estrogen receptor modulators

Summary

Summary: Substances that possess antiestrogenic actions but can also produce estrogenic effects as well. They act as complete or partial agonist or as antagonist. They can be either steroidal or nonsteroidal in structure.

Top Publications

  1. ncbi Hormone replacement therapy with tibolone: effects on sexual functioning in postmenopausal women
    Christian Egarter
    Department of Obstetrics and Gynecology, University of Vienna, Vienna, Austria
    Acta Obstet Gynecol Scand 81:649-53. 2002
  2. ncbi Safety of alternative treatments for menopausal symptoms after breast cancer: a qualitative systematic review
    C Antoine
    Department of Obstetrics and Gynaecology, Free Universities of Brussels, CHU Saint Pierre, Brussels, Belgium
    Climacteric 10:23-6. 2007
  3. ncbi Effect of letrozole versus placebo on bone mineral density in women with primary breast cancer completing 5 or more years of adjuvant tamoxifen: a companion study to NCIC CTG MA.17
    Edith A Perez
    St Michael s Hospital, Toronto, Canada
    J Clin Oncol 24:3629-35. 2006
  4. ncbi Does tibolone exacerbate atherosclerosis?
    Thomas B Clarkson
    Eur Heart J 27:635-7. 2006
  5. ncbi Tamoxifen for the prevention of breast cancer: current status of the National Surgical Adjuvant Breast and Bowel Project P-1 study
    Bernard Fisher
    Operations Center, National Surgical Adjuvant Breast and Bowel Project, Pittsburgh, USA
    J Natl Cancer Inst 97:1652-62. 2005
  6. ncbi Diverse gene expression and DNA methylation profiles correlate with differential adaptation of breast cancer cells to the antiestrogens tamoxifen and fulvestrant
    Meiyun Fan
    Medical Sciences, Indiana University School of Medicine, Bloomington, Indiana 47405, USA
    Cancer Res 66:11954-66. 2006
  7. ncbi Microsomal antiestrogen-binding site ligands induce growth control and differentiation of human breast cancer cells through the modulation of cholesterol metabolism
    Bruno Payre
    INSERM, U 563, Section métabolisme, Oncogenése et Différenciation Cellulaire, Centre de Physiopathologie de Toulouse Purpan, Institut Claudius Regaud, 24 rue du Pont Saint Pierre, F 31052 Toulouse Cedex, France
    Mol Cancer Ther 7:3707-18. 2008
  8. ncbi Enhanced epidermal growth factor receptor signaling in MCF7 breast cancer cells after long-term culture in the presence of the pure antiestrogen ICI 182,780 (Faslodex)
    R A McClelland
    Tenovus Cancer Research Center, Welsh School of Pharmacy, Cardiff University, Cathays Park, Cardiff, United Kingdom CF10 3XF
    Endocrinology 142:2776-88. 2001
  9. pmc The molecular mechanisms underlying the pharmacological actions of ER modulators: implications for new drug discovery in breast cancer
    Donald P McDonnell
    Department of Pharmacology and Cancer Biology, Duke University Medical Center, Durham, NC 27710, USA
    Curr Opin Pharmacol 10:620-8. 2010
  10. ncbi Estrogen receptor beta increases the efficacy of antiestrogens by effects on apoptosis and cell cycling in breast cancer cells
    Leslie Hodges-Gallagher
    Department of Medicine, University of California, San Francisco, CA 94143, USA
    Breast Cancer Res Treat 109:241-50. 2008

Detail Information

Publications286 found, 100 shown here

  1. ncbi Hormone replacement therapy with tibolone: effects on sexual functioning in postmenopausal women
    Christian Egarter
    Department of Obstetrics and Gynecology, University of Vienna, Vienna, Austria
    Acta Obstet Gynecol Scand 81:649-53. 2002
    ..Because hormonal changes in postmenopausal women may be accompanied by sexual problems and a worsening of various aspects of libido, the aim of this study was to assess the effect of tibolone (Liviel(R)) on sexual life...
  2. ncbi Safety of alternative treatments for menopausal symptoms after breast cancer: a qualitative systematic review
    C Antoine
    Department of Obstetrics and Gynaecology, Free Universities of Brussels, CHU Saint Pierre, Brussels, Belgium
    Climacteric 10:23-6. 2007
    ..This qualitative review analyzes systematically the safety of drugs used to alleviate menopausal symptoms, other than hormone replacement therapy, in breast cancer patients...
  3. ncbi Effect of letrozole versus placebo on bone mineral density in women with primary breast cancer completing 5 or more years of adjuvant tamoxifen: a companion study to NCIC CTG MA.17
    Edith A Perez
    St Michael s Hospital, Toronto, Canada
    J Clin Oncol 24:3629-35. 2006
    ..17B evaluated bone turnover markers and bone mineral density (BMD) in postmenopausal women randomly assigned to MA.17, a placebo-controlled trial of letrozole after standard adjuvant tamoxifen...
  4. ncbi Does tibolone exacerbate atherosclerosis?
    Thomas B Clarkson
    Eur Heart J 27:635-7. 2006
  5. ncbi Tamoxifen for the prevention of breast cancer: current status of the National Surgical Adjuvant Breast and Bowel Project P-1 study
    Bernard Fisher
    Operations Center, National Surgical Adjuvant Breast and Bowel Project, Pittsburgh, USA
    J Natl Cancer Inst 97:1652-62. 2005
    ..Side effects of varying clinical significance were observed. The trial was unblinded because of the positive results, and follow-up continued. This report updates our initial findings...
  6. ncbi Diverse gene expression and DNA methylation profiles correlate with differential adaptation of breast cancer cells to the antiestrogens tamoxifen and fulvestrant
    Meiyun Fan
    Medical Sciences, Indiana University School of Medicine, Bloomington, Indiana 47405, USA
    Cancer Res 66:11954-66. 2006
    ..Such knowledge of resistance-associated mechanisms could allow for identification of therapy targets and strategies for resensitization to these well-established antihormonal agents...
  7. ncbi Microsomal antiestrogen-binding site ligands induce growth control and differentiation of human breast cancer cells through the modulation of cholesterol metabolism
    Bruno Payre
    INSERM, U 563, Section métabolisme, Oncogenése et Différenciation Cellulaire, Centre de Physiopathologie de Toulouse Purpan, Institut Claudius Regaud, 24 rue du Pont Saint Pierre, F 31052 Toulouse Cedex, France
    Mol Cancer Ther 7:3707-18. 2008
    ..Together, these data show that AEBS ligands exert an antiproliferative effect on mammary cancer cells by inducing cell differentiation and growth arrest and highlight the importance of cholesterol metabolism in these effects...
  8. ncbi Enhanced epidermal growth factor receptor signaling in MCF7 breast cancer cells after long-term culture in the presence of the pure antiestrogen ICI 182,780 (Faslodex)
    R A McClelland
    Tenovus Cancer Research Center, Welsh School of Pharmacy, Cardiff University, Cathays Park, Cardiff, United Kingdom CF10 3XF
    Endocrinology 142:2776-88. 2001
    ....
  9. pmc The molecular mechanisms underlying the pharmacological actions of ER modulators: implications for new drug discovery in breast cancer
    Donald P McDonnell
    Department of Pharmacology and Cancer Biology, Duke University Medical Center, Durham, NC 27710, USA
    Curr Opin Pharmacol 10:620-8. 2010
    ..of this knowledge has come from a detailed dissection of the mechanism(s) of action of the Selective Estrogen Receptor Modulators (SERMs) tamoxifen and raloxifene, so called for their ability to function as ER agonists or antagonists ..
  10. ncbi Estrogen receptor beta increases the efficacy of antiestrogens by effects on apoptosis and cell cycling in breast cancer cells
    Leslie Hodges-Gallagher
    Department of Medicine, University of California, San Francisco, CA 94143, USA
    Breast Cancer Res Treat 109:241-50. 2008
    ....
  11. ncbi Anastrozole versus tamoxifen as first-line therapy for advanced breast cancer in 668 postmenopausal women: results of the Tamoxifen or Arimidex Randomized Group Efficacy and Tolerability study
    J Bonneterre
    Centre Oscar Lambret, Lille, France
    J Clin Oncol 18:3748-57. 2000
    ..To compare the efficacy and tolerability of anastrozole (Arimidex; AstraZeneca, Wilmington, DE, and Macclesfield, United Kingdom) with that of tamoxifen as first-line therapy for advanced breast cancer (ABC) in postmenopausal women...
  12. ncbi Endocrine therapy--current benefits and limitations
    Robert I Nicholson
    Tenovus Centre for Cancer Research, Welsh School of Pharmacy, Cardiff University, Cardiff, UK
    Breast Cancer Res Treat 93:S3-10. 2005
    ....
  13. pmc A variant of estrogen receptor-{alpha}, hER-{alpha}36: transduction of estrogen- and antiestrogen-dependent membrane-initiated mitogenic signaling
    Zhaoyi Wang
    Cancer Center, Creighton University, 2500 California Plaza, Omaha, NE 68178, USA
    Proc Natl Acad Sci U S A 103:9063-8. 2006
    ....
  14. 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...
  15. ncbi Importance of cholesterol and oxysterols metabolism in the pharmacology of tamoxifen and other AEBS ligands
    Philippe de Medina
    Cancer Research Center of Toulouse, UMR 1037 Inserm University of Toulouse III, Toulouse, France
    Chem Phys Lipids 164:432-7. 2011
    ..that binds different structural classes of ligands, including selective estrogen receptor modulators, several sigma receptor ligands, poly-unsaturated fatty acids and ring B oxysterols...
  16. 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
    ....
  17. pmc Co-inhibition of BCL-W and BCL2 restores antiestrogen sensitivity through BECN1 and promotes an autophagy-associated necrosis
    Anatasha C Crawford
    Lombardi Comprehensive Cancer Center and Department of Oncology, School of Medicine, Georgetown University, Washington, District of Columbia, United States of America
    PLoS ONE 5:e8604. 2010
    ..BCL-W, BCL2, and BECN1 integrate important functions in determining antiestrogen responsiveness, and the presence of functional autophagy may influence the balance between apoptosis and necrosis...
  18. ncbi c-Myc suppresses p21WAF1/CIP1 expression during estrogen signaling and antiestrogen resistance in human breast cancer cells
    Shibani Mukherjee
    Department of Microbiology and Molecular Genetics, Michigan State University, East Lansing, Michigan 48824, USA
    J Biol Chem 280:17617-25. 2005
    ..They further suggest that aberrant c-Myc expression, which is frequently observed in human breast cancers, can contribute to antiestrogen resistance by altering p21(WAF1/CIP1) regulation...
  19. ncbi A randomized trial of low-dose tamoxifen on breast cancer proliferation and blood estrogenic biomarkers
    Andrea Decensi
    Division of Chemoprevention, European Institute of Oncology, and University of Milan School of Medicine, Milan, Italy
    J Natl Cancer Inst 95:779-90. 2003
    ....
  20. pmc A model of acquired autoresistance to a potent ErbB2 tyrosine kinase inhibitor and a therapeutic strategy to prevent its onset in breast cancer
    Wenle Xia
    Department of Oncology Biology, GlaxoSmithKline, Research Triangle Park, NC 27709, USA
    Proc Natl Acad Sci U S A 103:7795-800. 2006
    ..Establishing clinically relevant models of acquired resistance to ErbB2 kinase inhibitors will enhance therapeutic strategies to improve clinical outcomes for patients with ErbB2-overexpressing breast cancers...
  21. 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
    ....
  22. ncbi The tamoxifen metabolite, endoxifen, is a potent antiestrogen that targets estrogen receptor alpha for degradation in breast cancer cells
    Xianglin Wu
    Department of Biochemistry and Molecular Biology, Mayo Clinic, Rochester, Minnesota 55905, USA
    Cancer Res 69:1722-7. 2009
    ..These results support the theory that endoxifen is the primary metabolite responsible for the overall effectiveness of tamoxifen in the treatment of ER-positive breast cancer...
  23. ncbi Identification and characterization of a negative regulatory element within the epidermal growth factor receptor gene first intron in hormone-dependent breast cancer cells
    Melissa A Wilson
    Department of Biochemistry and Molecular Biology, Lombardi Cancer Center, Georgetown University, Washington, DC 20007, USA
    J Cell Biochem 85:601-14. 2002
    ....
  24. ncbi Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 1. Receptor interactions
    V Craig Jordan
    Robert H Lurie Comprehensive Cancer Center, The Feinberg School of Medicine of Northwestern University, 303 East Chicago Avenue, MS N505, Chicago, Illinois 60611, USA
    J Med Chem 46:883-908. 2003
  25. ncbi Role of the estrogen receptor coactivator AIB1 (SRC-3) and HER-2/neu in tamoxifen resistance in breast cancer
    C Kent Osborne
    Department of Medicine, Baylor College of Medicine, Houston, TX 77030, USA
    J Natl Cancer Inst 95:353-61. 2003
    ....
  26. ncbi The ligand binding profiles of estrogen receptors alpha and beta are species dependent
    Heather A Harris
    Women s Health Research Institute, Wyeth Ayerst Research, 500 Arcola Road, Radnor, PA 19087, USA
    Steroids 67:379-84. 2002
    Estrogens and selective estrogen receptor modulators are used for the treatment and prevention of conditions resulting from menopause...
  27. ncbi CYP2D6 genotype, antidepressant use, and tamoxifen metabolism during adjuvant breast cancer treatment
    Yan Jin
    Division of Clinical Pharmacology, Department of Medicine, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    J Natl Cancer Inst 97:30-9. 2005
    ....
  28. ncbi Engineered chimeric enzymes as tools for drug discovery: generating reliable bacterial screens for the detection, discovery, and assessment of estrogen receptor modulators
    Georgios Skretas
    Department of Chemical Engineering, Princeton University, Princeton, New Jersey 08544, USA
    J Am Chem Soc 129:8443-57. 2007
    ..by screening a small compound library, which led to the identification of two structurally novel estrogen receptor modulators and the accurate prediction of their agonistic/antagonistic biocharacter in human cells...
  29. ncbi Estren is a selective estrogen receptor modulator with transcriptional activity
    Sofia Moverare
    Department of Internal Medicine, Division of Endocrinology, Grona Straket 8, 413 45 Gothenburg, Sweden
    Mol Pharmacol 64:1428-33. 2003
    ..Thus, estren has the capacity to exert genomic effects via both ERalpha and ERbeta. We conclude, in contrast to what was previously reported by others, that estren is a SERM with transcriptional activity...
  30. ncbi An estrogen-responsive element-targeted histone deacetylase enzyme has an antiestrogen activity that differs from that of hydroxytamoxifen
    Ediz Demirpence
    INSERM U439, 34090 Montpellier, France
    Cancer Res 62:6519-28. 2002
    ..It nevertheless accelerated the OHT-driven phenomenon. The antiestrogen effect of OHT thus differs from that of an ERE-targeted HDAC1 activity that might participate in irreversible silencing but is not sufficient to trigger it...
  31. 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...
  32. ncbi Phase II, randomized, double-blind study of two dose levels of arzoxifene in patients with locally advanced or metastatic breast cancer
    Aman Buzdar
    M D Anderson Cancer Center and US Oncology Research, Houston, and Baylor Sammons Cancer Center and Texas Oncology, Dallas, TX 77030, USA
    J Clin Oncol 21:1007-14. 2003
    ....
  33. ncbi Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands
    Johanne Renaud
    Novartis Pharma Research, WKL 136 3 25, CH 4002 Basel, Switzerland
    J Med Chem 46:2945-57. 2003
    As part of a program aimed at the development of selective estrogen receptor modulators (SERMs), tetrahydroisoquinoline derivative 27 was discovered by high throughput screening...
  34. ncbi mRNA expression of the type I growth factor receptors in the human breast cancer cells MCF-7: regulation by estradiol and tamoxifen
    Francoise Revillion
    Laboratoire d Oncologie Moléculaire Humaine, Centre Oscar Lambret, 3 Rue Frederic Combemale, BP 309, 59020 Lille, France
    Anticancer Res 23:1455-60. 2003
    ..In the present paper, we simultaneously quantified, for the first time, the mRNA expression of these four receptors in response to estradiol and 4-hydroxy-tamoxifen in the prototypical ER-positive human breast cancer cell line MCF-7...
  35. ncbi The molecular pharmacology of estrogen receptor modulators: implications for the treatment of breast cancer
    Donald P McDonnell
    Department of Pharmacology and Cancer Biology, Duke University Medical Center, Durham, North Carolina 27710, USA
    Clin Cancer Res 11:871s-7s. 2005
    ....
  36. ncbi Estrogen and antiestrogen regulation of cell cycle progression in breast cancer cells
    S F Doisneau-Sixou
    Cancer Research Program, Garvan Institute of Medical Research, St Vincent s Hospital, 384 Victoria Street, Darlinghurst, Sydney, NSW 2010, Australia
    Endocr Relat Cancer 10:179-86. 2003
    ....
  37. ncbi Bortezomib blocks the catabolic process of autophagy via a cathepsin-dependent mechanism, affects endoplasmic reticulum stress and induces caspase-dependent cell death in antiestrogen-sensitive and resistant ER+ breast cancer cells
    Sudharsan Periyasamy-Thandavan
    Department of Cellular Biology and Anatomy, Medical College of Georgia, Augusta, GA, USA
    Autophagy 6:19-35. 2010
    ..These findings indicate that combining a proteasome inhibitor like bortezomib with antiestrogen therapy may have therapeutic advantage in the management of early-stage breast cancer...
  38. ncbi Pure antiestrogen-induced G1-arrest in myeloma cells results from the reduced kinase activity of cyclin D3/CDK6 complexes whereas apoptosis is mediated by endoplasmic reticulum-dependent caspases
    Juliette Gauduchon
    Biologie Moléculaire et Cellulaire de la Signalisation, EA 3919, IFR 146, Universite de Caen, Caen, Cedex, France
    Int J Cancer 122:2130-41. 2008
    ..Therefore, RU mediates the inhibition of survival, the activation of apoptosis and finally potentiates anticancer drug. Those combinatory effects provide a basis for the potential use of pure AEs in MM treatment...
  39. pmc Advances in breast cancer treatment and prevention: preclinical studies on aromatase inhibitors and new selective estrogen receptor modulators (SERMs)
    Rachel Schiff
    The Breast Center, Department of Medicine, Baylor College of Medicine, Houston, TX, USA
    Breast Cancer Res 5:228-31. 2003
    ..Two recent studies in preclinical model systems that evaluate mechanisms of action of these new drugs and suggestions about their optimal clinical use are discussed...
  40. pmc Activation of ErbB3, EGFR and Erk is essential for growth of human breast cancer cell lines with acquired resistance to fulvestrant
    Thomas Frogne
    Department of Tumor Endocrinology, Institute of Cancer Biology, Danish Cancer Society, Copenhagen, Denmark
    Breast Cancer Res Treat 114:263-75. 2009
    ..Our data support that a concerted action against EGFR, ErbB2 and ErbB3 may be required to obtain complete growth suppression of fulvestrant resistant cells...
  41. ncbi Molecular mechanism of action at estrogen receptor alpha of a new clinically relevant antiestrogen (GW7604) related to tamoxifen
    D Bentrem
    Department of Surgery, The Robert H Lurie Comprehensive Cancer Center, Northwestern University Medical School, Chicago, Illinois 60611, USA
    Endocrinology 142:838-46. 2001
    ..This charge is restored in the D351Y ER, thus converting GW7604 from an antiestrogen to an estrogen-like molecule...
  42. ncbi p27(Kip1) induces quiescence and growth factor insensitivity in tamoxifen-treated breast cancer cells
    Jason S Carroll
    Cancer Research Program, Garvan Institute of Medical Research, 384 Victoria Street, Darlinghurst, New South Wales 2010, Australia
    Cancer Res 63:4322-6. 2003
    ..These data suggest that agents that up-regulate p27(Kip1) or inhibit growth factor signaling via the extracellular signal-regulated kinases should be tested as therapeutic strategies in tamoxifen-resistant breast cancer...
  43. ncbi Fulvestrant: a review of its development, pre-clinical and clinical data
    A M Wardley
    Department of Medical Oncology, Christie Hospital, Withington, Manchester, UK
    Int J Clin Pract 56:305-9. 2002
    ..Its place will be better defined by ongoing clinical trials...
  44. ncbi High-dose estrogen and clinical selective estrogen receptor modulators induce growth arrest, p21, and p53 in primate ovarian surface epithelial cells
    Jay W Wright
    Division of Reproductive Sciences, Oregon Regional Primate Research Center, Beaverton, Oregon 97006, USA
    J Clin Endocrinol Metab 90:3688-95. 2005
    ....
  45. ncbi Selective estrogen receptor modulators: tissue actions and potential for CNS protection
    M T Littleton-Kearney
    Johns Hopkins Medical Institutions, Baltimore, MD 21287, USA
    CNS Drug Rev 8:309-30. 2002
    ..Recently, a variety of selective estrogen receptor modulators (SERMs) have been developed to retain the favorable and minimize the adverse side effects of estrogens...
  46. ncbi 2,5-Diphenylfuran-based pure antiestrogens with selectivity for the estrogen receptor alpha
    Jochen Zimmermann
    Institut fur Pharmazie, Universitat Regensburg, D 93040 Regensburg, Germany
    J Steroid Biochem Mol Biol 94:57-66. 2005
    ..It inhibited the growth of wild-type MCF-7 cells with an IC(50) value of 22 nM. The data show that the 2,5-diphenylfuran system is appropriate for the development of pure antiestrogens with preference for ERalpha...
  47. ncbi Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 2. Clinical considerations and new agents
    V Craig Jordan
    Robert H Lurie Comprehensive Cancer Center, The Feinberg School of Medicine of Northwestern University, 303 East Chicago Avenue, MS N505, Chicago, Illinois 60611, USA
    J Med Chem 46:1081-111. 2003
  48. ncbi In vivo characterization of estrogen receptor modulators with reduced genomic versus nongenomic activity in vitro
    Christiane Otto
    Research Laboratories, Bayer Schering Pharma AG, D 13353 Berlin, Germany
    J Steroid Biochem Mol Biol 111:95-100. 2008
    ..We conclude that pathway-selective ER ligands may represent an interesting option for hormone therapy...
  49. ncbi Molecular structural characteristics of estrogen receptor modulators as determinants of estrogen receptor selectivity
    S Agatonovic-Kustrin
    School of Pharmacy and Molecular Sciences, James Cook University, Townsville, Australia
    Mini Rev Med Chem 8:943-51. 2008
    ..In addition, strategies likely to result in the development of a pharmacophore model that account for the differences in estrogenic effects between different ligands will be discussed...
  50. ncbi Antiestrogen resistance in breast cancer and the role of estrogen receptor signaling
    Robert Clarke
    Department of Oncology and Vincent T Lombardi Cancer Center, Georgetown University School of Medicine, 3970 Reservoir Road NW, Washington, DC 20057, USA
    Oncogene 22:7316-39. 2003
    ..The network also may involve signaling through ras and MAPK, implicating crosstalk with growth factors and cytokines. Ultimately, signaling affects the expression/function of the proliferation and/or apoptotic machineries...
  51. 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...
  52. pmc A subfamily of RNA-binding DEAD-box proteins acts as an estrogen receptor alpha coactivator through the N-terminal activation domain (AF-1) with an RNA coactivator, SRA
    M Watanabe
    Institute of Molecular and Cellular Biosciences, University of Tokyo, Yayoi, Bunkyo ku, Tokyo 113 0033, Japan
    EMBO J 20:1341-52. 2001
    ..These findings indicate that p72/p68 acts as an ER subtype-selective coactivator through ER alpha AF-1 by associating with the coactivator complex to bind its AF-2 through direct binding with SRA and the SRC-1/TIF2 family proteins...
  53. ncbi A role for macroautophagy in protection against 4-hydroxytamoxifen-induced cell death and the development of antiestrogen resistance
    Julia S Samaddar
    Department of Cellular Biology and Anatomy, Medical College of Georgia, Augusta, GA 30912, USA
    Mol Cancer Ther 7:2977-87. 2008
    ..We propose that targeting autophagosome function will improve the efficacy of hormonal treatment of ER+ breast cancer...
  54. ncbi Mifepristone induces growth arrest, caspase activation, and apoptosis of estrogen receptor-expressing, antiestrogen-resistant breast cancer cells
    Virgil T Gaddy
    Department of Cellular Biology and Anatomy, Medical College of Georgia, Augusta, Georgia 30912, USA
    Clin Cancer Res 10:5215-25. 2004
    ..In this study, we sought to determine whether antiprogestin treatment, used as a monotherapy or in combination with antiestrogen therapy, induced growth arrest and active cell death in antiestrogen-resistant breast cancer cells...
  55. ncbi The nuclear factor kappa B inhibitor parthenolide restores ICI 182,780 (Faslodex; fulvestrant)-induced apoptosis in antiestrogen-resistant breast cancer cells
    Rebecca B Riggins
    Lombardi Comprehensive Cancer Center, Georgetown University School of Medicine, Room W405A Research Building, 3970 Reservoir Road Northwest, Washington, DC 20057, USA
    Mol Cancer Ther 4:33-41. 2005
    ..Because parthenolide has shown safety in Phase I clinical trials, these findings have direct clinical relevance and provide support for the design of clinical studies combining antiestrogens and parthenolide in ER-positive breast cancer...
  56. ncbi Estrogen suppression of EGFR expression in breast cancer cells: a possible mechanism to modulate growth
    R I Yarden
    Department of Oncology, Georgetown University, Washington, DC 20007, USA
    J Cell Biochem Suppl . 2001
    ..J. Cell. Biochem. Suppl. 36: 232-246, 2001...
  57. ncbi Tamoxifen-bound estrogen receptor (ER) strongly interacts with the nuclear matrix protein HET/SAF-B, a novel inhibitor of ER-mediated transactivation
    S Oesterreich
    Department of Medicine, University of Texas Health Science Center, San Antonio 78284, USA
    Mol Endocrinol 14:369-81. 2000
    ..Furthermore, our data showing that HET/SAF-B binds to ER particularly strongly in the presence of tamoxifen suggests that it may be important for the antagonist effect of tamoxifen...
  58. ncbi Microtubule-associated protein-tau is a bifunctional predictor of endocrine sensitivity and chemotherapy resistance in estrogen receptor-positive breast cancer
    Fabrice Andre
    Breast Cancer Unit and Translational Research Unit, UPRES03535, Institut Gustave Roussy, Villejuif, France
    Clin Cancer Res 13:2061-7. 2007
    ..A molecular marker may be prognostic of outcome or predictive of response to therapy, or a combination of both...
  59. ncbi Characterization of BCAR4, a novel oncogene causing endocrine resistance in human breast cancer cells
    Marcia Godinho
    Department of Pathology, Josephine Nefkens Institute, Erasmus MC, University Medical Center, Rotterdam, The Netherlands
    J Cell Physiol 226:1741-9. 2011
    ..Due to its restricted expression, BCAR4 may be a good target for treating antiestrogen-resistant breast cancer...
  60. ncbi Clinical use of selective estrogen receptor modulators and down regulators with the main focus on breast cancer
    C K Baumann
    Clinic and Policlinic for Medical Oncology, University Hospital, Bern, Switzerland
    Minerva Ginecol 61:517-39. 2009
    Selective estrogen receptor modulators (SERMs) and selective estrogen down regulators (SERDs) act as estrogen receptor (ER) agonists or antagonist depending on the targeted tissue and the specific configuration of the used SERM or SERD...
  61. pmc Antiestrogen-resistant subclones of MCF-7 human breast cancer cells are derived from a common monoclonal drug-resistant progenitor
    Kathryn R Coser
    Center for Cancer Research, Massachusetts General Hospital Cancer Center and Harvard Medical School, Charlestown, MA 02129, USA
    Proc Natl Acad Sci U S A 106:14536-41. 2009
    ..Our results suggest the importance of clonal selection in endocrine therapy resistance of breast cancer...
  62. ncbi Fulvestrant, an estrogen receptor downregulator, reduces cell turnover index more effectively than tamoxifen
    Nigel J Bundred
    Department of Surgery, South Manchester University Hospital Education and Research Centre, UK
    Anticancer Res 22:2317-9. 2002
    ..This study was performed to determine whether drug action on breast tumours could also be analysed using a cell turnover index (CTI), a composite measurement of both proliferation and apoptosis...
  63. ncbi Antiestrogen ICI 182,780 decreases proliferation of insulin-like growth factor I (IGF-I)-treated MCF-7 cells without inhibiting IGF-I signaling
    Hemant Varma
    Department of Biochemistry and Molecular Biology, Michigan State University, East Lansing, Michigan 48824, USA
    Cancer Res 62:3985-91. 2002
    ....
  64. ncbi Selective estrogen receptor modulators for the chemoprevention of prostate cancer
    M S Steiner
    Department of Urology, University of Tennessee, Memphis, Tennessee 38104, USA
    Urology 57:68-72. 2001
    ..Selective estrogen receptor modulators (SERMs) have shown the ability to prevent (GTx-006 [acapodene]) and treat (GTx-006 and arzoxifene) ..
  65. pmc A phase I trial to assess the pharmacology of the new oestrogen receptor antagonist fulvestrant on the endometrium in healthy postmenopausal volunteers
    S Addo
    LCG Bioscience, Bourn Hall Clinic, Bourn, Cambridge, UK
    Br J Cancer 87:1354-9. 2002
    ....
  66. pmc Estrogen receptor beta inhibits 17beta-estradiol-stimulated proliferation of the breast cancer cell line T47D
    Anders Strom
    Department of Biosciences, Karolinska Institutet, Novum, S 14157 Huddinge, Sweden
    Proc Natl Acad Sci U S A 101:1566-71. 2004
    ..These findings suggest a possible role for ERbeta in breast cancer and imply that ERbeta-specific ligands may reduce proliferation of ER-positive breast cancer cells through actions on the G(1) phase cell-cycle machinery...
  67. pmc Functional ablation of pRb activates Cdk2 and causes antiestrogen resistance in human breast cancer cells
    Hemant Varma
    Department of Biochemistry and Molecular Biology, Michigan State University, East Lansing, Michigan, United States of America
    PLoS ONE 2:e1256. 2007
    ....
  68. ncbi A comparative study of genome-wide SNP, CGH microarray and protein expression analysis to explore genotypic and phenotypic mechanisms of acquired antiestrogen resistance in breast cancer
    Neil Johnson
    Northern Institute for Cancer Research, Paul O Gorman Building, Newcastle University, Framlington Place, Newcastle upon Tyne, NE2 4HH, UK
    Breast Cancer Res Treat 111:55-63. 2008
    ..However, the antiestrogen resistant phenotype was likely to be due to changes in gene expression and protein degradation rather than in altered gene copy number...
  69. ncbi Modulation of epidermal growth factor receptor in endocrine-resistant, estrogen-receptor-positive breast cancer
    R I Nicholson
    Tenovus Centre for Cancer Research, Welsh School of Pharmacy, Cardiff, Wales
    Ann N Y Acad Sci 963:104-15. 2002
    ..The considerable potential of the epidermal growth factor receptor-selective tyrosine kinase inhibitor Iressa (ZD 1839) to efficiently treat, and perhaps even prevent, endocrine-resistant breast cancer is highlighted...
  70. ncbi Postmenopausal women who progress on fulvestrant ('Faslodex') remain sensitive to further endocrine therapy
    I Vergote
    Department of Gynecologic Oncology, University Hospitals, Leuven, Belgium
    Breast Cancer Res Treat 79:207-11. 2003
    ....
  71. ncbi A randomized, placebo-controlled, crossover study of tibolone (Livial) on menopause symptoms, psychological well-being, and dyadic relationship of postmenopausal Chinese women and their spouses
    Po M Lam
    Department of Obstetrics and Gynecology, Prince of Wales Hospital, Shatin, Hong Kong SAR, China
    Menopause 11:416-22. 2004
    ..To investigate the effects of 6-month treatment of tibolone on menopause symptoms, psychological well-being, and the dyadic relationship of postmenopausal Chinese women and their spouses...
  72. ncbi Coronary heart disease mortality after 5 years of adjuvant tamoxifen therapy: results from a randomized trial
    Bo Nordenskjold
    Department of Oncology, Linkoping University Hospital, Linkoping, Sweden
    J Natl Cancer Inst 97:1609-10. 2005
    ..5% of those in the 2-year group had died from coronary heart disease. No statistically significant increases in mortality from other heart diseases, cerebrovascular diseases, or other vascular diseases were observed...
  73. ncbi Effects of tibolone and raloxifene on health-related quality of life and sexual function
    E A Nijland
    Department of Obstetrics and Gynecology, Academisch Ziekenhuis Groningen, 9713 GZ Groningen, The Netherlands
    Maturitas 58:164-73. 2007
    ..Study to compare the effects of tibolone and raloxifene on health-related quality of life, sexuality and vaginal atrophy...
  74. ncbi The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer
    Isabel Chu
    The Braman Breast Cancer Institute, UM Sylvester Comprehensive Cancer Center, University of Miami School of Medicine, Miami, FL 33136, USA
    Cancer Res 65:18-25. 2005
    ..These data provide strong preclinical data to support clinical trials of ErbB1/ErbB2 inhibitors in combination with tamoxifen in the treatment of human breast cancer...
  75. ncbi A pharmacophore-based evolutionary approach for screening selective estrogen receptor modulators
    Jinn Moon Yang
    Department of Biological Science and Technology, and Institute of Bioinformatics, National Chiao Tung University, Hsinchu, Taiwan
    Proteins 59:205-20. 2005
    ..These results suggest that GEMDOCK constitutes a robust tool for virtual database screening...
  76. pmc Novel image analysis approach for quantifying expression of nuclear proteins assessed by immunohistochemistry: application to measurement of oestrogen and progesterone receptor levels in breast cancer
    Elton Rexhepaj
    UCD School of Biomolecular and Biomedical Science, UCD Conway Institute, University College Dublin, Belfield, Ireland
    Breast Cancer Res 10:R89. 2008
    ..In the present article we describe the development of a novel approach for automatically quantifying oestrogen receptor (ER) and progesterone receptor (PR) protein expression assessed by IHC in primary breast cancer...
  77. ncbi Significant differential effects of hormone therapy or tibolone on markers of cardiovascular disease in postmenopausal women: a randomized, double-blind, placebo-controlled, crossover study
    Kwang Kon Koh
    Division of Cardiology, Gil Heart Center, Gachon Medical School, Namdong gu, Incheon, Korea
    Arterioscler Thromb Vasc Biol 23:1889-94. 2003
    ..The objective was to compare the effects of tibolone and hormone therapy (HT) on lipid profile, vasodilation, and factors associated with inflammation and hemostasis...
  78. pmc Down-regulation of p21WAF1/CIP1 or p27Kip1 abrogates antiestrogen-mediated cell cycle arrest in human breast cancer cells
    S Cariou
    Division of Cancer Biology Research, Sunnybrook and Women s College Health Science Centre, 2075 Bayview Avenue, Toronto, ON, Canada M4N 3M5
    Proc Natl Acad Sci U S A 97:9042-6. 2000
    ..These data demonstrate that depletion of either p21 or p27 can mimic estrogen-stimulated cell cycle activation and indicate that both of these KIPs are critical mediators of the therapeutic effects of antiestrogens in breast cancer...
  79. ncbi Expression of calcitonin gene-related peptide receptor components, calcitonin receptor-like receptor and receptor activity modifying protein 1, in the rat placenta during pregnancy and their cellular localization
    Y L Dong
    Department of Obstetrics and Gynecology, 301 University Blvd, Medical Research Building, Rm 11 138, The University of Texas Medical Branch, Galveston, TX 77555 1062, USA
    Mol Hum Reprod 9:481-90. 2003
    ..Elevated placental CRLR and RAMP(1) may be involved in CGRP-related increases in blood flow and therefore fetal growth and decreases at term labour may help minimize the blood loss...
  80. ncbi Tibolone and transdermal E2/NETA for the treatment of female sexual dysfunction in naturally menopausal women: results of a randomized active-controlled trial
    Esme A Nijland
    University Medical Center Groningen, Department of Psychosomatic Obstetrics and Gynaecology, Groningen, The Netherlands
    J Sex Med 5:646-56. 2008
    ..There are some data to suggest that tibolone improves sexual function in postmenopausal women. However, evidence about the effects of tibolone on female sexual dysfunction is lacking...
  81. ncbi Synthesis, biological evaluation, structural-activity relationship, and docking study for a series of benzoxepin-derived estrogen receptor modulators
    Irene Barrett
    School of Pharmacy and Pharmaceutical Sciences, Centre for Synthesis and Chemical Biology, Trinity College Dublin, Dublin 2, Ireland
    Bioorg Med Chem 16:9554-73. 2008
    ..series of novel benzoxepin-derived compounds are described as potent selective modulators of the human estrogen receptor modulators (SERMs). We report the antiproliferative effects of these compounds on human MCF-7 breast tumor cells...
  82. ncbi Cognitive function variations in postmenopausal women treated with continuous, combined HRT or tibolone. A comparison
    Hsien An Pan
    Departments of Obstetrics and Gynecology, Public Health and Neurology, National Cheng Kung University Hospital, Tainan, Taiwan
    J Reprod Med 48:375-80. 2003
    ..To compare cognitive function in postmenopausal women receiving continuous hormone replacement therapy and those receiving tibolone...
  83. ncbi Tibolone: clinical recommendations and practical guidelines. A report of the International Tibolone Consensus Group
    P Kenemans
    VU University Medical Center, Department of Obstetrics and Gynaecology, P O Box 7057, 1007 MB Amsterdam, The Netherlands
    Maturitas 51:21-8. 2005
    ....
  84. ncbi Tibolone relieves climacteric symptoms in highly symptomatic women with at least seven hot flushes and sweats per day
    M B Landgren
    Karolinska Hospital, Stockholm, Sweden
    Maturitas 50:222-30. 2005
    ....
  85. pmc The effects of tibolone in older postmenopausal women
    Steven R Cummings
    San Francisco Coordinating Center and the California Pacific Medical Center Research Institute, San Francisco, USA
    N Engl J Med 359:697-708. 2008
    ..Tibolone has estrogenic, progestogenic, and androgenic effects. Although tibolone prevents bone loss, its effects on fractures, breast cancer, and cardiovascular disease are uncertain...
  86. pmc Fulvestrant and the sequential endocrine cascade for advanced breast cancer
    S Johnston
    Department of Medicine Breast Unit, The Royal Marsden Hospital NHS Trust and Institute of Cancer Research, Fulham Road, London SW3 6JJ, UK
    Br J Cancer 90:S15-8. 2004
    ....
  87. ncbi Receptor profiling and endocrine interactions of tibolone
    Marcel E de Gooyer
    Department of Pharmacology, Research and Development, NV Organon, Molenstraat 110, P O Box 20, 5340 BH Oss, The Netherlands
    Steroids 68:21-30. 2003
    ..The estrogenic activity of the 3-hydroxytibolones masked the progestagenic activity of tibolone in rabbit endometrium. Full estrogenic response was observed in rat vaginal tissue after oral administration of tibolone...
  88. ncbi Identification of a negative regulatory surface within estrogen receptor alpha provides evidence in support of a role for corepressors in regulating cellular responses to agonists and antagonists
    Huey Jing Huang
    Department of Pharmacology and Cancer Biology, Duke University Medical Center, Durham, North Carolina 27710, USA
    Mol Endocrinol 16:1778-92. 2002
    ..In addition, our data suggest that corepressors, other than NCoR/SMRT, may be involved in ER signaling...
  89. ncbi Oestrogen-mediated suppression of tumour necrosis factor alpha-induced apoptosis in MCF-7 cells: subversion of Bcl-2 by anti-oestrogens
    M E Burow
    Center for Bioenvironmental Research, Tulane University Health Sciences Center, New Orleans, LA 70112, USA
    J Steroid Biochem Mol Biol 78:409-18. 2001
    ..Our results suggest that the effects of oestrogens/anti-oestrogens on the regulation of apoptosis may involve coordinate activation of signalling events and Bcl-2 expression...
  90. ncbi Utility of a juvenile fathead minnow screening assay for detecting (anti-)estrogenic substances
    Grace H Panter
    AstraZeneca Global Safety, Health and Environment, Brixham Environmental Laboratory, Devon, United Kingdom
    Environ Toxicol Chem 21:319-26. 2002
    ..The study showed that the use of VTG concentrations in mixed-sex juvenile fish provides a sensitive and robust assay for the detection of both estrogenic and antiestrogenic chemicals, with widely divergent potencies...
  91. ncbi The effects of tibolone on mood and libido
    Susan R Davis
    Jean Hailes Foundation, Clayton, Victoria, Australia
    Menopause 9:162-70. 2002
    ..To review published data pertaining to the effects of tibolone on sexual parameters, mood, and cognitive function in postmenopausal women...
  92. ncbi Quality of life and sexuality changes in postmenopausal women receiving tibolone therapy
    M H Wu
    Departments of Obstetrics and Gynecology, College of Medicine, National Cheng-Kung University, Tainan, Taiwan
    Climacteric 4:314-9. 2001
    ..CONCLUSIONS: The findings of this study indicate that both tibolone and continuous combined HRT have positive effects on the quality of life of Taiwanese postmenopausal women. Sexuality is affected more by tibolone than by HRT...
  93. ncbi Estrogen receptor modulators: relationships of ligand structure, receptor affinity and functional activity
    Owen B Wallace
    Lilly Research Laboratories, Indianapolis, IN 46285, USA
    Curr Top Med Chem 3:1663-82. 2003
    ..Recent advances in the design and synthesis of these non-steroidal and steroidal estrogen receptor ligands is reviewed. The relationship between the structural features of the ligand and receptor function is also discussed...
  94. ncbi The effect of tibolone versus 17beta-estradiol on climacteric symptoms in women with surgical menopause: a randomized, cross-over study
    A Somunkiran
    Abant Izzet Baysal University, Duzce Medical School, Department of Obstetrics and Gynecology, 81620 Konuralp, Duzce, Turkey
    Maturitas 56:61-8. 2007
    ..To compare the effectiveness of tibolone and 17beta-estradiol on climacteric symptoms, in a randomized, single-blind, cross-over study in surgically menopausal women...
  95. ncbi The role of tamoxifen in breast cancer prevention: issues sparked by the NSABP Breast Cancer Prevention Trial (P-1)
    N Wolmark
    Department of Human Oncology, Allegheny General Hospital, Pittsburgh, Pennsylvania 15212, USA
    Ann N Y Acad Sci 949:99-108. 2001
    ....
  96. ncbi Estrogen regulates Bcl-w and Bim expression: role in protection against beta-amyloid peptide-induced neuronal death
    Mingzhong Yao
    Davis School of Gerontology, University of Southern California, Los Angeles, California 90089, USA
    J Neurosci 27:1422-33. 2007
    ..These data provide new understanding into the mechanisms contributing to estrogen neuroprotection, a neural function with potential therapeutic relevance to Alzheimer's disease...
  97. ncbi Effects of tibolone and continuous combined hormone replacement therapy on mammographic breast density
    Eva Lundström
    Department of Obstetrics and Gynecology, Karolinska Hospital, Stockholm, Sweden
    Am J Obstet Gynecol 186:717-22. 2002
    ..Our purpose was to compare the effects of tibolone, continuous combined hormone replacement therapy, and placebo on mammographic breast density...
  98. ncbi Continuing outcomes relevant to Evista: breast cancer incidence in postmenopausal osteoporotic women in a randomized trial of raloxifene
    Silvana Martino
    Cancer Institute Medical Group, 2001 Santa Monica Blvd, Ste 560W, Santa Monica, CA 90404, USA
    J Natl Cancer Inst 96:1751-61. 2004
    ..We conducted the Continuing Outcomes Relevant to Evista (CORE) trial to examine the effect of 4 additional years of raloxifene therapy on the incidence of invasive breast cancer in women in MORE who agreed to continue in CORE...
  99. ncbi Estrogens and antiestrogens as etiological factors and therapeutics for prostate cancer
    Shuk Mei Ho
    Department of Environmental Health, College of Medicine, University of Cincinnati, Cincinnati, OH 45267, USA
    Ann N Y Acad Sci 1089:177-93. 2006
    ..These findings open new avenues for drug design that now focuses on developing a new generation of estrogen-based PCa therapies with maximal proapoptotic action but few or no side effects...
  100. ncbi The effect of tibolone and continuous combined conjugated equine oestrogens plus medroxyprogesterone acetate on progression of carotid intima-media thickness: the Osteoporosis Prevention and Arterial effects of tiboLone (OPAL) study
    Michiel L Bots
    Julius Center for Health Sciences and Primary Care, HP Str 6 131 University Medical Center Utrecht, Heidelberglaan 100, 3584 CX Utrecht, The Netherlands
    Eur Heart J 27:746-55. 2006
    ..Because the overall effect of tibolone on cardiovascular risk was unknown, the OPAL study was designed...
  101. ncbi Identification of novel oestrogen receptor target genes in human ZR75-1 breast cancer cells by expression profiling
    M Soulez
    Molecular Endocrinology Laboratory, Imperial Cancer Research Fund, 44 Lincoln's Inn Fields, London WC2A 3PX, UK
    J Mol Endocrinol 27:259-74. 2001
    ..Further analysis of this set of markers will provide alternative approaches to the investigation of the mitogenicity of oestrogens in breast cancer cells...

Research Grants67

  1. Personalized Clinical Diagnostics and Beyond: Integrated Ring Resonator Arrays
    Ryan Bailey; Fiscal Year: 2009
    ..This technology promises to broadly impact the landscape of the biomedical sciences, both meeting the clinical diagnostic challenges of today and pioneering the paradigm-shifting discoveries of tomorrow. ..
  2. Development of VN/14-1 and Related Analogs for Breast Cancer Therapy
    VINCENT COLLINS OFUKA NJAR; Fiscal Year: 2013
    ..and also antagonize uterine hyperplasia, characteristics that are distinct from those of selective estrogen receptor modulators (SERMs), such as tamoxifen and aromatase inhibitors (AIs)...
  3. Metabolic mechanisms of antiestrogen resistance in breast cancer
    UBALDO EMILIO MARTINEZ OUTSCHOORN; Fiscal Year: 2013
    ..I hope to become a physician scientist who links the laboratory and clinical research aspects to improve the lives of patients with breast cancer. 1 ..
  4. Runx Proteins and Sex Steroid Signaling in Bone
    Baruch Frenkel; Fiscal Year: 2009
    ..Incorporated into Aims 1-3 are experiments addressing novel mechanisms of action of selective estrogen receptor modulators (SERMs). Like estradiol, SERMs promote a physical interaction between ER[unreadable] and Runx2...
  5. INTERACTION OF THE ESTROGEN RECEPTOR WITH DNA
    ANN NARDULLI; Fiscal Year: 2013
    ..Estrogens and selective estrogen receptor modulators are widely used in regulating fertility, alleviating postmenopausal symptoms, and preventing and ..
  6. Sex Steroids and Runx Signaling in Bone
    Baruch Frenkel; Fiscal Year: 2013
    ..Incorporated into Aims 1-3 are experiments addressing novel mechanisms of action of selective estrogen receptor modulators (SERMs). Like estradiol, SERMs promote a physical interaction between ERa and Runx2...
  7. Optic Nerve Aging and Glaucoma
    Thasarat Vajaranant; Fiscal Year: 2013
    ..provide a foundation for future studies investigating the effects of aromatase inhibitors, selective estrogen receptor modulators and other anti- estrogen treatments on the optic nerve...
  8. REGULATION OF ATROPHY-INDUCED PROGENITOR CELLS IN THE GASTRIC CORPUS
    Jason C Mills; Fiscal Year: 2013
    ..Thus, the experiments proposed may help us begin to understand stem cell response to injury in multiple tissues and diseases. Finally, our new finding that the key drug tamoxifen causes gastric toxicity warrants further study in humans. ..
  9. Chemoprevention of Tamoxifen-induced Endometrial cancer by black cohosh and red c
    BIRGIT MARIA DIETZ; Fiscal Year: 2010
    ..We hypothesize that red clover and black cohosh, both frequently used for the alleviation of menopausal symptoms, will reduce tamoxifen-induced endometrial cancer due to their cancer chemopreventive properties. ..
  10. A novel therapy for HER2 positive hormone refractory breast cancer
    Anne W Hamburger; Fiscal Year: 2010
    ..Our studies would establish EBP1 as a new therapeutic agent in breast cancer to restore hormone sensitivity in cells which overexpress ErbB receptors. ..
  11. Regulation of miRNA in breast cancer
    Carolyn M Klinge; Fiscal Year: 2013
    ....
  12. Regulation of miRNA expression in breast cancer cells
    CAROLYN KLINGE; Fiscal Year: 2009
    ..It is our long term hope that miRNAs may provide novel biomarkers and new insights into the mechanisms by which breast tumors gain TAM/antiestrogen-resistance and become invasive and metastatic. ..
  13. Oxysterols, Estrogen Receptor Antagonism, and Vascular Disease
    Philip W Shaul; Fiscal Year: 2013
    ..By accomplishing these aims, we will increase our basic understanding of the biology of the only known endogenous SERM in the context of vascular health and disease. ..
  14. Estrogen Receptor-Coregulator Functional Interactions
    Carolyn Louise Smith; Fiscal Year: 2012
    ..latter interactions are important for determining the relative antagonist activity of selective estrogen receptor modulators (SERMs) such as 4HT...
  15. The Utility of Empiric Medical Treatment of Infertile Oligo-asthenospermic Men
    Peter R Casson; Fiscal Year: 2013
    ..The potential benefits of this therapy are enormous: 1) reduced healthcare cost;2) improved pregnancy outcomes;and 3) improved quality of life for previously infertile couples. ..
  16. Targeting Src Signaling Pathways to Promote Cell Cycle Arrest in Ovarian Cancer
    Fiona Simpkins; Fiscal Year: 2013
    ..Anti-estrogen treatment of early stage OVCA may prove to prevent or delay recurrence, which has never been explored. ..
  17. MOLECULAR PROBES FOR STEROID RECEPTORS
    John A Katzenellenbogen; Fiscal Year: 2012
    ..1) to understand the molecular basis of the diverse pharmacology of estrogens, including the selective estrogen receptor modulators (SERMs) and antiestrogens, (2) to develop novel inhibitors of estrogen action that act by blocking ..
  18. Mechanisms of Breast Tumor Cell Growth, Motility, and Antiestrogen Response
    Amy H Bouton; Fiscal Year: 2013
    ..abstract_text> ..
  19. A Hypersensitive ER alpha Mutant in Breast Cancer Hormone Resistance
    Suzanne Aw Fuqua; Fiscal Year: 2012
    ..We will test whether the mutation is associated with poor response to tamoxifen and the aromatase inhibitor anastrazole. ..
  20. A Neoadjuvant Trial of Anastrazole and A Novel SRC Inhibitor, AZD0530, for LABC
    JOYCE MARIE contact SLINGERLAND; Fiscal Year: 2010
    ..This trial may form the basis for subsequent, larger clinical trials to enhance the efficacy of endocrine therapy for breast cancer. ..
  21. Estrogen and Memory: Genetic Variation and Neuroimaging
    Susan K Conroy; Fiscal Year: 2013
    ..We will also investigate how changes in estrogen as a result of breast cancer treatment alter brain function, and relate these changes to memory function. ..
  22. Assessing and modifying bone quality in chronic kidney disease
    Chris Newman; Fiscal Year: 2013
    ..This study provides an important step in achieving this goal by examining these changes and their potential corrections in a rat model with the spontaneous and progressive development of chronic kidney disease. ..
  23. Mass spectrometry to decode PTM patterns and enhance the Biomarker utility of ER
    Christopher Benz; Fiscal Year: 2013
    ....
  24. Estrogen receptors in benign prostatic hyperplasia
    TRISTAN MARRINER NICHOLSON; Fiscal Year: 2013
    ..Prevention of BPH development will be tested with experimental selective estrogen receptor modulators (SERMs) that target relevant ER subtypes and the clinically relevant SERMs Raloxifene and Fulvestrant...
  25. Carcinogenic Metabolites Formed from Antiestrogen
    Judy L Bolton; Fiscal Year: 2013
    ..abstract_text> ..
  26. Second line breast cancer therapy through a novel Phytoantiestrogen
    SYREETA LATATIA TILGHMAN; Fiscal Year: 2013
    ....
  27. IRF1 regulation of BCL2 family members determines breast cancer cell fate
    JESSICA LEA ROBERTS; Fiscal Year: 2013
    ..The studies will also determine whether induction of IRF1 signaling can improve responsiveness to AEs when combined with a BCL2 inhibitor. ..
  28. Development of BRCA1-mimetic drugs for breast cancer
    Eliot M Rosen; Fiscal Year: 2013
    ..the BRCA1-mimetic compounds interact with ER-1 in a manner that is distinct from that of the selective estrogen receptor modulators (SERMs), such as Tamoxifen and Raloxifene...
  29. Epigenetic Marks of Xenoestrogen Exposure
    David J Waxman; Fiscal Year: 2010
    ....
  30. Botanical Estrogens: Mechanisms, Dose and Target Tissues
    William G Helferich; Fiscal Year: 2013
    ..of whether these botanical estrogens have activities similar to or distinct from estradiol or selective estrogen receptor modulators (SERMs)...
  31. The Role of CCN5 in Progression of Breast Cancer
    Sushanta K Banerjee; Fiscal Year: 2013
    ....
  32. Estrogen-neuroprotection due to astroglial Glu transporters occurs via TGF-a/b1
    EUN SOOK YU LEE; Fiscal Year: 2013
    ..goal of our research is to elucidate the neuroprotective mechanisms of 17B-Estradiol (E2) and selective estrogen receptor modulators (SERMs) and develop strategies for the discovery of suitable SERMs that can be used as neuroprotectants ..
  33. Phytoestrogen and Endogenous Estrogen Exposure and Risk of Stroke
    Xianglan Zhang; Fiscal Year: 2013
    ..evidence suggests that exposure to exogenous estrogens and estrogenic compounds such as selective estrogen receptor modulators (SERMs) and tibolone may increase the risk of stroke in women...
  34. Biointeractions of antiestrogens with nitric oxide
    Gregory R J Thatcher; Fiscal Year: 2013
    ..Selective estrogen receptor modulators (SERMs) could provide an alternative to HRT, but development has stalled because of the risk of side ..
  35. Estrogen support of Cerebellar Neurotransmission
    Paul G Mermelstein; Fiscal Year: 2013
    ..In addition, these results will have important implications in the use of estrogen receptor modulators to benefit health and its impact in the treatment of disease.
  36. Estrogen Receptors in Human Prostate Stem-Progenitor Cells
    Gail S Prins; Fiscal Year: 2013
    ..Targeted ER knockdown and selective estrogen receptor modulators (SERMs) will be tested to delineate estrogen actions and regulate PCa growth in vivo...
  37. Effects of chemotherapeutic agents on learning and memory in mice
    ELLEN ANN WALKER; Fiscal Year: 2013
    ..If certain drugs/combinations produce more adverse effects than others do, clinicians can make informed choices about their patients'therapy and improve the quality of life for cancer survivors and their families. ..
  38. G protein-coupled estrogen receptor GPER and breast carcinogenesis
    Eric R Prossnitz; Fiscal Year: 2013
    ..Anti-estrogen therapies in the form of selective estrogen receptor modulators (SERMs, such as tamoxifen) and selective estrogen receptor down regulators (SERDs, such as Fulvestrant) ..
  39. Molecular mechanism of ID1 function in advanced breast cancer
    Meiyun Fan; Fiscal Year: 2013
    ..abstract_text> ..
  40. Genetic Predictors of Anti-Estrogen Clinical Activity in Breast Cancer Patients
    James Michael Rae; Fiscal Year: 2013
    ..We hypothesize that a genetic approach can identify specific subsets of patients form whom one form of endocrine therapy (tamoxifen vs anastrozole) is better than the other. ..
  41. Development of an animal model to study how to prevent progression of hormone dep
    Gudmundur Thordarson; Fiscal Year: 2009
    ..abstract_text> ..
  42. Effects of herbs on transcription and cell proliferation
    Dale Leitman; Fiscal Year: 2003
    Multiple lines of evidence indicate that estrogens promote breast cancer, Selective estrogen receptor modulators (SERMs), such as tamoxifen are first-line drugs used as adjuvant therapy for preventing recurrences and reducing mortality ..
  43. Alternative mechanisms of selective estrogen receptor modulation in cancer preven
    Chin Yo Lin; Fiscal Year: 2010
    ..Selective estrogen receptor modulators (SERMs) have been shown to be effective in both preventing and treating ER- positive breast cancers...
  44. Rosiglitazone and Clomiphene for Ovulation Induction
    Nicholas Cataldo; Fiscal Year: 2002
    ..The effects of rosiglitazone on insulin secretion on OGTT will be correlated with its effects on the levels of the above hormones and binding proteins. ..
  45. Molecular Mechanisms and Application of Ah Receptor-MicroRNA Interactions
    Stephen H Safe; Fiscal Year: 2013
    ..The proposed studies will be the first to characterize the molecular mechanisms of AhR-miR interactions and development of SAhRMs for clinical applications in the treatment of ER-negative breast cancer. ..
  46. Assessment of Breast Cancer Risk with High Spectral and Spatial Resolution MRI
    Gillian Newstead; Fiscal Year: 2013
    ..We will compare the sensitivity of HiSS MRI to effects of tamoxifen therapy with that of 2D X-ray mammography and conventional MRI. ..
  47. Pharmacogenetics of Hormonal Therapy for Breast Cancer
    SUSAN ANN KADLUBAR; Fiscal Year: 2010
    ....
  48. BCAR3 and its Role in Breast Tumor Progression, Invasion, and Metastasis
    ASHLEY LAUREN WILSON; Fiscal Year: 2013
    ..Together, this training plan will provide a solid foundation upon which to build a career as a successful, independent breast cancer researcher. ..
  49. C. trachomatis increases transmission of HIV: mechanisms in the endocervix
    Danny J Schust; Fiscal Year: 2011
    ..trachomatis and HIV-1, including selective estrogen receptor modulators (SERMs), toll-like receptor modulators and probiotics. Our in vitro models for dual infection with C...
  50. Mechanisms of Cell Signaling in BCAR3-mediated Anti-Estrogen Resistance
    Michael S Guerrero; Fiscal Year: 2010
    ..In addition, by understanding the mechanisms responsible for resistance, it may be possible to develop new targeted therapies that can render perviously resistant tumors sensitive to these drugs. ..
  51. Understanding the origin,initiation,and progression of high-grade serous ovarian
    Jaeyeon Kim; Fiscal Year: 2013
    ..More important, the knowledge we will gain from these proposed studies will offer vital translational insights ? not only for the early detection and screening of ovarian cancer, but also for a new treatment for advanced ovarian cancer. ..
  52. PRESCRIPTION PATTERNS & PRACT FOR POSTMEMOPAUSAL THERAPY
    JENNIFER MIGLIONICO; Fiscal Year: 2000
    ..g., drugs to prevent and treat osteoporosis and selective estrogen receptor modulators) are being used to alleviate menopausal symptoms and, in some cases, to prevent some of the diseases ..
  53. Female Hormones and Vision
    Alvin Eisner; Fiscal Year: 2006
    ..The clinical emphasis will be on 2 types of medications - selective estrogen receptor modulators (SERMS) and aromatase inhibitors...
  54. SPORE IN BREAST CANCER
    Carlos L Arteaga; Fiscal Year: 2013
    ..The proposed Projects will require additional personnel and funded effort over that already maximally utilized in equivalent institutional Core Resources. ..
  55. TAMOXIFEN--RISK OF MI, STROKE AND VENOUS THROMBOEMBOLISM
    Leslie Bernstein; Fiscal Year: 2001
    ....
  56. Hormone Replacement Therapy, SERMs & Leg Blood Flow in Postmenopausal Women
    DOUGLAS SEALS; Fiscal Year: 2007
    ..The results should provide new insight into the effects of HRT and a SERM for augmenting LBF and LVC in estrogen deficient postmenopausal women and the underlying physiological mechanisms. ..
  57. Antiestrogen Regulation of Bladder Cancer
    Carolyn Smith; Fiscal Year: 2009
    ..of tumors;2) ER[unreadable] is expressed in multiple bladder cancer cell lines tested;3) the selective estrogen receptor modulators (SERMs), raloxifene and tamoxifen, inhibit growth of bladder cancer cell lines in vitro and 4) ..
  58. Chemoprevention of Uterine Cancer Risk by Antioxidants
    Minoti Sharma; Fiscal Year: 2003
    ..The long-term goal of this proposal is to evaluate if the combination of Tam or estrogen with nontoxic antioxidants will cooperate to reduce uterine cancer risk associated with chronic exposure to Tam or estrogen. ..
  59. REGULATION OF ESTROGEN-RESPONSIVE GENES
    ANN NARDULLI; Fiscal Year: 2007
    ..Moreover, estrogens and selective estrogen receptor modulators (SERMs) are widely used in regulating fertility, alleviating postmenopausal symptoms, and preventing ..
  60. A Pilot Trial of Oral Melatonin Supplementation in Breast Cancer Survivors
    Eva Schernhammer; Fiscal Year: 2007
    ..This pilot data could lay the groundwork for a large scale trial to assess the chemopreventive potential of melatonin in women, both with and without a personal history of breast cancer. [unreadable] [unreadable] [unreadable]..
  61. PSYCHOBIOLOGY OF ESTROGEN RECEPTOR MODULATORS
    Mark Wilson; Fiscal Year: 2003
    ..mediated through subtypes of the estrogen receptor (ER), the compounds are described as selective estrogen receptor modulators (SERMs)...
  62. MECHANISMS OF INHIBITION OF CHEMICAL CARCINOGENESIS
    George Bailey; Fiscal Year: 1999
    ..This renewal, along with a separate R-29 (RHD) and R01 (LFB), aim to provide the additional dose-response, risk-benefit, and mechanism studies that we believe necessary if I3C and chlorophylls are to proceed toward clinical trials. ..
  63. Dietary Isoflavones, Tamoxifen, and Tumor Growth
    William Helferich; Fiscal Year: 2005
    ..abstract_text> ..
  64. ESTROGEN AND THE MALE REPRODUCTIVE TRACT
    Rex Hess; Fiscal Year: 2000
    ..This research will provide basic information that will allow us to study disease processes that target the head of the epididymis and lead to male infertility. ..
  65. ANTIPROGESTINS AND ACTIVE CELL DEATH IN BREAST CANCER
    M El Etreby; Fiscal Year: 2001
    ..The studies could also impact the future clinical development of "antiprogestins" for this indication. ..
  66. Interactions between SERMs, soy and black cohosh
    Heather Shaw; Fiscal Year: 2007
    ..abstract_text> ..
  67. Phosphorylation of Estrogen Receptor and Coregulators
    BRIAN ROWAN; Fiscal Year: 2009
    ..abstract_text> ..