estrogen antagonists

Summary

Summary: Compounds which inhibit or antagonize the action or biosynthesis of estrogenic compounds.

Top Publications

  1. ncbi Double-blind, randomized trial comparing the efficacy and tolerability of fulvestrant versus anastrozole in postmenopausal women with advanced breast cancer progressing on prior endocrine therapy: results of a North American trial
    C K Osborne
    Breast Center at Baylor College of Medicine, 1 Baylor Plaza, MS 600, Houston, TX 77030, USA
    J Clin Oncol 20:3386-95. 2002
  2. ncbi Tamoxifen for prevention of breast cancer: report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study
    B Fisher
    National Surgical Adjuvant Breast and Bowel Project, Allegheny University of the Health Sciences, Pittsburgh, PA 15212 5234, USA
    J Natl Cancer Inst 90:1371-88. 1998
  3. ncbi The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen
    A K Shiau
    Howard Hughes Medical Institute and the Department of Biochemistry and Biophysics, University of California at San Francisco, 94143 0448, USA
    Cell 95:927-37. 1998
  4. pmc Estradiol downregulates miR-21 expression and increases miR-21 target gene expression in MCF-7 breast cancer cells
    Nalinie S Wickramasinghe
    Department of Biochemistry and Molecular Biology, Center for Genetics and Molecular Medicine, University of Louisville School of Medicine, Louisville, KY 40292, USA
    Nucleic Acids Res 37:2584-95. 2009
  5. ncbi Mechanisms of tamoxifen resistance
    Alistair Ring
    Academic Department of Biochemistry, Royal Marsden Hospital, Fulham Rd, London SW3 6JJ, UK
    Endocr Relat Cancer 11:643-58. 2004
  6. ncbi The estrogen receptor: a model for molecular medicine
    Elwood V Jensen
    Department of Cell Biology, Vontz Center for Molecular Studies, University of Cincinnati, Ohio 45267, USA
    Clin Cancer Res 9:1980-9. 2003
  7. ncbi Changes in breast cancer biomarkers in the IGF1R/PI3K pathway in recurrent breast cancer after tamoxifen treatment
    S C Drury
    Translational Research, The Breakthrough Breast Cancer Research Centre, London, UK
    Endocr Relat Cancer 18:565-77. 2011
  8. ncbi The estrogen receptor beta-isoform (ERbeta) of the human estrogen receptor modulates ERalpha transcriptional activity and is a key regulator of the cellular response to estrogens and antiestrogens
    J M Hall
    Department of Pharmacology and Cancer Biology, Duke University, Medical Center, Durham, North Carolina 27710, USA
    Endocrinology 140:5566-78. 1999
  9. ncbi NFκB signaling is important for growth of antiestrogen resistant breast cancer cells
    Christina W Yde
    Breast Cancer Group, Cell Death and Metabolism, Danish Cancer Society Research Center, Strandboulevarden 49, 2100, Copenhagen Ø, Denmark
    Breast Cancer Res Treat 135:67-78. 2012
  10. pmc Development and evolution of therapies targeted to the estrogen receptor for the treatment and prevention of breast cancer
    V Craig Jordan
    Fox Chase Cancer Center, 333 Cottman Avenue, Philadelphia, PA 19111 2497, United States
    Steroids 72:7-25. 2007

Detail Information

Publications242 found, 100 shown here

  1. ncbi Double-blind, randomized trial comparing the efficacy and tolerability of fulvestrant versus anastrozole in postmenopausal women with advanced breast cancer progressing on prior endocrine therapy: results of a North American trial
    C K Osborne
    Breast Center at Baylor College of Medicine, 1 Baylor Plaza, MS 600, Houston, TX 77030, USA
    J Clin Oncol 20:3386-95. 2002
    ..To compare the efficacy and tolerability of fulvestrant (formerly ICI 182,780) with anastrozole in the treatment of advanced breast cancer in patients whose disease progresses on prior endocrine treatment...
  2. ncbi Tamoxifen for prevention of breast cancer: report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study
    B Fisher
    National Surgical Adjuvant Breast and Bowel Project, Allegheny University of the Health Sciences, Pittsburgh, PA 15212 5234, USA
    J Natl Cancer Inst 90:1371-88. 1998
    ..To test this hypothesis, the National Surgical Adjuvant Breast and Bowel Project initiated the Breast Cancer Prevention Trial (P-1) in 1992...
  3. ncbi The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen
    A K Shiau
    Howard Hughes Medical Institute and the Department of Biochemistry and Biophysics, University of California at San Francisco, 94143 0448, USA
    Cell 95:927-37. 1998
    ..These structures reveal the two distinct mechanisms by which structural features of OHT promote this "autoinhibitory" helix 12 conformation...
  4. pmc Estradiol downregulates miR-21 expression and increases miR-21 target gene expression in MCF-7 breast cancer cells
    Nalinie S Wickramasinghe
    Department of Biochemistry and Molecular Biology, Center for Genetics and Molecular Medicine, University of Louisville School of Medicine, Louisville, KY 40292, USA
    Nucleic Acids Res 37:2584-95. 2009
    ..These results are the first to demonstrate that E(2) represses the expression of an oncogenic miRNA, miR-21, by activating estrogen receptor in MCF-7 cells...
  5. ncbi Mechanisms of tamoxifen resistance
    Alistair Ring
    Academic Department of Biochemistry, Royal Marsden Hospital, Fulham Rd, London SW3 6JJ, UK
    Endocr Relat Cancer 11:643-58. 2004
    ..The experimental and clinical evidence supporting these mechanisms of tamoxifen resistance are discussed in this review...
  6. ncbi The estrogen receptor: a model for molecular medicine
    Elwood V Jensen
    Department of Cell Biology, Vontz Center for Molecular Studies, University of Cincinnati, Ohio 45267, USA
    Clin Cancer Res 9:1980-9. 2003
    ....
  7. ncbi Changes in breast cancer biomarkers in the IGF1R/PI3K pathway in recurrent breast cancer after tamoxifen treatment
    S C Drury
    Translational Research, The Breakthrough Breast Cancer Research Centre, London, UK
    Endocr Relat Cancer 18:565-77. 2011
    ..There is no evidence for IGF1R gain in tamoxifen resistance; increases in stathmin levels suggest that activation of the PI3K pathway may have contributed, but PTEN loss and PIK3CA hotspot mutations were relatively rare...
  8. ncbi The estrogen receptor beta-isoform (ERbeta) of the human estrogen receptor modulates ERalpha transcriptional activity and is a key regulator of the cellular response to estrogens and antiestrogens
    J M Hall
    Department of Pharmacology and Cancer Biology, Duke University, Medical Center, Durham, North Carolina 27710, USA
    Endocrinology 140:5566-78. 1999
    ....
  9. ncbi NFκB signaling is important for growth of antiestrogen resistant breast cancer cells
    Christina W Yde
    Breast Cancer Group, Cell Death and Metabolism, Danish Cancer Society Research Center, Strandboulevarden 49, 2100, Copenhagen Ø, Denmark
    Breast Cancer Res Treat 135:67-78. 2012
    ..Our results imply that targeting NFκB might serve as a potential novel treatment strategy for breast cancer patients with resistance toward antiestrogen...
  10. pmc Development and evolution of therapies targeted to the estrogen receptor for the treatment and prevention of breast cancer
    V Craig Jordan
    Fox Chase Cancer Center, 333 Cottman Avenue, Philadelphia, PA 19111 2497, United States
    Steroids 72:7-25. 2007
    ..Current clinical trials are addressing the value of aromatase inhibitors as chemopreventive agents for postmenopausal women...
  11. ncbi The human estrogen receptor-alpha is a ubiquitinated protein whose stability is affected differentially by agonists, antagonists, and selective estrogen receptor modulators
    A L Wijayaratne
    Department of Pharmacology and Molecular Cancer Biology, Duke University Medical Center, Durham, North Carolina 27710, USA
    J Biol Chem 276:35684-92. 2001
    ..We conclude that the different conformational states adopted by ERalpha in the presence of different ligands influence transcriptional activity directly by regulating cofactor binding and indirectly by modulating receptor stability...
  12. ncbi Estrogen-like activity of ginsenoside Rg1 derived from Panax notoginseng
    Robbie Y K Chan
    The Open Laboratory of Chirotechnology, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong, Peoples Republic of China
    J Clin Endocrinol Metab 87:3691-5. 2002
    ..Our results indicate that ginsenosides Rg1 has estrogen-like activity and should be classified as a novel class of potent phytoestrogen...
  13. ncbi Endoxifen (4-hydroxy-N-desmethyl-tamoxifen) has anti-estrogenic effects in breast cancer cells with potency similar to 4-hydroxy-tamoxifen
    Young Chai Lim
    Division of Clinical Pharmacology, Indiana University School of Medicine, 1001 West 10th Street, WD Myers Bldg, W7123, Indianapolis, Indiana 46202, USA
    Cancer Chemother Pharmacol 55:471-8. 2005
    ..We, therefore, determined the effect of endoxifen and 4-OH-Tam on 17beta-estradiol (E2)-induced PR mRNA expression in an estrogen receptor-positive human breast cancer cell line...
  14. pmc Estradiol stimulates transcription of nuclear respiratory factor-1 and increases mitochondrial biogenesis
    Kathleen A Mattingly
    Department of Biochemistry and Molecular Biology, University of Louisville School of Medicine, 580 South Preston Street, Louisville, Kentucky 40202, USA
    Mol Endocrinol 22:609-22. 2008
    ..Knockdown of NRF-1 blocked E(2) stimulation of mitochondrial biogenesis and activity, indicating a mechanism by which estrogens regulate mitochondrial function by increasing NRF-1 expression...
  15. ncbi The histone deacetylase inhibitor trichostatin A sensitizes estrogen receptor alpha-negative breast cancer cells to tamoxifen
    Eun Ryoung Jang
    Research Institute and Hospital, National Cancer Center, 411 764, Republic of Korea
    Oncogene 23:1724-36. 2004
    ..Together, these results show that the HDAC inhibitor TSA sensitized ER alpha-negative, antihormone-unresponsive breast cancer cells to tamoxifen treatment possibly by upregulating ER beta activity...
  16. ncbi Tamoxifen and metabolite concentrations in serum and breast cancer tissue during three dose regimens in a randomized preoperative trial
    Elton R Kisanga
    Hormone Laboratory, Haukeland University Hospital, Department of Medicine, and Centre for International Health, University of Bergen, Bergen, Norway
    Clin Cancer Res 10:2336-43. 2004
    ..Furthermore we studied tamoxifen effects on the cancer proliferation marker Ki-67, and on sex hormone-binding globulin (SHBG)...
  17. ncbi 17beta-Estradiol-induced enhancement of estrogen receptor biosynthesis via MAPK pathway in mouse skeletal muscle myoblasts
    J Hatae
    Department of Physiology, School of Medicine, Fukuoka University, 7 45 1 Nanakuma, Jonan ku, Fukuoka, 814 0180, Japan
    J Physiol Sci 59:181-90. 2009
    ..Further, the expression of ER in these cells may be significantly upregulated by estrogen itself via increased biosynthesis linked to membrane-bound ER and downstream MAPK-mediated signaling pathways...
  18. ncbi Estrogen receptors in human myeloma cells
    T Otsuki
    Department of Hygiene, Kawasaki Medical School, Kurashiki, Okayama, Japan
    Cancer Res 60:1434-41. 2000
    ....
  19. ncbi Breast cancer chemoprevention: risk-benefit effects of the antioestrogen tamoxifen
    Karen Brown
    Cancer Biomarkers and Prevention Group, The Biocentre, University of Leicester, University Road, Leicester, LE1 7RH, UK
    Expert Opin Drug Saf 1:253-67. 2002
    ....
  20. ncbi Human X-box binding protein-1 confers both estrogen independence and antiestrogen resistance in breast cancer cell lines
    Bianca P Gomez
    Department of Oncology and Lombardi Comprehensive Cancer Center, Georgetown University School of Medicine, 3970 Reservoir Rd, NW, Washington, DC 20057, USA
    FASEB J 21:4013-27. 2007
    ..XBP1 and/or the UPR may be a useful molecular target for the development of novel predictive and therapeutic strategies in breast cancer...
  21. ncbi Comparison of the short-term biological effects of 7alpha-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)-nonyl]estra-1,3,5, (10)-triene-3,17beta-diol (Faslodex) versus tamoxifen in postmenopausal women with primary breast cancer
    J F Robertson
    Department of Surgery, Nottingham City Hospital, Nottingham, United Kingdom
    Cancer Res 61:6739-46. 2001
    ..Reductions in tumor cell proliferative activity (as indicated by Ki67LI) show that ICI 182,780 is likely to have antitumor activity in the clinical setting...
  22. ncbi 4-Hydroxytamoxifen inhibits proliferation of multiple myeloma cells in vitro through down-regulation of c-Myc, up-regulation of p27Kip1, and modulation of Bcl-2 family members
    Juliette Gauduchon
    UFR de Medecine, Universite de Caen Basse Normandie, CHU Cote de Nacre, 14032 Caen Cedex, France
    Clin Cancer Res 11:2345-54. 2005
    ..Our approach was to analyze the in vitro effects of a selective estrogen receptor modulator, 4-hydroxytamoxifen (4-OHT), on six multiple myeloma cell lines...
  23. pmc Blockade of estrogen receptor signaling inhibits growth and migration of medulloblastoma
    Scott M Belcher
    Department of Pharmacology and Cell Biophysics University of Cincinnati College of Medicine, Cincinnati, Ohio 45267 0575, USA
    Endocrinology 150:1112-21. 2009
    ..These studies have revealed that functional ERbeta expression is a fundamental aspect of MD biology and has defined antiestrogen therapy as a potentially efficacious clinical approach to improve the long-term outcomes for MD patients...
  24. ncbi Development and characterization of a cell line that stably expresses an estrogen-responsive luciferase reporter for the detection of estrogen receptor agonist and antagonists
    Vickie S Wilson
    US Environmental Protection Agency, ORD, NHEERL, Reproductive Toxicology Division, Research Triangle Park, NC 27711, USA
    Toxicol Sci 81:69-77. 2004
    ..In addition, herein we also provide key protocol recommendations necessary to identify and eliminate common problems encountered in in vitro screening for estrogenicity...
  25. ncbi Intracellular pathways mediating estrogen-induced cholangiocyte proliferation in the rat
    Domenico Alvaro
    Department of Clinical Medicine, Division of Gastroenterology, University of Rome, La Sapienza, Rome, Italy
    Hepatology 36:297-304. 2002
    ..This might suggest that pharmacologic modulation of ER, ERK, and/or Src could be proposed for the treatment of human pathology characterized by dysregulation of cholangiocyte proliferation...
  26. ncbi Cross-talk between non-genomic and genomic signalling pathways--distinct effect profiles of environmental estrogens
    Elisabete Silva
    Centre for Toxicology, School of Pharmacy, University of London, 29 39 Brunswick Square, London, WC1N 1AX, UK
    Toxicol Appl Pharmacol 245:160-70. 2010
    ..Otherwise, chemicals devoid of ER affinity, such as beta-HCH, but with an effect profile otherwise similar to estrogens might be overlooked in safety testing...
  27. pmc Histone deacetylase 7 and FoxA1 in estrogen-mediated repression of RPRM
    Simeen Malik
    Department of Molecular and Cellular Biology, 3 Baylor College of Medicine, Houston, Texas 77030, USA
    Mol Cell Biol 30:399-412. 2010
    ....
  28. ncbi Tamoxifen and AEBS ligands induced apoptosis and autophagy in breast cancer cells through the stimulation of sterol accumulation
    Philippe de Medina
    Affichem, Toulouse, France
    Autophagy 5:1066-7. 2009
    ..Moreover these data give pharmacological clues to improve the apoptotic efficacy of AEBS ligands...
  29. ncbi Phosphatidylinositol 3-kinase/AKT-mediated activation of estrogen receptor alpha: a new model for anti-estrogen resistance
    R A Campbell
    Department of Surgery, Indiana University School of Medicine, Indianapolis 46202, USA
    J Biol Chem 276:9817-24. 2001
    ..Taken together, these results define a molecular link between activation of the PI 3-kinase/AKT survival pathways, hormone-independent activation of ERalpha, and inhibition of tamoxifen-induced apoptotic regression...
  30. ncbi Identification of tamoxifen-DNA adducts in the endometrium of women treated with tamoxifen
    S Shibutani
    Laboratory of Chemical Biology, Department of Pharmacological Sciences, Division of Oncology and Division of Obstetrics and Gynecology, School of Medicine, State University of New York at Stony Brook, Stony Brook, NY 11794, USA
    Carcinogenesis 21:1461-7. 2000
    ..The level of adducts found, coupled with the previous demonstration of their mutagenicity [Cancer Res., 59, 2091, 1999], suggest that a genotoxic mechanism may be responsible for TAM-induced endometrial cancer...
  31. ncbi The effect of raloxifene on risk of breast cancer in postmenopausal women: results from the MORE randomized trial. Multiple Outcomes of Raloxifene Evaluation
    S R Cummings
    Department of Medicine, University of California, San Francisco, USA
    JAMA 281:2189-97. 1999
    ..Raloxifene hydrochloride is a selective estrogen receptor modulator that has antiestrogenic effects on breast and endometrial tissue and estrogenic effects on bone, lipid metabolism, and blood clotting...
  32. ncbi Fulvestrant versus anastrozole for the treatment of advanced breast carcinoma in postmenopausal women: a prospective combined analysis of two multicenter trials
    John F R Robertson
    Department of Surgery, Nottingham City Hospital, Nottingham, United Kingdom
    Cancer 98:229-38. 2003
    ....
  33. ncbi Various phosphorylation pathways, depending on agonist and antagonist binding to endogenous estrogen receptor alpha (ERalpha), differentially affect ERalpha extractability, proteasome-mediated stability, and transcriptional activity in human breast cancer
    Veronique Marsaud
    Pharmacologie Cellulaire et Moléculaire des Anticancéreux, Unité Mixte de Recherche 8612, Centre National de la Recherche Scientifique, 92296 Chatenay Malabry, France
    Mol Endocrinol 17:2013-27. 2003
    ....
  34. pmc Phosphorylation of human estrogen receptor alpha by protein kinase A regulates dimerization
    D Chen
    CRC Laboratories, Department of Cancer Medicine, Division of Medicine, Imperial College of Science, Technology and Medicine, London W6 8RP, United Kingdom
    Mol Cell Biol 19:1002-15. 1999
    ..Thus, phosphorylation of ERalpha in the DNA binding domain provides a mechanism by which dimerization and thereby DNA binding by the estrogen receptor is regulated...
  35. ncbi Increasing tamoxifen dose in breast cancer patients based on CYP2D6 genotypes and endoxifen levels: effect on active metabolite isomers and the antiestrogenic activity score
    M F Barginear
    Division of Hematology and Medical Oncology, Department of Medicine, Mount Sinai School of Medicine, New York, New York, USA
    Clin Pharmacol Ther 90:605-11. 2011
    ..Further studies involving increasing/decreasing the Tam dosage based on the AAS may determine whether dose adjustment can optimize treatment and improve long-term survival...
  36. ncbi Stromal cell-derived factor 1, a novel target of estrogen receptor action, mediates the mitogenic effects of estradiol in ovarian and breast cancer cells
    Julie M Hall
    Receptor Biology Section, National Institute of Environmental Health Sciences, Research Triangle Park, North Carolina 27709, USA
    Mol Endocrinol 17:792-803. 2003
    ....
  37. ncbi Cellular and molecular pharmacology of antiestrogen action and resistance
    R Clarke
    Vincent T Lombardi Cancer Center, Georgetown University School of Medicine, Washington, DC 20007, USA
    Pharmacol Rev 53:25-71. 2001
    ..These include changes in oxidative stress responses, specific protein kinase C isoform activation, calmodulin function, and cell membrane structure/function...
  38. ncbi Estrogen receptor binding to DNA is not required for its activity through the nonclassical AP1 pathway
    M Jakacka
    Division of Endocrinology, Metabolism, and Molecular Medicine, Northwestern University Medical School, Chicago, Illinois 60611, USA
    J Biol Chem 276:13615-21. 2001
    ..These data supported a model in which ER-mediated transcriptional activation or repression is dependent on the ligand and the nature of the response element in the target gene...
  39. ncbi Identification of estrogen-responsive genes by complementary deoxyribonucleic acid microarray and characterization of a novel early estrogen-induced gene: EEIG1
    Dong yu Wang
    Department of Chemical Engineering and Applied Chemistry, University of Toronto, 200 College Street, Toronto, Ontario M5S 3E5, Canada
    Mol Endocrinol 18:402-11. 2004
    ..These results provide evidence that some estrogenic compounds differentially enhance the transcription of estrogen-regulated genes and suggest a role for EEIG1 in estrogen action...
  40. ncbi Synergistic activation of functional estrogen receptor (ER)-alpha by DNA methyltransferase and histone deacetylase inhibition in human ER-alpha-negative breast cancer cells
    X Yang
    The Johns Hopkins Oncology Center, Johns Hopkins University, Baltimore, Maryland 21231, USA
    Cancer Res 61:7025-9. 2001
    ..These data suggest that the activities of both DNMT1 and HDAC are key regulators of methylation-mediated ER gene silencing...
  41. ncbi Smad3 specific inhibitor, naringenin, decreases the expression of extracellular matrix induced by TGF-beta1 in cultured rat hepatic stellate cells
    Xingjun Liu
    National Laboratory of Biomacromolecules, Institute of Biophysics, Chinese Academy of Sciences, 15 Datun Road, Beijing, 100101, China
    Pharm Res 23:82-9. 2006
    ....
  42. ncbi Requirement of estrogen receptor-alpha in insulin-like growth factor-1 (IGF-1)-induced uterine responses and in vivo evidence for IGF-1/estrogen receptor cross-talk
    Diane M Klotz
    Laboratory of Molecular Carcinogenesis, NIEHS, National Institutes of Health, Research Triangle Park, North Carolina 27709, USA
    J Biol Chem 277:8531-7. 2002
    ....
  43. ncbi Determination of tamoxifen--DNA adducts in leukocytes from breast cancer patients treated with tamoxifen
    Atsushi Umemoto
    Department of Surgery, School of Medicine, University of Tokushima, Kuramoto cho 3 18 15, Tokushima 770 8503, Japan
    Chem Res Toxicol 17:1577-83. 2004
    ..6 +/- 3.0 adducts/10(9) nucleotides. No adducts were detected in the controls. The presence of TAM-DNA adducts in the leukocyte DNA samples was confirmed using several 32P-postlabeling/HPLC systems...
  44. ncbi Effects of estrogen antagonists and agonists on the ACTH response to restraint stress in female rats
    E A Young
    Department of Psychiatry and Mental Health Research Institute, University of Michigan, Ann Arbor, MI 48109 0729, USA
    Neuropsychopharmacology 25:881-91. 2001
    ..To determine whether estrogen contributes to this sex difference, we examined the effects of the estrogen antagonists tamoxifen and C1628 on the ACTH and corticosterone responses to restraint stress...
  45. ncbi Tamoxifen and toremifene concentrations in plasma are greatly decreased by rifampin
    K T Kivistö
    Department of Clinical Pharmacology, University of Helsinki, Finland
    Clin Pharmacol Ther 64:648-54. 1998
    ..Rifampin (INN, rifampicin) is a potent inducer of cytochrome P450 (CYP) enzymes involved in drug metabolism and therefore causes many drug interactions...
  46. ncbi Results of the ATAC (Arimidex, Tamoxifen, Alone or in Combination) trial after completion of 5 years' adjuvant treatment for breast cancer
    A Howell
    Christie Hospital, Manchester, UK
    Lancet 365:60-2. 2005
    ..Anastrozole should be the preferred initial treatment for postmenopausal women with localised hormone-receptor-positive breast cancer...
  47. ncbi Treatment with the pure antiestrogen faslodex (ICI 182780) induces tumor necrosis factor receptor 1 (TNFR1) expression in MCF-7 breast cancer cells
    K Smolnikar
    Institute of Morphology and Tumor Research, DSHS Cologne, Germany
    Breast Cancer Res Treat 63:249-59. 2000
    ..The superiority of the pure antiestrogen ICI to induce apoptosis in MCF-7 cells may result from its capability to modulate the induction of apoptosis via Bcl-2 as well as TNF-associated signal transduction pathways...
  48. ncbi The evolution of tamoxifen therapy in breast cancer: selective oestrogen-receptor modulators and downregulators
    Ruth M O'Regan
    Robert H Lurie Comprehensive Cancer Center, Northwestern University, Chicago, IL 60611, USA
    Lancet Oncol 3:207-14. 2002
    ..Furthermore, two different classes of hormonal agents, the aromatase inhibitors and oestrogen-receptor downregulators, which have no oestrogen-like properties at any site, are promising new treatments for breast cancer...
  49. ncbi Tamoxifen inhibits the release of arachidonic acid stimulated by thapsigargin in estrogen receptor-negative A549 cells
    J D Croxtall
    Department of Biochemical Pharmacology, The William Harvey Research Institute, St Bartholomew s and the Royal London School of Medicine and Dentistry, UK
    Biochim Biophys Acta 1349:275-84. 1997
    ....
  50. ncbi Estrogen and antiestrogens alter breast cancer invasiveness by modulating the transforming growth factor-β signaling pathway
    Natsuka Goto
    Graduate School of Life and Environmental Sciences, University of Tsukuba, Tsukuba, Japan
    Cancer Sci 102:1501-8. 2011
    ..The expression of these genes was not decreased by antiestrogens. These observations provide a new insight into estrogen function and the mechanisms underlying estrogen-mediated suppression of tumor progression...
  51. ncbi Overview of the main outcomes in breast-cancer prevention trials
    J Cuzick
    Cancer Research UK, London, UK
    Lancet 361:296-300. 2003
    ..Early findings on the use of tamoxifen or raloxifene as prophylaxis against breast cancer have been mixed; we update available data and overview the combined results...
  52. ncbi Fulvestrant: expanding the endocrine treatment options for patients with hormone receptor-positive advanced breast cancer
    Stephen Chia
    Division of Medical Oncology, British Columbia Cancer Agency, University of British Columbia, 600 West 10th Avenue, Vancouver, BC, V5Z 4E6, Canada
    Breast 17:S16-21. 2008
    ....
  53. ncbi Synergistic effects of ICI 182,780 on the cytotoxicity of cisplatin in cervical carcinoma cell lines
    Patricia Garcia-Lopez
    División de Investigación Básica, Instituto Nacional de Cancerología Av San Fernando 22, Tlalpan 14000, Apartado Postal 22026 México D F, Mexico
    Cancer Chemother Pharmacol 53:533-40. 2004
    ..We investigated the ability of the novel pure antiestrogen ICI 182,780 to modulate the cytotoxic effects of cisplatin in several cervical cancer cell lines...
  54. ncbi Continued breast cancer risk reduction in postmenopausal women treated with raloxifene: 4-year results from the MORE trial. Multiple outcomes of raloxifene evaluation
    J A Cauley
    Department of Epidemiology, University of Pittsburgh, PA 15261, USA
    Breast Cancer Res Treat 65:125-34. 2001
    ..Additional randomized clinical trials continue to evaluate this effect in postmenopausal women with osteoporosis, at risk for cardiovascular disease, and at high risk for breast cancer...
  55. ncbi Improved antitumoral properties of pure antiestrogen RU 58668-loaded liposomes in multiple myeloma
    Sébastien Maillard
    CNRS UMR 8612, Universite de Paris Sud, Chatenay Malabry, France
    J Steroid Biochem Mol Biol 100:67-78. 2006
    ..Thus, these combined enhanced activities of RU-liposomes support that such a delivery of an AE may constitute a strategy of benefit for MM treatment...
  56. ncbi Autophagy facilitates the progression of ERalpha-positive breast cancer cells to antiestrogen resistance
    Patricia V Schoenlein
    Department of Cellular Biology and Anatomy, Medical College of Georgia, Augusta, GA 30912, USA
    Autophagy 5:400-3. 2009
    ..We discuss the potential benefit of blocking autophagosome function to significantly reduce the emergence of antiestrogen-resistant breast cancer cells...
  57. ncbi Effects of tamoxifen on normal human dermal fibroblasts
    Mauro B Ruffy
    Wound Healing and Tissue Engineering Laboratory, Department of Otolaryngology Head and Neck Surgery, Stanford University Medical Center, Stanford, CA, USA
    Arch Facial Plast Surg 8:329-32. 2006
    ..To evaluate the effects of tamoxifen on the growth and autocrine growth factor production of human dermal fibroblasts from the face...
  58. ncbi Identification of PUMA as an estrogen target gene that mediates the apoptotic response to tamoxifen in human breast cancer cells and predicts patient outcome and tamoxifen responsiveness in breast cancer
    C G Roberts
    Cancer Research Program, Garvan Institute of Medical Research, Darlinghurst, New South Wales, Australia
    Oncogene 30:3186-97. 2011
    ..Moreover, they provide a convincing rationale for exploring new therapeutic approaches involving endocrine and non-endocrine therapies that target apoptotic pathways as an effective strategy for tackling endocrine refractory disease...
  59. ncbi Endocrine therapy in the treatment of metastatic breast cancer
    A U Buzdar
    Department of Breast Medical Oncology, M.D. Anderson Cancer Center, 1515 Holcombe Blvd, Houston, TX 77037, USA
    Semin Oncol 28:291-304. 2001
    ..Results are anxiously awaited from trials of new endocrine agents including the first member of a new class of endocrine agent, the estrogen-receptor downregulator class. Semin Oncol 28:291-304...
  60. ncbi Contrasting effects of prenyltransferase inhibitors on estrogen-dependent cell cycle progression and estrogen receptor-mediated transcriptional activity in MCF-7 cells
    Sophie F Doisneau-Sixou
    Département Innovation thérapeutique et Oncologie Moléculaire, Centre de Physiopathologie de Toulouse Purpan, Institut National de la Sante et de la Recherche Medicale U563, and Institut Claudius Regaud, 31052 Toulouse Cedex, France
    Endocrinology 144:989-98. 2003
    ..However, they antagonize the ability of ER alpha to stimulate estrogen response element-dependent transcriptional activity, acting presumably through coregulator complex formation...
  61. ncbi ICI 182,780 acts as a partial agonist and antagonist of estradiol effects in specific cells of the sheep uterus
    J A Robertson
    Department of Animal Science, Texas A and M University, College Station, TX 77843-2471, USA
    J Steroid Biochem Mol Biol 77:281-7. 2001
    ..Thus, we conclude that the agonist versus antagonist effects of ICI relative to those of E2 are a function of the gene examined as well as the specific cell within the uterus...
  62. ncbi A paraneoplastic retroperitoneal fibrosis resistant to corticosteroids treated with tamoxifen
    S Costanzi
    Renal Unit, Catholic University of the Sacred Heart, Rome, Italy
    Clin Nephrol 70:172-5. 2008
    ..Tamoxifen can be considered as an effective alternative to corticosteroids and immunosuppressors in treating RPF...
  63. ncbi Fulvestrant (ICI 182,780) sensitizes breast cancer cells expressing estrogen receptor alpha to vinblastine and vinorelbine
    Meihua Sui
    Program of Innovative Cancer Therapeutics, First Affiliated Hospital, Zhejiang University School of Medicine, 310003 Hangzhou, China
    Breast Cancer Res Treat 121:335-45. 2010
    ....
  64. ncbi ERBB2 influences the subcellular localization of the estrogen receptor in tamoxifen-resistant MCF-7 cells leading to the activation of AKT and RPS6KA2
    Sunil Pancholi
    Institute of Cancer Research, The Breakthrough Breast Cancer Research Centre, 237 Fulham Road, London SW3 6JB, UK
    Endocr Relat Cancer 15:985-1002. 2008
    ....
  65. pmc Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action
    C K Osborne
    Department of Medicine, Baylor College of Medicine, Houston, TX, USA
    Br J Cancer 90:S2-6. 2004
    ..Preclinical and clinical study data are presented in support of the novel mechanism of action of this new type of ER antagonist...
  66. ncbi Fulvestrant (ICI 182,780) down-regulates androgen receptor expression and diminishes androgenic responses in LNCaP human prostate cancer cells
    Rumi S Bhattacharyya
    Department of Medicine, Stanford University School of Medicine, Stanford, CA 94305 5103, USA
    Mol Cancer Ther 5:1539-49. 2006
    ..Our study suggests that AR down-regulation by ICI would be an effective strategy for the treatment of all prostate cancer, especially AR-dependent androgen-independent prostate cancer...
  67. ncbi Differential ligand activation of estrogen receptors ERalpha and ERbeta at AP1 sites
    K Paech
    Department of Pharmaceutical Chemistry, University of California, San Francisco, CA 94143 0446, USA
    Science 277:1508-10. 1997
    ..Thus, the two ERs signal in different ways depending on ligand and response element. This suggests that ERalpha and ERbeta may play different roles in gene regulation...
  68. ncbi Mechanisms of endocrine resistance and novel therapeutic strategies in breast cancer
    Nicola Normanno
    Cell Biology and Preclinical Models, INT Fondazione Pascale, Naples, Italy
    Endocr Relat Cancer 12:721-47. 2005
    ..More importantly, the knowledge of the mechanisms involved in the resistance of breast cancer cells to endocrine therapy offers potential for novel therapeutic strategies...
  69. pmc Influence of anastrozole (Arimidex), a selective, non-steroidal aromatase inhibitor, on in vivo aromatisation and plasma oestrogen levels in postmenopausal women with breast cancer
    J Geisler
    Department of Oncology, Haukeland University Hospital, Bergen, Norway
    Br J Cancer 74:1286-91. 1996
    ..Contrary to previous studies on other aromatase inhibitors, this study revealed an internal consistency between the percentage aromatase inhibition and suppression of plasma oestrone sulphate...
  70. ncbi Steroid receptor regulation of epidermal growth factor signaling through Src in breast and prostate cancer cells: steroid antagonist action
    Antimo Migliaccio
    Dipartimento di Patologia Generale, Facolta di Medicina e Chirurgia, II Universita di Napoli, Naples, Italy
    Cancer Res 65:10585-93. 2005
    ..Understanding of EGF-triggered growth and invasiveness of mammary and prostate cancer cells expressing steroid receptors is enhanced by this report, which reveals novel aspects of steroid receptor action...
  71. ncbi Crosstalk between EGFR and extranuclear steroid receptors
    Antimo Migliaccio
    Dipartimento di Patologia Generale, Facolta di Medicina e Chirurgia, II Universita di Napoli, Via L De Crecchio, 7 80138 Naples, Italy
    Ann N Y Acad Sci 1089:194-200. 2006
    ..In these cells, the AR/ER/Src complex is required for the EGF action, as the growth factor effects are abolished upon receptor silencing by specific SiRNAs and steroid antagonists or Src inhibition by the kinase inhibitor PP2...
  72. pmc Differential regulation of estrogen-inducible proteolysis and transcription by the estrogen receptor alpha N terminus
    Christopher C Valley
    Department of Physiology, 1300 University Ave, 120 SMI, University of Wisconsin Madison, Madison, Wisconsin 53706, USA
    Mol Cell Biol 25:5417-28. 2005
    ....
  73. ncbi Fulvestrant, formerly ICI 182,780, is as effective as anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment
    A Howell
    Department of Medical Oncology, Christie Hospital NHS Trust, Wilmslow Road, Manchester M20 4BX, United Kingdom
    J Clin Oncol 20:3396-403. 2002
    ..To compare the efficacy and tolerability of fulvestrant (formerly ICI 182,780) and anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment...
  74. ncbi Sequential tamoxifen and aminoglutethimide versus tamoxifen alone in the adjuvant treatment of postmenopausal breast cancer patients: results of an Italian cooperative study
    F Boccardo
    Professorial Unit of Medical Oncology, University and National Cancer Research Institute, Largo R Benzi 10, 16132 Genoa, Italy
    J Clin Oncol 19:4209-15. 2001
    ..To determine whether switching patients from tamoxifen to antiaromatase treatment would prevent some of the relapses or deaths that we assume would occur if tamoxifen were continued...
  75. ncbi Phytoestrogens restore nitric oxide-mediated relaxation in isolated pulmonary arteries from chronically hypoxic rats
    M R Karamsetty
    Division of Pulmonary and Critical Care Medicine, Rhode Island Hospital and Brown University School of Medicine, Providence, Rhode Island, USA
    J Pharmacol Exp Ther 297:968-74. 2001
    ....
  76. ncbi Breast cancer treatment outcome with adjuvant tamoxifen relative to patient CYP2D6 and CYP2C19 genotypes
    Werner Schroth
    Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, D 70376 Stuttgart, Germany
    J Clin Oncol 25:5187-93. 2007
    ..We investigated the predictive value of genetic variants of CYP2D6, CYP2C19, and three other cytochrome P450 enzymes for tamoxifen treatment outcome...
  77. ncbi Loss of tumourigenicity of stably ERbeta-transfected MCF-7 breast cancer cells
    D Behrens
    Max Delbrueck Center for Molecular Medicine, Experimental Pharmacology, Robert Roessle Strasse 10, 13125 Berlin, Germany
    Mol Cell Endocrinol 274:19-29. 2007
    ..These observations support the notion that ERbeta is a tumour suppressor and is exploitable in terms of cancer prevention, improving therapeutic response or predicting disease progression...
  78. ncbi Changes in expression of steroid receptors, their downstream target genes and their associated co-regulators during the sequential acquisition of tamoxifen resistance in vitro
    D J Scott
    Leeds Institute of Molecular Medicine, University of Leeds, Leeds, UK
    Int J Oncol 31:557-65. 2007
    ..Based on our results, it appears that increased co-activator expression, in concert with alterations in genes associated with controlling cell proliferation and survival contribute to TAMr in breast cancer...
  79. pmc Pathways to tamoxifen resistance
    Rebecca B Riggins
    Department of Oncology, Lombardi Comprehensive Cancer Center, Georgetown University, Washington, DC 20057, USA
    Cancer Lett 256:1-24. 2007
    ..Here, we review common mechanisms of antiestrogen resistance and discuss the implications for prediction of response and design of effective combinatorial treatments...
  80. ncbi Anti-estrogenic activity of mansorins and mansonones from the heartwood of Mansonia gagei DRUMM
    Ali Mahmoud El-Halawany
    Institute of Natural Medicine, University of Toyama, Toyama, Japan
    Chem Pharm Bull (Tokyo) 55:1332-7. 2007
    ..All the tested compounds showed higher binding affinities to ERbeta than to ERalpha in the yeast two-hybrid assay. Mansonones F and S showed the most potent estrogen binding and estrogen antagonistic effects...
  81. ncbi Oestrogen receptor beta is required for androgen-stimulated proliferation of LNCaP prostate cancer cells
    Marcello Maggiolini
    Department of Pharmaco Biology, University of Calabria, 87036 Rende CS, Italy
    J Mol Endocrinol 32:777-91. 2004
    ..Thus our findings implicate ERbeta as a potential target for the treatment of prostate tumours...
  82. ncbi Inhibition of histone deacetylase enhances the anti-proliferative action of antiestrogens on breast cancer cells and blocks tamoxifen-induced proliferation of uterine cells
    Leslie Hodges-Gallagher
    Department of Medicine, University of California, P O Box 1640, San Francisco, CA 94143, USA
    Breast Cancer Res Treat 105:297-309. 2007
    ..Our in vitro results suggest that VPA and other HDAC inhibitors have the potential to enhance hormonal therapy for ER alpha-positive breast cancer and simultaneously reverse the adverse effects of antiestrogens in the uterus...
  83. ncbi Differential SERM effects on corepressor binding dictate ERalpha activity in vivo
    Paul Webb
    Diabetes Center and the Department of Medicine, University of California, San Francisco, California 94143, USA
    J Biol Chem 278:6912-20. 2003
    ..Together, our results suggest that differential SERM effects on corepressor binding can explain differences in SERM effects on ERalpha activity. We propose a model for differential effects of SERMs on N-CoR binding...
  84. ncbi ER beta: identification and characterization of a novel human estrogen receptor
    S Mosselman
    N V Organon, Department of Biotechnology and Biochemistry, The Netherlands
    FEBS Lett 392:49-53. 1996
    ..Interestingly, the level of transactivation by 17 beta-estradiol is higher for ER alpha than for ER beta, which may reflect suboptimal conditions for ER beta at the level of the ligand, responsive element or cellular context...
  85. ncbi Novel antitumor effect of estradiol in athymic mice injected with a T47D breast cancer cell line overexpressing protein kinase Calpha
    M J Chisamore
    Robert H. Lurie Comprehensive Cancer Center, Northwestern University Medical School, Chicago, IL 60611, USA
    Clin Cancer Res 7:3156-65. 2001
    ..Furthermore, the finding that E2 has an antitumor effect on breast tumors overexpressing PKCalpha is a novel observation that may have important therapeutic implications...
  86. ncbi Letrozole is more effective neoadjuvant endocrine therapy than tamoxifen for ErbB-1- and/or ErbB-2-positive, estrogen receptor-positive primary breast cancer: evidence from a phase III randomized trial
    M J Ellis
    Duke University Breast Cancer Program, Duke University Comprehensive Cancer Center, Durham, NC 27710, USA
    J Clin Oncol 19:3808-16. 2001
    ..A neoadjuvant study for primary breast cancer that randomized treatment between letrozole and tamoxifen provided a context within which these issues could be addressed prospectively...
  87. ncbi Formulation and evaluation of sustained release microspheres of poly-lactide-co-glycolide containing tamoxifen citrate
    S Sehra
    Department of Pharmaceutical Sciences, Guru Jambheshwar Univeristy, Hisar, Haryana, India
    J Microencapsul 22:521-8. 2005
    ..Drug, polymer and PVA concentrations were varied to obtain optimum release profile for sustaining the action of drug...
  88. pmc BRG1/BRM and prohibitin are required for growth suppression by estrogen antagonists
    Sheng Wang
    Boston University School of Medicine, Cancer Research Center, Boston, MA 02118, USA
    EMBO J 23:2293-303. 2004
    b>Estrogen antagonists are universally employed in the breast cancer therapy, although antagonist therapy is limited by the inevitable development of cellular resistance...
  89. ncbi Locally produced estrogen promotes fetal rat metatarsal bone growth; an effect mediated through increased chondrocyte proliferation and decreased apoptosis
    A S Chagin
    Pediatric Endocrinology Unit, Department of Woman and Child Health, Karolinska Institute, Karolinska University Hospital, SE 171 76 Stockholm, Sweden
    J Endocrinol 188:193-203. 2006
    ..In addition, longitudinal growth is promoted by estrogens locally produced within the epiphyseal growth plate...
  90. ncbi Selective estrogen receptor modulators: discrimination of agonistic versus antagonistic activities by gene expression profiling in breast cancer cells
    Jonna Frasor
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine, 407 South Goodwin Avenue, Urbana, IL 61801, USA
    Cancer Res 64:1522-33. 2004
    ..Hence, gene expression profiling can discern fundamental differences among SERMs and provides insight into the distinct biologies of TOT, Ral, and ICI in breast cancer...
  91. ncbi Re-expression of estrogen receptor alpha using a tetracycline-regulated gene expression system induced estrogen-mediated growth inhibition of the MDA-MB-231 breast cancer cell line
    Arturo Barrón-González
    Department of Biochemistry and Molecular Biology, National Institute of Perinatology, Lomas de Virreyes, Mexico City, Mexico
    Biochem Cell Biol 82:335-42. 2004
    ..These results suggest that the re-expression of ER alpha in ER-negative breast cancer cells recreate, at least partially, a hormone-responsive phenotype and may be useful as a therapeutic approach to control this pathology...
  92. ncbi Estrogen to antiestrogen with a single methylene group resulting in an unusual steroidal selective estrogen receptor modulator
    Jing xin Zhang
    Department of Obstetrics and Gynecology, Yale University School of Medicine, New Haven, CT 06520, USA
    J Clin Endocrinol Metab 89:3527-35. 2004
    ..E11-2,2 with its short, nonpolar side-chain, lacks this critical structure, presenting the possibility that it might act through a unique mechanism...
  93. ncbi Differential effects of estrogen receptor antagonists on pituitary lactotroph proliferation and prolactin release
    Sanjay Kansra
    Department of Cell Biology, Neurobiology and Anatomy, University of Cincinnati College of Medicine, 3125 Eden Avenue, Cincinnati, OH 45267 0521, USA
    Mol Cell Endocrinol 239:27-36. 2005
    ..These data highlight the importance of studying the effects of anti-estrogens in multiple systems...
  94. ncbi Neoadjuvant percutaneous 4-hydroxytamoxifen decreases breast tumoral cell proliferation: a prospective controlled randomized study comparing three doses of 4-hydroxytamoxifen gel to oral tamoxifen
    Philippe Rouanet
    Centre Val d Aurelle, 34298 Montpellier, France
    J Clin Oncol 23:2980-7. 2005
    ..This randomized study was designed to analyze if 4-OHT gel, administered percutaneously on the breast skin, can inhibit the proliferation of malignant breast cells to the same extent as orally administered tamoxifen...
  95. ncbi [Effects of gestrinone on experimental endometriosis in rabbits]
    Y Giu
    Institute of Integrated Traditional Chinese and Western Medicine, Shenzhen Red Cross Hospital, Shenzhen
    Zhonghua Fu Chan Ke Za Zhi 30:735-7. 1995
    ..To study the therapeutic effects of gestrinone on experimental endometriosis in rabbits...
  96. ncbi Evaluation of tamoxifen and alpha-hydroxytamoxifen 32P-post-labelled DNA adducts by the development of a novel automated on-line solid-phase extraction HPLC method
    E A Martin
    MRC Toxicology Unit, Leicester, UK
    Carcinogenesis 19:1061-9. 1998
    ..Activation of 4-hydroxytamoxifen by the peroxidase/H2O2 system in vitro gives a more polar DNA adduct seen only at trace levels in liver DNA from tamoxifen-treated rats and mice...
  97. ncbi Estrogen-induced vasoprotection is estrogen receptor dependent: evidence from the balloon-injured rat carotid artery model
    S Bakir
    The Vascular Biology and Hypertension Program, Division of Cardiovascular Disease, Department of Medicine, University of Alabama at Birmingham, USA
    Circulation 101:2342-4. 2000
    ..This study used ICI 182,780, a nonselective ER antagonist, to test the hypothesis that the vasoprotective effect of E2 in the rat carotid injury model is ER mediated...
  98. ncbi Growth factor signalling and resistance to selective oestrogen receptor modulators and pure anti-oestrogens: the use of anti-growth factor therapies to treat or delay endocrine resistance in breast cancer
    R I Nicholson
    Tenovus Centre for Cancer Research, Welsh School of Pharmacy, Cardiff University, Cardiff, UK
    Endocr Relat Cancer 12:S29-36. 2005
    ....
  99. ncbi Downstream targets of growth factor and oestrogen signalling and endocrine resistance: the potential roles of c-Myc, cyclin D1 and cyclin E
    Alison J Butt
    Cancer Research Program, Garvan Institute of Medical Research, St Vincent s Hospital, Darlinghurst, New South Wales 2010, Australia
    Endocr Relat Cancer 12:S47-59. 2005
    ....
  100. ncbi Estrogen receptor (ER)alpha and ERbeta exhibit unique pharmacologic properties when coupled to activation of the mitogen-activated protein kinase pathway
    C B Wade
    Department of Pharmacology, University of Washington, School of Medicine, Seattle 98195, USA
    Endocrinology 142:2336-42. 2001
    ..These data show that these nuclear ERs are necessary for estrogen's effects at the membrane. This model system will be useful in identifying molecular interactions involved in the rapid effects mediated by the ERs...
  101. pmc Steroid-free medium discloses oestrogenic effects of the bisphosphonate clodronate on breast cancer cells
    F Journe
    Laboratory of Endocrinology and Bone Diseases, Institut Jules Bordet, Centre des Tumeurs de l Universite Libre de Bruxelles, Brussels, Belgium
    Br J Cancer 91:1703-10. 2004
    ..Moreover, our data suggest that ER is involved in these effects of clodronate on cancer cell growth...

Research Grants62

  1. Endocrine Targets for Prevention of Lung Cancer
    Robert M Bigsby; Fiscal Year: 2012
    ..These minimal studies will pave the way for testing receptor specific estrogen antagonists and additional PR-specific antagonists in prevention of tumor growth and progression in the lung.
  2. Brain aromatase availability in steroid users: PET studies with [11C]vorozole
    Thomas B Hildebrandt; Fiscal Year: 2013
    ..develop novel therapeutic targets to prevent and treat AAS addiction;specifically, aromatase inhibitors and estrogen antagonists may be used as pharmacological agents to treat AAS intoxication...
  3. Mechanisms of Action and Signaling by Steroid Hormone Antagonists
    Douglas V Faller; Fiscal Year: 2013
    ..b>Estrogen antagonists and androgen antagonists comprise the most widely-used endocrine therapies for breast cancer and prostate ..
  4. Dietary and serum phytoestrogens and women's health conditions in midlife
    Gail A Greendale; Fiscal Year: 2012
    ..Thus, phytoestrogens may be estrogen antagonists (cancer prevention) or relative agonists (fracture prevention)...
  5. LRH-1 Antagonism: Impact on Estrogen-dependent Breast Cancer
    Marcia I Dawson; Fiscal Year: 2013
    ..with an LRH-1 antagonist would locally reduce estrogen levels compared to adjuvant therapeutics such as estrogen antagonists and aromatase inhibitors and, thereby, attenuate the adverse systemic effects caused by whole-body estrogen ..
  6. Role of HIC1 in suppression of breast cancer growth and tamoxifen resistance
    Sheng Wang; Fiscal Year: 2010
    DESCRIPTION (provided by applicant): Estrogen antagonists comprise the most frequently used hormonal therapy for breast cancer...
  7. RADIOPHARMACEUTICALS FOR BREAST TUMOR IMAGING & THERAPY
    John Katzenellenbogen; Fiscal Year: 2006
    Most breast tumors contain estrogen receptors (ER) that regulate tumor cell growth and mediate the action of estrogen antagonists such as tamoxifen. Not all breast cancers, however, respond to hormone therapy...
  8. SXR--A TARGET FOR BREAST CANCER PREVENTION AND TREATMENT
    Bruce Blumberg; Fiscal Year: 2001
    ..In vitro, phytoestrogens, estrogen antagonists such as tamoxifen, anandamide and RXR agonists all share the ability to activate a heterodimer of the ..
  9. STUDY OF HORMONE-CONTROLLED SEX-ORGAN DIFFERENTIATION
    CHING TENG; Fiscal Year: 1980
    ..After the in vivo administration of estrogen, estrogen antagonists, or testosterone, its influence on the biochemical activities of the developing left Mullerian duct will be ..
  10. LIGAND/PROTEIN INTERACTIONS IN ESTROGEN RECEPTORS
    Richard Miksicek; Fiscal Year: 1993
    ..responsible for the antagonist activities of anti-estrogens, and underlying justification for these experiments is to assist the development of improved estrogen antagonists for use in the clinical therapy of estrogen-dependent tumors.
  11. REGULATION OF TESTICULAR GONOCYTE DEVELOPMENT
    Martine Culty; Fiscal Year: 2002
    ..This will be examined by studying 1) the effects of estrogen antagonists of PDGF-dependent cell proliferation, kinase activities and protein phosphorylation patterns and 2) the ..
  12. Rational Design of Novel Estrogen Receptor Antagonists
    MARTIN SAFO; Fiscal Year: 2007
    ..relationships of the new tetrahydroisoquinoline scaffold; (2) X-ray crystallographic analysis of estrogen antagonists: In collaboration with Dr. F...
  13. Environmental toxicants and reproductive health
    Mozhgan Savabieasfahani; Fiscal Year: 2003
    ..or triggered by the presence of endocrine disrupting compounds (EDCs) which act as estrogen mimics or estrogen antagonists. Such perturbations during critical stages of fetal development can lead to abnormal and irreversible ..
  14. ESTROGEN EFFECTS ON ANXIETY RELATED NEURAL SYSTEMS
    Margaret Altemus; Fiscal Year: 2004
    ..stria terminalis, and medial prefrontal cortex will be studied using local administration of estrogen and estrogen antagonists. The training portion of this proposal consists of basic neuroscience coursework and seminars as well as ..
  15. ANDROGEN SYNTHESIS INHIBITORS FOR PROSTATE CANCER
    Angela Brodie; Fiscal Year: 2008
    ..Determine effective doses, scheduling, and route of administration and b. Compare the effect of lead inhibitors and castration on apoptosis to identify the best compound. ..
  16. Pharmacogenetics of Sulfate Conjugation
    VIRGIL JORDAN; Fiscal Year: 2006
    ..These results will increase our understanding of the contribution of SULT1A1 pharmacogenetics to individual variation in response to estrogens and an important antiestrogen. ..
  17. EFFECT OF RALOXIFENE ON SALIVARY STEROIDS
    VIRGIL JORDAN; Fiscal Year: 2002
    ..Most importantly, completion of the study will validate an important new methodology to monitor the ovarian effects of any new chemopreventive that can be used in premenopausal women. ..
  18. ALKYL PCDFS--INHIBITION OF MAMMARY CANCER
    Stephen Safe; Fiscal Year: 2001
    ..Thus the proposed studies will define a new mechanism-based class of antiestrogens that can be used alone or in combination with tamoxifen for treatment of breast and endometrial cancer. ..
  19. Inhibition of Pancreatic Cancer by New PPARgamma Agonis*
    Stephen Safe; Fiscal Year: 2008
    ..PPAR? -active C-substituted DIMs that inhibit pancreatic cancer cell growth in vitro and in vivo, and these will serve as lead compounds for development of new drugs for clinical treatment of this devastating disease ..
  20. ESTROGEN INDUCED RESPONSES VIA ER/SPL COMPLEXES
    Stephen Safe; Fiscal Year: 2002
    ..These results will ultimately facilitate design of chemotherapeutic approaches which target specific genes. ..
  21. Mechanisms of Growth Factor-Estrogen Receptor Crosstalk
    Stephen Safe; Fiscal Year: 2006
    ..abstract_text> ..
  22. TOXICOLOGY OF ENVIRONMENT CONTAMINANTS
    Stephen Safe; Fiscal Year: 2007
    ..The proposed training program will continue to provide trainees with a challenging academic and research environment that will prepare them for future careers in academic, industry and government. ..
  23. Coactivation of Estrogen Receptor alpha/Sp1
    Stephen Safe; Fiscal Year: 2006
    ..abstract_text> ..
  24. Colon Cancer Inhibition by a Class of PPARgamma Agonists
    Stephen Safe; Fiscal Year: 2009
    ..The proposed studies will provide mechanistic insights on PPARy-dependent inhibition of colon cancer and identify compounds for future clinical studies. ..
  25. 2,3,7,8,--TCDD Effects on the Estrogenic Responses
    Stephen Safe; Fiscal Year: 2006
    ..The proposed Aims will address important mechanistic considerations on IDRE-independent inhibitory AhR-ERa crosstalk and pathways critical for inhibition of mammary tumor growth by SAhRMs. ..
  26. ROLE OF THE CELL CYCLE IN HYPERSENSITIVITY TO ESTRADIOL
    Richard Santen; Fiscal Year: 2008
    ..A clinical trial in women, which is designed to specifically demonstrate that high dose estrogen induces tumor regression through the mechanism of apoptosis will be conducted. ..
  27. DETERMINANTS OF TISSUE ESTRADIOL SENSITIVITY
    Richard Santen; Fiscal Year: 2009
    ..FTS, a novel mTOR inhibitor will be used in vitro to activate the stress kinase pathway and apoptosis. In vivo, FTS will be used to enhance estradiol induced apoptosis in nude mice. ..
  28. Determinants of Chemoprevention by SERMs
    MONICA MONTANO; Fiscal Year: 2008
    ..These mechanistic studies are critical for developing molecular-targeted approaches for chemoprevention, and the development of other models for testing promising new agents. [unreadable] [unreadable] [unreadable]..
  29. Estrogen regulation of uterine microRNAs: Novel factors in MMP-9 regulation
    Warren Nothnick; Fiscal Year: 2008
    ..Enhancing our understanding on the regulation of MMP-9 expression may lead to the establishment of novel approaches to counteract mis-expression of this protease and the diseases associated with it. [unreadable] [unreadable] [unreadable]..
  30. Antiestrogen-induced autophagy: a mechanism of cell survival in ER+ breast cancer
    Patricia V Schoenlein; Fiscal Year: 2010
    ....
  31. The Role of TIMP-1 in Uterine Physiology
    Warren Nothnick; Fiscal Year: 2005
    ..These studies will broaden our understanding on the role of TIMP-1 in uterine physiology and may help to develop new strategies to treat uterine disorders such as infertility, endometriosis and uterine cancer. ..
  32. ANTIESTROGEN REGULATION OF QUINONE REDUCTASE
    MONICA MONTANO; Fiscal Year: 2002
    ....
  33. SPECIFIC PROBES FOR THE ER HORMONE BINDING DOMAIN
    Robert Hanson; Fiscal Year: 2002
    ..The conclusions will aid in the design of better second generation ligands and the development of a better hypothesis for the interactions of the hormone-receptor-effector complex. ..
  34. Role of Prohibitin in Mediating Suppression of Breast Cancer Growth by Estrogen *
    Sheng Wang; Fiscal Year: 2004
    Background: Estrogen antagonists are widely employed in the treatment of breast cancer. They also comprise the most promising drugs for breast cancer chemo-prevention...
  35. ROLE OF VEGF AND NRP 1 IN ESTROGEN INDUCED ANGIOGENESIS
    Sushanta Banerjee; Fiscal Year: 2002
    ..Specific aim 4will address the question whether negative regulators like thrombospondin-1 that influence the action of VEGF164 during the development of estrogen induced tumor angiogenesis control the expression of NRP-1. ..
  36. A Genome-Wide Association Study of Non-Hodgkin Lymphoma
    Christine F Skibola; Fiscal Year: 2010
    ..The data generated from this study will provide a framework for further investigation within the NHL consortium, InterLymph. Results will later be combined with that from other InterLymph case-control studies in pooled analyses. ..
  37. Development of Hydrogel Spinal Disc Replacement
    Barbara Boyan; Fiscal Year: 2004
    ..abstract_text> ..
  38. Chemoprevention of Estrogen Receptor Negative Breast Cancer
    Michael Sporn; Fiscal Year: 2007
    ..These studies on apoptosis will be supplemented by measuring effects of chemopreventive agents on Myc gene expression. [unreadable] [unreadable] [unreadable]..
  39. Xenoestrogen effects on reproduction in male trout
    JAMES NAGLER; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  40. 2006 AUA/SBUR Summer Research Conference "Urothelial Biology & Bladder Cancer"
    Dale Bjorling; Fiscal Year: 2006
    ..unreadable] [unreadable]..
  41. Estrogen Influences on Fetal Adrenocorticotropin
    Charles Wood; Fiscal Year: 2006
    ..abstract_text> ..
  42. AIRWAY PARTICLE CLEARANCE--ROLE OF BRONCHIAL CIRCULATION
    Elizabeth Wagner; Fiscal Year: 2001
    ..Furthermore, the results will contribute to an understanding of the factors that both limit and enhance uptake and distribution of aerosols. ..
  43. Role of integrins and activin in granulosa cell growth
    Kutluk Oktay; Fiscal Year: 2007
    ..Cell proliferation and survival will be determined before and after transfection with the dominant-negative mutants. ..
  44. MECHANISMS OF ESTROGEN BIOSYNTHESIS IN ENDOMETRIOSIS
    Serdar Bulun; Fiscal Year: 2008
    ..Investigation of local feedback mechanisms responsible for interactions between estrogen biosynthesis, tissue growth, and inflammation will lead to the rational design of novel drug treatments. ..
  45. BONE FACTORS AND ENDOCHONDRAL OSSIFICATION
    Barbara Boyan; Fiscal Year: 2001
    ..It is suggested that these results will provide insight into the role these factors play in bone development and repair. ..
  46. LIGAND STRUCTURE AND ER MEDIATED TRANSACTIVATION
    JANICE SCHWARTZ; Fiscal Year: 2002
    ....
  47. N-3 fatty acid & binding protein MRG on mammary tumor
    YUENIAN SHI; Fiscal Year: 2006
    ..These studies will help to identify MRG as mediator for differentiation for mammary gland and for interaction with n-3 PUPA on inhibition of mammary tumorigenesis. ..
  48. ADJUVANT HORMONAL THERAPY IN VIETNAMESE BREAST CANCER
    Richard Love; Fiscal Year: 2005
    ..The investigators have a trial with a rich database and systems to develop further useful data on breast cancer relevant to all women. ..
  49. FUNCTIONS OF ESTROGEN RECEPTOR COACTIVATORS IN BREAST TI
    Meei Huey Jeng; Fiscal Year: 2003
    ..abstract_text> ..
  50. Phytochemicals and estrogen-enhanced cancers
    Karen Auborn; Fiscal Year: 2006
    ..We will use gene chip technology to look for induction or repression of other genes involved in apoptosis and cell cycle progression. ..
  51. ERBB RECEPTOR CONTROL OF BREAST CANCER GROWTH
    Anne Hamburger; Fiscal Year: 2006
    ..An understanding of the mechanisms by which Ebp1 inhibits cell growth and induces differentiation may contribute to the design of new molecular targets for cancer therapy. ..
  52. Peripheral NMDA receptors in visceral nociception
    JAMES MCROBERTS; Fiscal Year: 2009
    ..These studies are likely to contribute significantly to our understanding of the mechanisms underlying enhanced visceral pain associated with functional and inflammatory disorders of the Gl tract. ..
  53. SEX HORMONES AND BODY FLUID REGULATION
    NINA STACHENFELD; Fiscal Year: 2003
    ....
  54. Perinatal xenoestrogen exposure: epigenesis and neoplasia
    ANA SOTO; Fiscal Year: 2007
    ..This will also have a great impact on the way we study risk factors and conduct epidemiological studies; it may even influence public policy about breast cancer prevention. [unreadable] [unreadable] [unreadable] [unreadable]..
  55. Biomarker modulation/COX-2 inhibitor/Breast Cancer
    Banu Arun; Fiscal Year: 2003
    ..Ultimately, the development of non-hormonal chemoprevention agents, and identification of surrogate markers will allow us to plan large-scale, phase III chemoprevention studies with the endpoint of cancer incidence. ..
  56. Exploratory Program Grant for Frontier Medicine
    Karen Prestwood; Fiscal Year: 2004
    ..Theresa Smith) The effect of therapeutic touch on human fibroblast biology; and Project #4 (Dr. Susan Lutgendorf) Healing touch in advanced cervical cancer: immune effects and mechanisms. ..
  57. Influence of Sex and Gender on Musculoskeletal Health
    Barbara Boyan; Fiscal Year: 2004
    ..Worldwide current and future clinical trials will be discussed. Short papers on the workshop topics, future directions, and scientific updates will be published via Internet and summary papers in peer-reviewed journals. ..
  58. Nanoparticles for the Treatment of Lung Cancer
    Mingzhong Zheng; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  59. GILZ Controls TLR-Induced NF-kB Activity In Acute Asthma
    Bruce Zuraw; Fiscal Year: 2008
    ..We anticipate that this proposal will provide novel and clinically relevant data regarding the mechanisms of acute asthma exacerbations. ..
  60. PHASE I TRIAL OF A PEPTIDE VACCINE AGAINST EGFRVIII
    Bruce Montgomery; Fiscal Year: 2005
    ..To characterize effects of human anti-EGFRvIII antibodies on EGFRvIII signaling. 4. To determine the level of EGFR specific T cell response after immunization with EGFRvIII peptide. ..
  61. Treatment of Crohn's Disease with Growth Hormone
    Tamara Hannon; Fiscal Year: 2006
    ....