ICI 182,780

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Cat.No. 1047 - ICI 182,780 | C32H47F5O3S | CAS No. 129453-61-8
Description: Estrogen receptor antagonist
Chemical Name: 7α,17β-[9-[(4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol
Purity: ≥99% (HPLC)
Datasheet
Citations (212)
Literature
Pathways

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.

Compound Libraries

ICI 182,780 is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 606.77
Formula C32H47F5O3S
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 129453-61-8
PubChem ID 17756771
InChI Key VWUXBMIQPBEWFH-LQKBAPIOSA-N
Smiles OC1=CC=C2C(C[C@@H](CCCCCCCCCS(CCCC(F)(C(F)(F)F)F)=O)C3([H])[C@@]([H])2CC[C@@]4(C)[C@@](CC[C@@H]4O)3[H])=C1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 60.68 100
ethanol 30.34 50

Preparing Stock Solutions

The following data is based on the product molecular weight 606.77. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.65 mL 8.24 mL 16.48 mL
5 mM 0.33 mL 1.65 mL 3.3 mL
10 mM 0.16 mL 0.82 mL 1.65 mL
50 mM 0.03 mL 0.16 mL 0.33 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

Thomas et al (2005) Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. Endocrinology. 146 624 PMID: 15539556

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 ICI 182,780, please let us know.

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Keywords: ICI 182,780, supplier, High, affinity, GPR30, agonist, Estrogen, receptors, antagonists, ER, ERR, ICI182780, AstraZeneca, GPER, Estrogen, and, Related, Receptors, Tocris Bioscience

212 Citations for ICI 182,780

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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 recept J Biol Chem 285 8743 PMID: 20042609

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Stender (2017) Structural and molecular mechanisms of cytokine-mediated endocrine resistance in human breast cancer cells. Mol Cell 65 1122 PMID: 28306507

Zhu (2017) Differential and directional estrogenic signaling pathways induced by enterolignans and their precursors. PLoS One 12 e0171390 PMID: 28152041

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

Mao et al (2016) Antiestrogen resistant cell lines expressing estrogen receptor α mutations upregulate the unfolded protein response and are killed by BHPI Scientific Reports 6 34753 PMID: 27713477

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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


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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Nuclear Receptors

Nuclear Receptors Product Listing

A collection of over 150 products for key nuclear receptors, the listing includes research tools for the study of:

  • Androgen Receptors
  • Estrogen Receptors
  • Retinoic Acid Receptors
  • Retinoid X Receptors
  • Vitamin D Receptors

Pathways for ICI 182,780

Estrogen

Estrogen Signaling Pathway

Estrogen is a steroid hormone that is responsible for the regulation of growth, differentiation and function of the reproductive system. Estrogen signaling is often dysregulated in breast cancer and osteoporosis.

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