ-dependent effects on uterine endothelial cells are cell specific and mediated via Sp1.
    Authors: Greaves Et al.
    Hum Reprod 2013;28:2490
  48. The effect of estrogen compounds on human embryoid bodies.
    Authors: Kim Et al.
    Proc Natl Acad Sci U S A 2013;20:661
  49. Amphiregulin mediates progesterone-induced mammary ductal development during puberty.
    Authors: Aupperlee Et al.
    J Neurosci 2013;15:R44
  50. Estradiol promotes the development of a fibrotic phenotype and is increased in the serum of patients with systemic sclerosis.
    Authors: Aida-Yasuoka Et al.
    J Neurosci 2013;15:R10
  51. Fulvestrant regulates epidermal growth factor (EGF) family ligands to activate EGF receptor (EGFR) signaling in breast cancer cells.
    Authors: Zhang Et al.
    Environ Health Perspect 2013;139:351
  52. Differential action of monohydroxylated polycyclic aromatic hydrocarbons with estrogen receptors α and β.
    Authors: Sievers Et al.
    Proc Natl Acad Sci U S A 2013;132:359
  53. Endocrine disruptors fludioxonil and fenhexamid stimulate miR-21 expression in breast cancer cells.
    Authors: Teng Et al.
    Toxicol Sci 2013;131:71
  54. 17β-Estradiol-induced interaction of ERα with NPPA regulates gene expression in cardiomyocytes.
    Authors: Mahmoodzadeh Et al.
    Cardiovasc Res 2012;96:411
  55. Modulation of ovine SBD-1 expression by 17beta-estradiol in ovine oviduct epithelial cells.
    Authors: Wen Et al.
    BMC Vet Res 2012;8:143
  56. Bisphenol A inhibits follicle growth and induces atresia in cultured mouse antral follicles independently of the genomic estrogenic pathway.
    Authors: Peretz Et al.
    Biol Reprod 2012;87:63
  57. p130Cas over-expression impairs mammary branching morphogenesis in response to estrogen and EGF.
    Authors: Leal Et al.
    PLoS One 2012;7:e49817
  58. The DEK oncogene is a target of steroid hormone receptor signaling in breast cancer.
    Authors: Vinnedge Et al.
    Neuroscience 2012;7:e46985
  59. Insulinotropic effect of the non-steroidal compound STX in pancreatic β-cells.
    Authors: Ropero Et al.
    PLoS One 2012;7:e34650
  60. Estrogen prevents oxidative damage to the mitochondria in Friedreich's ataxia skin fibroblasts.
    Authors: Richardson Et al.
    Endocrinology 2012;7:e34600
  61. Estrogen receptor β dependent attenuation of cytokine-induced cyclooxygenase-2 by androgens in human brain vascular smooth muscle cells and rat mesenteric arteries.
    Authors: Zuloaga Et al.
    Exp Neurol 2012;77:835
  62. Glucose-regulated protein 78 controls cross-talk between apoptosis and autophagy to determine antiestrogen responsiveness.
    Authors: Cook Et al.
    Int J Mol Sci 2012;72:3337
  63. Pre-B cell to macrophage transdifferentiation without significant promoter DNA methylation changes.
    Authors: Rodriguez-Ubreva Et al.
    Nucleic Acids Res 2012;40:1954
  64. Estrogen receptor is activated by korean red ginseng in vitro but not in vivo.
    Authors: Shim and Lee
    J Ginseng Res 2012;36:169
  65. Activation of Estrogen Receptor by Bavachin from Psoralea corylifolia.
    Authors: Park Et al.
    Proc Natl Acad Sci U S A 2012;20:183
  66. MGMT inhibition restores ERα functional sensitivity to antiestrogen therapy.
    Authors: Bobustuc Et al.
    Mol Med 2012;18:913
  67. Estradiol increases cell growth in human astrocytoma cell lines through ERα activation and its interaction with SRC-1 and SRC-3 coactivators.
    Authors: González-Arenas Et al.
    Biochim Biophys Acta 2012;1823:379
  68. Effects of gonadal hormones on the peripheral cannabinoid receptor 1 (CB1R) system under a myositis condition in rats.
    Authors: Niu Et al.
    J Cereb Blood Flow Metab 2012;153:2283
  69. Estradiol directly attenuates sodium currents and depolarizing afterpotentials in isolated gonadotropin-releasing hormone neurons.
    Authors: Wang and Kuehl-Kovarik
    Brain Res 2012;1436:81
  70. 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.
    Authors: Babu Et al.
    J Nutr 2012;142:724
  71. Estrogen receptor β activation is antinociceptive in a model of visceral pain in the rat.
    Authors: Cao Et al.
    J Pain 2012;13:685
  72. Inhibition of p38-MAPK alters SRC coactivation and estrogen receptor phosphorylation.
    Authors: Antoon Et al.
    Cancer Biol Ther 2012;13:1026
  73. Antiestrogenic activity of flavonoid phytochemicals mediated via the c-Jun N-terminal protein kinase pathway. Cell-type specific regulation of estrogen receptor alpha.
    Authors: Collins-Burow Et al.
    J Steroid Biochem Mol Biol 2012;132:186
  74. Estrogen-like activity of aqueous extract from Agrimonia pilosa Ledeb. in MCF-7 cells.
    Authors: Lee Et al.
    Endocrinology 2012;12:260
  75. Inhibition of XO or NOX attenuates diethylstilbestrol-induced endothelial nitric oxide deficiency without affecting its effects on LNCaP cell invasion and apoptosis.
    Authors: Youn Et al.
    Clin Sci (Lond) 2012;123:509
  76. 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.
    Authors: Guido Et al.
    Int J Clin Exp Pathol 2012;11:2911
  77. 17β-Estradiol enhances breast cancer cell motility and invasion via extra-nuclear activation of actin-binding protein ezrin.
    Authors: Zheng Et al.
    PLoS One 2011;6:e22439
  78. mTOR controls ovarian follicle growth by regulating granulosa cell proliferation.
    Authors: Yu Et al.
    PLoS One 2011;6:e21415
  79. Daidzein prevents the increase in CD4+CD28null T cells and B lymphopoesis in ovariectomized mice: a key mechanism for anti-osteoclastogenic effect.
    Authors: Tyagi Et al.
    PLoS One 2011;6:e21216
  80. The effect of 17β-estradiol on cholesterol content in human macrophages is influenced by the lipoprotein milieu.
    Authors: Corcoran Et al.
    Clin Cancer Res 2011;47:109
  81. Complete estrogen receptor blocker ICI182,780 promotes the proliferation of vascular smooth muscle cells.
    Authors: He Et al.
    Acta Biochim Biophys Sin (Shanghai) 2011;43:118
  82. Selective mutations in estrogen receptor alpha D-domain alters nuclear translocation and non-estrogen response element gene regulatory mechanisms.
    Authors: Burns Et al.
    J Biol Chem 2011;286:12640
  83. Tamoxifen increases nuclear respiratory factor 1 transcription by activating estrogen receptor beta and AP-1 recruitment to adjacent promoter binding sites.
    Authors: Ivanova Et al.
    FASEB J 2011;25:1402
  84. The liver receptor homolog-1 (LRH-1) is expressed in human islets and protects {β}-cells against stress-induced apoptosis.
    Authors: Baquié Et al.
    FEMS Immunol Med Microbiol 2011;20:2823
  85. 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.
    Authors: Hsu Et al.
    J Vet Sci 2011;18:61
  86. Expression and regulation of Enpp2 in rat uterus during the estrous cycle.
    Authors: Ahn Et al.
    Toxicol Sci 2011;12:379
  87. 17beta-Estradiol inhibits matrix metalloproteinase-2 transcription via MAP kinase in fibroblasts.
    Authors: Mahmoodzadeh Et al.
    Cardiovasc Res 2010;85:719
  88. Developmental exposures of male rats to soy isoflavones impact Leydig cell differentiation.
    Authors: Sherrill Et al.
    Biol Reprod 2010;83:488
  89. Interdependence of platelet-derived growth factor and estrogen-signaling pathways in inducing neonatal rat testicular gonocytes proliferation.
    Authors: Thuillier Et al.
    Biol Reprod 2010;82:825
  90. Hepatocyte growth factor system in the mouse uterus: variation across the estrous cycle and regulation by 17-β-estradiol and progesterone.
    Authors: Zhang
    Clin Cancer Res 2010;82:1037
  91. BRD7, a subunit of SWI/SNF complexes, binds directly to BRCA1 and regulates BRCA1-dependent transcription.
    Authors: Harte Et al.
    Cancer Res 2010;70:2538
  92. Estrogen suppresses MLK3-mediated apoptosis sensitivity in ER+ breast cancer cells.
    Authors: Rangasamy Et al.
    Cancer Res 2010;70:1731
  93. Cell cycle and anti-estrogen effects synergize to regulate cell proliferation and ER target gene expression.
    Authors: Dalvai and Bystricky
    PLoS One 2010;5:e11011
  94. Estrogen-receptor-mediated protection of cerebral endothelial cell viability and mitochondrial function after ischemic insult in vitro.
    Authors: Guo Et al.
    PLoS One 2010;30:545
  95. c-Jun activation is required for 4-hydroxytamoxifen-induced cell death in breast cancer cells.
    Authors: Madeo Et al.
    Oncogene 2010;29:978
  96. Estrogen receptor α (ERα) mediates 17β-estradiol (E2)-activated expression of HBO1.
    Authors: Wang Et al.
    Proc Natl Acad Sci U S A 2010;29:140
  97. 5-HT(1A), SST(1), and SST(2) receptors mediate inhibitory postsynaptic potentials in the submucous plexus of the guinea pig ileum.
    Authors: Foong Et al.
    Receptors Clin Investig 2010;298:G384
  98. Bisphenol A and estradiol are equipotent in antagonizing cisplatin-induced cytotoxicity in breast cancer cells.
    Authors: LaPensee Et al.
    Cancer Res 2010;290:167
  99. 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 recept
    Authors: Sunters Et al.
    J Biol Chem 2010;285:8743
  100. Androgen receptor-dependent transactivation of growth arrest-specific gene 6 mediates inhibitory effects of testosterone on vascular calcification.
    Authors: Son Et al.
    J Biol Chem 2010;285:7537
  101. Proinflammatory cytokines enhance estrogen-dependent expression of the multidrug transporter gene ABCG2 through estrogen receptor and NF{kappa}B cooperativity at adjacent response elements.
    Authors: Pradhan Et al.
    J Biol Chem 2010;285:31100
  102. 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.
    Authors: Suzuki Et al.
    J Biol Chem 2010;285:13444
  103. Estrogen receptor-alpha promotes breast cancer cell motility and invasion via focal adhesion kinase and N-WASP.
    Authors: Sanchez Et al.
    Mol Endocrinol 2010;24:2114
  104. Unexpected hormonal activity of a catechol equine estrogen metabolite reveals reversible glutathione conjugation.
    Authors: Peng Et al.
    Chem Res Toxicol 2010;23:1374
  105. Roles of 17β-estradiol involve regulation of reelin expression and synaptogenesis in the dentate gyrus.
    Authors: Bender Et al.
    Cereb Cortex 2010;20:2985
  106. Proliferation of human mammary cancer cells exposed to 27-hydroxycholesterol.
    Authors: Cruz Et al.
    J Expo Sci Environ Epidemiol 2010;1:531
  107. B7-H1-dependent sex-related differences in tumor immunity and immunotherapy responses.
    Authors: Lin Et al.
    J Immunol 2010;185:2747
  108. Estradiol suppresses NF-kappa B activation through coordinated regulation of let-7a and miR-125b in primary human macrophages.
    Authors: Murphy Et al.
    J Immunol 2010;184:5029
  109. Prolactin and oestrogen synergistically regulate gene expression and proliferation of breast cancer cells.
    Authors: Rasmussen Et al.
    Endocr Relat Cancer 2010;17:809
  110. Progesterone increases systemic and local uterine proportions of CD4+CD25+ Treg cells during midterm pregnancy in mice.
    Authors: Mao Et al.
    Endocrinology 2010;151:5477
  111. Estrogen stimulates proliferation and differentiation of neural stem/progenitor cells through different signal transduction pathways.
    Authors: Okada Et al.
    Am J Physiol Heart Circ Physiol 2010;11:4114
  112. Bisphenol A impairs the double-strand break repair machinery in the germline and causes chromosome abnormalities.
    Authors: Allard and Colaiácovo
    Proc Natl Acad Sci U S A 2010;107:20405
  113. Autocrine regulation of cell proliferation by estrogen receptor-alpha in estrogen receptor-alpha-positive breast cancer cell lines.
    Authors: Tan Et al.
    BMC Cancer 2009;9:31
  114. Blockade of estrogen action upregulates estrogen receptor-alpha mRNA in the fetal brain.
    Authors: Schaub and Wood
    Neonatology 2009;96:115
  115. The estrogen receptor alpha pathway induces oncogenic Wip1 phosphatase gene expression.
    Authors: Han Et al.
    Mol Cancer Res 2009;7:713
  116. Tamoxifen inhibits TRPV6 activity via estrogen receptor-independent pathways in TRPV6-expressing MCF-7 breast cancer cells.
    Authors: Bolanz Et al.
    Mol Cancer Res 2009;7:2000
  117. Characterization of a novel small molecule subtype specific estrogen-related receptor alpha antagonist in MCF-7 breast cancer cells.
    Authors: Chisamore Et al.
    PLoS One 2009;4:e5624
  118. The oxysterol receptor LXR inhibits proliferation of human breast cancer cells.
    Authors: Vedin Et al.
    Cancer Res 2009;30:575
  119. CRK7 modifies the MAPK pathway and influences the response to endocrine therapy.
    Authors: Iorns Et al.
    Carcinogenesis 2009;30:1696
  120. Estradiol-induced estrogen receptor-α trafficking.
    Authors: Bondar Et al.
    Mol Cell Endocrinol 2009;29:15323
  121. Cytoskeletal changes underlie estrogen's acute effects on synaptic transmission and plasticity.
    Authors: Kramár Et al.
    Hum Mol Genet 2009;29:12982
  122. K+-dependent Na+/Ca2+ exchanger 3 is involved in renal active calcium transport and is differentially expressed in the mouse kidney.
    Authors: Lee Et al.
    Am J Physiol Renal Physiol 2009;297:F371
  123. A novel mechanism of natural vitamin E tocotrienol activity: involvement of ERbeta signal transduction.
    Authors: Comitato Et al.
    Am J Physiol Endocrinol Metab 2009;297:E427
  124. Mutational analysis of progesterone receptor functional domains in stable cell lines delineates sets of genes regulated by different mechanisms.
    Authors: Quiles Et al.
    Mol Endocrinol 2009;23:809
  125. Mechanism of the salutary effects of estrogen on kupffer cell phagocytic capacity following trauma-hemorrhage: pivotal role of Akt activation.
    Authors: Hsieh Et al.
    J Immunol 2009;182:4406
  126. Differential actions of estrogen and SERMs in regulation of the actin cytoskeleton of endometrial cells.
    Authors: Flamini Et al.
    Mol Hum Reprod 2009;15:675
  127. Soy phytoestrogens are neuroprotective against stroke-like injury in vitro.
    Authors: Schreihofer and Redmond
    Neuroscience 2009;158:602
  128. 17Beta-estradiol at low concentrations acts through distinct pathways in normal versus benign prostatic hyperplasia-derived prostate stromal cells.
    Authors: Park Et al.
    Endocrinology 2009;150:4594
  129. Identification of the potent phytoestrogen glycinol in elicited soybean (Glycine max).
    Authors: Boue Et al.
    Endocrinology 2009;150:2446
  130. Hes-6, an inhibitor of Hes-1, is regulated by 17β-estradiol and promotes breast cancer cell proliferation.
    Authors: Hartman Et al.
    Arthritis Res Ther 2009;11:R79
  131. Estrogen determines sex differences in airway responsiveness after allergen exposure.
    Authors: Matsubara Et al.
    Reprod Sci 2008;38:501
  132. Estrogen prevents intestinal inflammation after trauma-hemorrhage via downregulation of angiotensin II and angiotensin II subtype I receptor.
    Authors: Chen Et al.
    J Mol Endocrinol 2008;295:G1131
  133. Tyrosine phosphorylation of the nuclear receptor coactivator AIB1/SRC-3 is enhanced by Abl kinase and is required for its activity in cancer cells.
    Authors: Oh Et al.
    Mol Cell Biol 2008;28:6580
  134. 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.
    Authors: Subtil-Rodríguez Et al.
    Mol Cell Biol 2008;28:3830
  135. Hormonal regulation of BCRP expression in human placental BeWo cells.
    Authors: Wang Et al.
    Pharm Res 2008;25:444
  136. Differential regulation of the inducible nitric oxide synthase gene by estrogen receptors 1 and 2.
    Authors: Tsutsumi Et al.
    Tissue Eng Part C Methods 2008;199:267
  137. The expression and ovarian steroid regulation of endometrial micro-RNAs.
    Authors: Toloubeydokhti Et al.
    J Exp Clin Cancer Res 2008;15:993
  138. Roles of estrogen receptor alpha and beta in modulating urothelial cell proliferation.
    Authors: Teng Et al.
    Endocr Relat Cancer 2008;15:351
  139. Effects of estradiol and progesterone on the proinflammatory cytokine production by mononuclear cells from patients with chronic hepatitis C.
    Authors: Yuan Et al.
    World J Gastroenterol 2008;14:2200
  140. Estrogen-enhanced gene expression of lipoprotein lipase in heart is antagonized by progesterone.
    Authors: Liu Et al.
    Endocrinology 2008;149:711
  141. The novel estrogen receptor, G protein-coupled receptor 30, mediates the proliferative effects induced by 17β-estradiol on mouse spermatogonial GC-1 cell line.
    Authors: Sirianni Et al.
    Int J Oncol 2008;149:5043
  142. The nutritional flavanone naringenin triggers antiestrogenic effects by regulating estrogen receptor alpha-palmitoylation.
    Authors: Galluzzo Et al.
    Endocrinology 2008;149:2567
  143. Identification of CDK10 as an important determinant of resistance to endocrine therapy for breast cancer.
    Authors: Iorns Et al.
    Cancer Cell 2008;13:91
  144. Differential expression of microRNAs in myometrium and leiomyomas and regulation by ovarian steroids.
    Authors: Pan Et al.
    J Biol Chem 2008;12:227
  145. G-protein-coupled receptor 30 and estrogen receptor-alpha are involved in the proliferative effects induced by atrazine in ovarian cancer cells.
    Authors: Albanito Et al.
    Environ Health Perspect 2008;116:1648
  146. Blockade of estrogen receptors decreases CNS and pituitary prostaglandin synthase expression in fetal sheep.
    Authors: Schaub Et al.
    FASEB J 2007;87:121
  147. Definition of functionally important mechanistic differences among selective estrogen receptor down-regulators.
    Authors: Wittmann Et al.
    Cancer Res 2007;67:9549
  148. 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.
    Authors: Albanito Et al.
    Cancer Res 2007;67:1859
  149. NM23-H2, an estrogen receptor β-associated protein, shows diminished expression with progression of atherosclerosis.
    Authors: Rayner Et al.
    Reprod Sci 2007;292:R743
  150. Regulation of GREB1 transcription by estrogen receptor α through a multipartite enhancer spread over 20 kb of upstream flanking sequences.
    Authors: Deschênes Et al.
    BMC Complement Altern Med 2007;282:17335
  151. The silencing mediator of retinoic acid and thyroid hormone receptor (SMRT) corepressor is required for full estrogen receptor alpha transcriptional activity.
    Authors: Peterson Et al.
    Mol Cell Biol 2007;27:5933
  152. 17β-Estradiol utilizes the estrogen receptor to regulate CD16 expression in monocytes.
    Authors: Kramer Et al.
    Stroke 2007;279:16
  153. Kruppel-like factor 9 is a negative regulator of ligand-dependent estrogen receptor alpha signaling in Ishikawa endometrial adenocarcinoma cells.
    Authors: Velarde Et al.
    Mol Endocrinol 2007;21:2988
  154. Modulation of estrogen receptor α protein level and survival function by DBC-1.
    Authors: Trauernicht Et al.
    Br J Pharmacol 2007;21:1526
  155. Neuroprotection by estrogen against MPP+-induced dopamine neuron death is mediated by ERα in primary cultures of mouse mesencephalon.
    Authors: Bains Et al.
    Biol Reprod 2007;204:767
  156. Resveratrol inhibits expression and binding activity of the monocyte chemotactic protein-1 receptor, CCR2, on THP-1 monocytes.
    Authors: Cullen Et al.
    Atherosclerosis 2007;195:e125
  157. Activation of estrogen receptor-mediated gene transcription by the equine estrogen metabolite, 4-methoxyequilenin, in human breast cancer cells.
    Authors: Chang Et al.
    Endocrinology 2007;148:4793
  158. Exposure to phytoestrogens in the perinatal period affects androgen secretion by testicular Leydig cells in the adult rat.
    Authors: Akingbemi Et al.
    Endocrinology 2007;148:4475
  159. Estradiol-17beta regulates mouse uterine epithelial cell proliferation through insulin-like growth factor 1 signaling.
    Authors: Zhu and Pollard
    Proc Natl Acad Sci U S A 2007;104:15847
  160. Additive growth inhibitory effects of ibandronate and antiestrogens in estrogen receptor-positive breast cancer cell lines.
    Authors: Journé Et al.
    Cancer Res 2006;8:R2
  161. Farnesyl-transferase inhibitor R115,777 enhances tamoxifen inhibition of MCF-7 cell growth through estrogen receptor dependent and independent pathways.
    Authors: Dalenc Et al.
    Breast Cancer Res 2006;7:R1159
  162. 17beta-estradiol, genistein, and 4-hydroxytamoxifen induce the proliferation of thyroid cancer cells through the g protein-coupled receptor GPR30.
    Authors: Vivacqua Et al.
    Mol Pharmacol 2006;70:1414
  163. Estrogens, selective estrogen receptor modulators, and a selective estrogen receptor down-regulator inhibit endothelial production of tissue factor pathway inhibitor 1.
    Authors: Dahm Et al.
    BMC Cardiovasc Disord 2006;6:40
  164. Cyclin D1 is necessary for tamoxifen-induced cell cycle progression in human breast cancer cells.
    Authors: Kilker and Planas-Silva
    Breast Cancer Res 2006;66:11478
  165. Efficient intracellular multiplication of Legionella pneumophila in human monocytes requires functional host cell L-type calcium channels.
    Authors: Wieland Et al.
    Am J Physiol Gastrointest Liver Physiol 2006;47:296
  166. 17β-Estradiol inhibits subarachnoid hemorrhage-induced inducible nitric oxide synthase gene expression by interfering with the nuclear factor κ B transactivation.
    Authors: Shih Et al.
    Proc Natl Acad Sci U S A 2006;37:3025
  167. Convergent transcriptional profiles induced by endogenous estrogen and distinct xenoestrogens in breast cancer cells.
    Authors: Buterin Et al.
    Carcinogenesis 2006;27:1567
  168. Antiestrogens and the formation of DNA damage in rats: a comparison.
    Authors: Kim Et al.
    Infect Immun 2006;19:852
  169. Activation of insulin-like growth factor I receptor-mediated pathway by ginsenoside Rg1.
    Authors: Chen Et al.
    Br J Pharmacol 2006;147:542
  170. Biological role of estrogen receptor β in salivary gland adenocarcinoma cells.
    Authors: Ohshiro Et al.
    Exp Ther Med 2006;12:5994
  171. The estrogenic effect of bisphenol A disrupts pancreatic β-cell function in vivo and induces insulin resistance.
    Authors: Alonso-Magdalena Et al.
    Am J Physiol Gastrointest Liver Physiol 2006;114:106
  172. Disruption of estrogen receptor DNA-binding domain and related intramolecular communication restores tamoxifen sensitivity in resistant breast cancer.
    Authors: Wang Et al.
    BMC Immunol 2006;10:487
  173. A model of acquired autoresistance to a potent ErbB2 tyrosine kinase inhibitor and a therapeutic strategy to prevent its onset in breast cancer.
    Authors: Xia Et al.
    Br J Cancer 2006;103:7795
  174. An inherent role of microtubule network in the action of nuclear receptor.
    Authors: Manavathi Et al.
    J Endocrinol 2006;103:15981
  175. Estrogen receptor signaling protects against immune suppression by UV radiation exposure.
    Authors: Widyarini Et al.
    Neuroendocrinology 2006;103:12837
  176. Estrogen receptor alpha pathway is involved in the regulation of Calbindin-D9k in the uterus of immature rats.
    Authors: Lee Et al.
    Toxicol Sci 2005;84:270
  177. Membrane estrogen receptor-alpha levels predict estrogen-induced ERK1/2 activation in MCF-7 cells.
    Authors: Zivadinovic and Watson
    Breast Cancer Res 2005;7:R130
  178. 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.
    Authors: Crane-Godreau and Wira
    Breast Cancer Res Treat 2005;73:4231
  179. Estren promotes androgen phenotypes in primary lymphoid organs and submandibular glands.
    Authors: Islander Et al.
    Reprod Nutr Dev 2005;6:16
  180. Estrogen increases mitochondrial efficiency and reduces oxidative stress in cerebral blood vessels.
    Authors: Stirone Et al.
    Mol Pharmacol 2005;68:959
  181. Regulation of endogenous gene expression in human non-small cell lung cancer cells by estrogen receptor ligands.
    Authors: Hershberger Et al.
    Cancer Cell 2005;65:1598
  182. The effects of dietary phytoestrogens on aromatase activity in human endometrial stromal cells.
    Authors: Edmunds Et al.
    Environ Health Perspect 2005;45:709
  183. Formation of an IKKalpha-dependent transcription complex is required for estrogen receptor-mediated gene activation.
    Authors: Park Et al.
    Mol Cell 2005;18:71
  184. Palmitoylation-dependent estrogen receptor alpha membrane localization: regulation by 17beta-estradiol.
    Authors: Acconcia Et al.
    Mol Biol Cell 2005;16:231
  185. Progesterone antagonizes the permissive action of estradiol on tumor necrosis factor-α-induced apoptosis of anterior pituitary cells.
    Authors: Candolfi Et al.
    Proc Natl Acad Sci U S A 2005;146:736
  186. Firing pattern and rapid modulation of activity by estrogen in primate luteinizing hormone releasing hormone-1 neurons.
    Authors: Abe and Terasawa
    Endocrinology 2005;146:4312
  187. Estrogen modulates endothelial and neuronal nitric oxide synthase expression via an estrogen receptor beta-dependent mechanism in hypothalamic slice cultures.
    Authors: Gingerich and Krukoff
    Endocrinology 2005;146:2933
  188. Identification of target genes in breast cancer cells directly regulated by the SRC-3/AIB1 coactivator.
    Authors: Labhart Et al.
    Proc Natl Acad Sci U S A 2005;102:1339
  189. Steroid-free medium discloses oestrogenic effects of the bisphosphonate clodronate on breast cancer cells.
    Authors: Journe Et al.
    Breast Cancer Res 2004;91:1703
  190. 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.
    Authors: Levine
    Proc Natl Acad Sci U S A 2004;4:49
  191. Age-related reduction in estrogen receptor-mediated mechanisms of vascular relaxation in female spontaneously hypertensive rats.
    Authors: Wynne Et al.
    Hypertension 2004;43:405
  192. Wnt/β-catenin and estrogen signaling converge in vivo.
    Authors: Kouzmenko Et al.
    Am J Respir Cell Mol Biol 2004;279:40255
  193. The G protein-coupled receptor GPR30 mediates c-fos up-regulation by 17beta-estradiol and phytoestrogens in breast cancer cells.
    Authors: Maggiolini Et al.
    J Biol Chem 2004;279:27008
  194. Morphological effects of estrogen on cholinergic neurons in vitro involves activation of extracellular signal-regulated kinases.
    Authors: Dominguez Et al.
    Carcinogenesis 2004;24:982
  195. HES-1 inhibits 17β-estradiol and heregulin-β1-mediated upregulation of E2F-1.
    Authors: Hartman Et al.
    J Cell Mol Med 2004;23:8826
  196. Nuclear insulin receptor substrate 1 interacts with estrogen receptor alpha at ERE promoters.
    Authors: Morelli Et al.
    Oncogene 2004;23:7517
  197. Estrogen receptor beta isoforms exhibit differences in ligand-activated transcriptional activity in an estrogen response element sequence-dependent manner.
    Authors: Ramsey Et al.
    Endocrinology 2004;145:149
  198. Xenoestrogen-induced ERK-1 and ERK-2 activation via multiple membrane-initiated signaling pathways.
    Authors: Bulayeva and Watson
    Environ Health Perspect 2004;112:1481
  199. Human epidermal growth factor receptor 2 status modulates subcellular localization of and interaction with estrogen receptor α in breast cancer cells.
    Authors: Yang Et al.
    Oncogene 2004;10:3621
  200. Regulation of PDGF production and ERK activation by estrogen is associated with TSC2 gene expression.
    Authors: Finlay Et al.
    Am J Physiol Cell Physiol 2003;285:C409
  201. 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.
    Authors: Kimmins Et al.
    Reprod Biol Endocrinol 2003;1:38
  202. Inhibition of prolactin (PRL)-induced proliferative signals in breast cancer cells by a molecular mimic of phosphorylated PRL, S179D-PRL.
    Authors: Schroeder Et al.
    Biomol Ther (Seoul) 2003;144:5300
  203. Environmental estrogens alter early development in Xenopus laevis.
    Authors: Bevan Et al.
    J Endocrinol 2003;111:488
  204. Involvement of bone morphogenetic protein 4 (BMP-4) in pituitary prolactinoma pathogenesis through a Smad/estrogen receptor crosstalk.
    Authors: Paez-Pereda Et al.
    BMC Cancer 2003;100:1034
  205. Testosterone attenuates expression of vascular cell adhesion molecule-1 by conversion to estradiol by aromatase in endothelial cells: implications in atherosclerosis.
    Authors: Mukherjee Et al.
    Mol Endocrinol 2002;99:4055
  206. Estradiol reduces F2α-isoprostane production in cultured human endothelial cells.
    Authors: Hermenegildo Et al.
    Biol Reprod 2002;283:H2644
  207. Receptor-mediated ethinylestradiol-induced oxidative DNA damage in rat testicular cells.
    Authors: Wellejus and Loft
    Proc Natl Acad Sci U S A 2002;16:195
  208. 17-β-oestradiol-induced vasorelaxation in vitro is mediated by eNOS through hsp90 and akt/pkb dependent mechanism.
    Authors: Bucci Et al.
    Drug Metab Dispos 2002;135:1695
  209. Estrogen alters thresholds for B cell apoptosis and activation.
    Authors: Grimaldi Et al.
    J Clin Invest 2002;109:1625
  210. The antioxidant neuroprotective effects of estrogens and phenolic compounds are independent from their estrogenic properties.
    Authors: Moosmann and Behl
    Chem Res Toxicol 1999;96:8867
  211. Estrogen receptor (ER) modulators each induce distinct conformational changes in ER α and ER β.
    Authors: Paige Et al.
    J Biomed Sci 1999;96:3999
  212. Estradiol induces the calcium-dependent translocation of endothelial nitric oxide synthase.
    Authors: Goetz Et al.
    J Neurosci 1999;96:2788
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