selective estrogen receptor modulators

Summary

Summary: A structurally diverse group of compounds distinguished from ESTROGENS by their ability to bind and activate ESTROGEN RECEPTORS but act as either an agonist or antagonist depending on the tissue type and hormonal milieu. They are classified as either first generation because they demonstrate estrogen agonist properties in the ENDOMETRIUM or second generation based on their patterns of tissue specificity. (Horm Res 1997;48:155-63)

Top Publications

  1. ncbi Selective estrogen receptor modulators decrease the production of interleukin-6 and interferon-gamma-inducible protein-10 by astrocytes exposed to inflammatory challenge in vitro
    M Cerciat
    Instituto Cajal, CSIC, Madrid, Spain
    Glia 58:93-102. 2010
  2. ncbi Effects of tamoxifen vs raloxifene on the risk of developing invasive breast cancer and other disease outcomes: the NSABP Study of Tamoxifen and Raloxifene (STAR) P-2 trial
    Victor G Vogel
    Magee Womens Hospital, University of Pittsburgh School of Medicine, University of Pittsburgh, Pittsburgh, PA 15213 3221, USA
    JAMA 295:2727-41. 2006
  3. ncbi Effects of raloxifene on cardiovascular events and breast cancer in postmenopausal women
    Elizabeth Barrett-Connor
    Department of Family and Preventive Medicine, University of California, San Diego, La Jolla 92093 0607, USA
    N Engl J Med 355:125-37. 2006
  4. ncbi Molecular determinants for the tissue specificity of SERMs
    Yongfeng Shang
    Department of Adult Oncology, Dana Farber Cancer Institute, 44 Binney Street, and Department of Medicine, Brigham and Women s Hospital and Harvard Medical School, Boston, MA 02115, USA
    Science 295:2465-8. 2002
  5. ncbi Chemoprevention of breast cancer with selective oestrogen-receptor modulators
    V Craig Jordan
    Fox Chase Cancer Center, 333 Cottman Avenue, Philadelphia, Pennsylvania 19111 2497, USA
    Nat Rev Cancer 7:46-53. 2007
  6. pmc Rapid activation of nuclear factor κB by 17β-estradiol and selective estrogen receptor modulators: pathways mediating cellular protection
    James P Stice
    Molecular and Cellular Cardiology, University of California, Davis, Davis, CA 95616, USA
    Shock 38:128-36. 2012
  7. pmc Effects of the selective estrogen receptor modulator raloxifene on coronary outcomes in the Raloxifene Use for The Heart trial: results of subgroup analyses by age and other factors
    Peter Collins
    Department of Cardiology, Royal Brompton and Harefield NHS Trust and NHLI, Imperial College London, Sydney Street, London, UK
    Circulation 119:922-30. 2009
  8. ncbi Bazedoxifene/conjugated estrogens and quality of life in postmenopausal women
    Wulf Utian
    Rapid Medical Research, Cleveland, OH, USA
    Maturitas 63:329-35. 2009
  9. ncbi Breast cancer incidence in the randomized PEARL trial of lasofoxifene in postmenopausal osteoporotic women
    Andrea Z LaCroix
    Fred Hutchinson Cancer Research Center, Seattle, WA 98109 1024, USA
    J Natl Cancer Inst 102:1706-15. 2010
  10. pmc The 2.0 A crystal structure of the ERalpha ligand-binding domain complexed with lasofoxifene
    Felix F Vajdos
    Department of Exploratory Medicinal Sciences, Pfizer Global Research and Development, Pfizer Inc, Groton, Connecticut 06340 8001, USA
    Protein Sci 16:897-905. 2007

Research Grants

Detail Information

Publications323 found, 100 shown here

  1. ncbi Selective estrogen receptor modulators decrease the production of interleukin-6 and interferon-gamma-inducible protein-10 by astrocytes exposed to inflammatory challenge in vitro
    M Cerciat
    Instituto Cajal, CSIC, Madrid, Spain
    Glia 58:93-102. 2010
    ..In addition, the possible anti-inflammatory effect of several selective estrogen receptor modulators (SERMs) was also assessed...
  2. ncbi Effects of tamoxifen vs raloxifene on the risk of developing invasive breast cancer and other disease outcomes: the NSABP Study of Tamoxifen and Raloxifene (STAR) P-2 trial
    Victor G Vogel
    Magee Womens Hospital, University of Pittsburgh School of Medicine, University of Pittsburgh, Pittsburgh, PA 15213 3221, USA
    JAMA 295:2727-41. 2006
    ..Tamoxifen is approved for the reduction of breast cancer risk, and raloxifene has demonstrated a reduced risk of breast cancer in trials of older women with osteoporosis...
  3. ncbi Effects of raloxifene on cardiovascular events and breast cancer in postmenopausal women
    Elizabeth Barrett-Connor
    Department of Family and Preventive Medicine, University of California, San Diego, La Jolla 92093 0607, USA
    N Engl J Med 355:125-37. 2006
    ..The effect of raloxifene, a selective estrogen-receptor modulator, on coronary heart disease (CHD) and breast cancer is not established...
  4. ncbi Molecular determinants for the tissue specificity of SERMs
    Yongfeng Shang
    Department of Adult Oncology, Dana Farber Cancer Institute, 44 Binney Street, and Department of Medicine, Brigham and Women s Hospital and Harvard Medical School, Boston, MA 02115, USA
    Science 295:2465-8. 2002
    b>Selective estrogen receptor modulators (SERMs) mimic estrogen action in certain tissues while opposing it in others...
  5. ncbi Chemoprevention of breast cancer with selective oestrogen-receptor modulators
    V Craig Jordan
    Fox Chase Cancer Center, 333 Cottman Avenue, Philadelphia, Pennsylvania 19111 2497, USA
    Nat Rev Cancer 7:46-53. 2007
    ..New medicines now promise to provide chemoprevention strategies for women at risk for the development of many diseases...
  6. pmc Rapid activation of nuclear factor κB by 17β-estradiol and selective estrogen receptor modulators: pathways mediating cellular protection
    James P Stice
    Molecular and Cellular Cardiology, University of California, Davis, Davis, CA 95616, USA
    Shock 38:128-36. 2012
    ..with NF-κB activation and the protective response and compared them with the effects of two selective estrogen receptor modulators (SERMs), raloxifene and tamoxifen...
  7. pmc Effects of the selective estrogen receptor modulator raloxifene on coronary outcomes in the Raloxifene Use for The Heart trial: results of subgroup analyses by age and other factors
    Peter Collins
    Department of Cardiology, Royal Brompton and Harefield NHS Trust and NHLI, Imperial College London, Sydney Street, London, UK
    Circulation 119:922-30. 2009
    ..We provide detailed results of the effect of raloxifene on coronary outcomes over time and for 24 subgroups (17 predefined, 7 post hoc)...
  8. ncbi Bazedoxifene/conjugated estrogens and quality of life in postmenopausal women
    Wulf Utian
    Rapid Medical Research, Cleveland, OH, USA
    Maturitas 63:329-35. 2009
    ..To assess the effects of bazedoxifene/conjugated estrogens (BZA/CE) on sleep parameters and health-related quality of life (HR-QOL)...
  9. ncbi Breast cancer incidence in the randomized PEARL trial of lasofoxifene in postmenopausal osteoporotic women
    Andrea Z LaCroix
    Fred Hutchinson Cancer Research Center, Seattle, WA 98109 1024, USA
    J Natl Cancer Inst 102:1706-15. 2010
    Currently available selective estrogen receptor modulators reduce the risk of breast cancer, but they are not widely used...
  10. pmc The 2.0 A crystal structure of the ERalpha ligand-binding domain complexed with lasofoxifene
    Felix F Vajdos
    Department of Exploratory Medicinal Sciences, Pfizer Global Research and Development, Pfizer Inc, Groton, Connecticut 06340 8001, USA
    Protein Sci 16:897-905. 2007
    ..The results suggest general features of ERalpha/SERM recognition, and add a new dimension to efforts to rationalize differences between the biological activity profiles exhibited by these important pharmacological agents...
  11. ncbi Ospemifene inhibits the growth of dimethylbenzanthracene-induced mammary tumors in Sencar mice
    Gregory T Wurz
    University of California, Davis, Department of Internal Medicine, Division of Hematology and Oncology, Cancer Center, Sacramento, 95817, USA
    J Steroid Biochem Mol Biol 97:230-40. 2005
    ..The results of these two studies suggest that women taking ospemifene for osteoporosis and/or urogenital atrophy may further benefit from ospemifene's breast cancer chemopreventive effects...
  12. 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
    ..Much 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 ..
  13. ncbi Effects of ospemifene, a novel SERM, on hormones, genital tract, climacteric symptoms, and quality of life in postmenopausal women: a double-blind, randomized trial
    Eeva Marja Rutanen
    Department of Obstetrics and Gynecology, Helsinki University Central Hospital, Helsinki, Finland
    Menopause 10:433-9. 2003
    ..We studied the effects of ospemifene on hormone levels, genital tract organs, climacteric symptoms, and quality of life...
  14. ncbi Lasofoxifene in postmenopausal women with osteoporosis
    Steven R Cummings
    San Francisco Coordinating Center, California Pacific Medical Center Research Institute, and University of California, San Francisco, San Francisco, USA
    N Engl J Med 362:686-96. 2010
    ..The effects of lasofoxifene on the risk of fractures, breast cancer, and cardiovascular disease are uncertain...
  15. ncbi Selective estrogen receptor modulators (SERMS) and their roles in breast cancer prevention
    Woo Chan Park
    Lynn Sage Breast Cancer Research Program, Robert H Lurie Comprehensive Cancer Center, Olson Pavilion 8258, 303 E Chicago Avenue, Chicago, IL 60611, USA
    Trends Mol Med 8:82-8. 2002
    ..Emerging knowledge about the action of SERMs will provide clues for the design of mechanism-based medicines...
  16. pmc Estrogen receptor and progesterone receptor as predictive biomarkers of response to endocrine therapy: a prospectively powered pathology study in the Tamoxifen and Exemestane Adjuvant Multinational trial
    John M S Bartlett
    Endocrine Cancer Group, Edinburgh Cancer Research Centre, Western General Hospital, Crewe Rd South, Edinburgh, EH4 2XR, United Kingdom
    J Clin Oncol 29:1531-8. 2011
    ....
  17. ncbi Sustained efficacy and safety of bazedoxifene in preventing fractures in postmenopausal women with osteoporosis: results of a 5-year, randomized, placebo-controlled study
    S L Silverman
    Cedars Sinai Medical Center and University of California, Los Angeles, CA, USA
    Osteoporos Int 23:351-63. 2012
    ..Bazedoxifene significantly increased bone mineral density and reduced bone turnover versus placebo and was generally safe and well tolerated...
  18. ncbi High levels of Cre expression in neuronal progenitors cause defects in brain development leading to microencephaly and hydrocephaly
    Paolo E Forni
    Department of Anatomy, Pharmacology, and Forensic Medicine, University of Turin, 10126 Turin, Italy
    J Neurosci 26:9593-602. 2006
    ..Furthermore, they underscore the potential risks for developmental studies of high levels of nuclear Cre in neurogenic cells...
  19. ncbi Signaling by estrogens
    Boris J Cheskis
    Women s Health and Musculoskeletal Biology, Wyeth Research, Collegeville, Pennsylvania 19426, USA
    J Cell Physiol 213:610-7. 2007
    ....
  20. pmc Neuroprotective actions of selective estrogen receptor modulators
    Lydia L Doncarlos
    Department of Cell Biology, Neurobiology and Anatomy, Stritch School of Medicine, Loyola University Chicago, 2160 South First Avenue, Maywood, IL 60153, USA
    Psychoneuroendocrinology 34:S113-22. 2009
    ..A potential therapeutic alternative to promote neuroprotection is the use of selective estrogen receptor modulators (SERMs), which may be designed to act with tissue selectivity as estrogen receptor agonists in the ..
  21. ncbi Selective estrogen receptor modulators as brain therapeutic agents
    Maria Angeles Arevalo
    Instituto Cajal, CSIC, Avenida Doctor Arce 37, E 28002 Madrid, Spain
    J Mol Endocrinol 46:R1-9. 2011
    b>Selective estrogen receptor modulators (SERMs), used for the treatment of breast cancer, osteoporosis, and menopausal symptoms, affect the nervous system...
  22. ncbi Selective estrogen receptor modulators decrease reactive astrogliosis in the injured brain: effects of aging and prolonged depletion of ovarian hormones
    George Barreto
    Instituto Cajal, Consejo Superior de Investigaciones Cientificas, Avenida Doctor Arce 37, E 28002 Madrid, Spain
    Endocrinology 150:5010-5. 2009
    ..In this study we assessed whether raloxifene and tamoxifen, two selective estrogen receptor modulators, have effects similar to estradiol in astrocytes...
  23. pmc Selectively targeting estrogen receptors for cancer treatment
    Erin K Shanle
    McArdle Laboratory for Cancer Research, University of Wisconsin, 1400 University Avenue, Madison, WI 53706, USA
    Adv Drug Deliv Rev 62:1265-76. 2010
    ..This review will present the mechanistic and structural features of ERs that determine tissue and subtype selectivity with an emphasis on current approaches to selectively target ERα and ERβ for cancer treatment...
  24. ncbi Clinical significance of estrogen receptor phosphorylation
    Leigh C Murphy
    Department of Biochemistry and Medical Genetics, Faculty of Medicine Manitoba Institute of Cell Biology, University of Manitoba, 675 McDermot Avenue, Winnipeg, Manitoba, Canada
    Endocr Relat Cancer 18:R1-14. 2011
    ..This suggests the hypothesis that phospho-profiling of ERα in human breast tumors to establish an 'ERα phosphorylation code', may be a more accurate marker of prognosis and/or response to endocrine therapy in human breast cancer...
  25. pmc Update on estrogens and the skeleton
    Sundeep Khosla
    Endocrine Research Unit, Guggenheim 7, College of Medicine, Mayo Clinic, 200 First Street SW, Rochester, Minnesota 55905, USA
    J Clin Endocrinol Metab 95:3569-77. 2010
    ..Given the diminishing clinical use of estrogen, it is logical to question whether estrogen regulation of bone remains a relevant issue at a clinical or basic research level...
  26. 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...
  27. ncbi Protective effects of estrogen and selective estrogen receptor modulators in the brain
    Krishnan M Dhandapani
    Institute of Molecular Medicine and Genetics, Program in Neurobiology, and Department of Neurology, Medical College of Georgia, Augusta, Georgia 30912, USA
    Biol Reprod 67:1379-85. 2002
    ..The important issue of whether clinically relevant selective estrogen receptor modulators (SERMs) such as tamoxifen and raloxifene and estrogen replacement therapy can exert ..
  28. ncbi Tamoxifen treatment for breast cancer and risk of endometrial cancer: a case-control study
    Anthony J Swerdlow
    Section of Epidemiology, Brookes Lawley Building, Institute of Cancer Research, Sutton, Surrey SM2 5NG, UK
    J Natl Cancer Inst 97:375-84. 2005
    ..We conducted a case-control study in Britain to investigate these risks...
  29. pmc Estrogen receptor transcription and transactivation: Estrogen receptor alpha and estrogen receptor beta: regulation by selective estrogen receptor modulators and importance in breast cancer
    B S Katzenellenbogen
    Department of Molecular and Integrative Physiology, University of Illinois at Urbana Champaign, 407 South Goodwin Avenue, Urbana, IL 61801 3704, USA
    Breast Cancer Res 2:335-44. 2000
    ..Certain compounds that act through the estrogen receptor (ER), now referred to as selective estrogen receptor modulators (SERMs), can demonstrate remarkable differences in activity in the various estrogen target tissues,..
  30. ncbi Cytochrome P450 3A4-mediated bioactivation of raloxifene: irreversible enzyme inhibition and thiol adduct formation
    Qing Chen
    Department of Drug Metabolism, Merck Research Laboratories, Rahway, New Jersey 07065, USA
    Chem Res Toxicol 15:907-14. 2002
    ..The significance of these findings with respect to the clinical use of raloxifene remains to be determined...
  31. ncbi Regulation of human cbfa1 gene transcription in osteoblasts by selective estrogen receptor modulators (SERMs)
    L Tou
    Harvard-Thorndike and Charles A. Dana Research Laboratories, Division of Bone and Mineral Metabolism, Department of Medicine, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA 02115, USA
    Mol Cell Endocrinol 183:71-9. 2001
    ..We examined the effect of selective estrogen receptor modulators (SERMs) on human cbfa1 gene promoter activity using cell-based luciferase reporter transcriptional ..
  32. ncbi Prevention of bone loss in postmenopausal women treated with lasofoxifene compared with raloxifene
    Michael R McClung
    Oregon Osteoporosis Center, Portland, OR 97213, USA
    Menopause 13:377-86. 2006
    ..The objective of this study was to compare the effects of lasofoxifene with raloxifene and placebo on indices of bone health in postmenopausal women...
  33. pmc Bioactivation of Selective Estrogen Receptor Modulators (SERMs)
    Tamara S Dowers
    Department of Medicinal Chemistry and Pharmacognosy M C 781, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, Illinois 60612 7231, USA
    Chem Res Toxicol 19:1125-37. 2006
  34. ncbi Bone turnover matters: the raloxifene treatment paradox of dramatic decreases in vertebral fractures without commensurate increases in bone density
    B Lawrence Riggs
    J Bone Miner Res 17:11-4. 2002
  35. ncbi Selective estrogen receptor modulators as inhibitors of repopulation of human breast cancer cell lines after chemotherapy
    Wu Licun
    Division of Experimental Therapeutics and Department of Medical Oncology and Hematology, Princess Margaret Hospital and University of Toronto, Toronto, Ontario M5G 2M9 Canada
    Clin Cancer Res 9:4614-8. 2003
    ..Here we study inhibition of repopulation of hormone-responsive human breast cancer cell lines by selective estrogen receptor (ER) modulators (SERMs) during courses of chemotherapy...
  36. ncbi A new approach to menopausal therapy: the tissue selective estrogen complex
    Barry S Komm
    Women s Health and Musculoskeletal Biology Research, Discovery Liaison, Wyeth Research, Collegeville, Pennsylvania 01242, USA
    Reprod Sci 15:984-92. 2008
    ..tissue selective estrogen complex may provide the therapeutic benefits of estrogens and selective estrogen receptor modulators with better tolerability and safety than either therapy alone...
  37. pmc Designing the ideal selective estrogen receptor modulator--an achievable goal?
    Hugh S Taylor
    Division of Reproductive Endocrinology, Yale University School of Medicine, New Haven, CT 06520 8063, USA
    Menopause 16:609-15. 2009
    b>Selective estrogen receptor modulators (SERMs), which lack the estrogen steroid moiety yet retain the ability to bind the estrogen receptor (ER), are known to confer mixed ER agonist or antagonist effects depending on the target tissue...
  38. ncbi SERMs: current status and future trends
    Karla C Morello
    Department of Internal Medicine, Division of Hematology Oncology, Cancer Center, University of California, Davis, 4501 X Street Room 3016, Sacramento, CA 95817, USA
    Crit Rev Oncol Hematol 43:63-76. 2002
    b>Selective estrogen receptor modulators, or SERMs, are a class of compounds that can act as estrogen receptor (ER) agonists in some tissues while acting as ER antagonists in others...
  39. ncbi Anti-inflammatory effect of selective estrogen receptor modulators (SERMs) in microglial cells
    T Suuronen
    Department of Neuroscience and Neurology, University of Kuopio, PO Box 1627, 70211 Kuopio, Finland
    Inflamm Res 54:194-203. 2005
    ..Our aim was to study how different SERMs modulate the inflammatory responses induced by lipopolysaccharide (LPS) or unmethylated CpG-oligonucleotides in mouse and rat microglial cells...
  40. ncbi Arzoxifene: a promising new selective estrogen receptor modulator for clinical chemoprevention of breast cancer
    Michael B Sporn
    Department of Pharmacology, Dartmouth Medical School, Hanover, New Hampshire 03755, USA
    Clin Cancer Res 10:5313-5. 2004
  41. ncbi Long-term dosing of arzoxifene lowers cholesterol, reduces bone turnover, and preserves bone quality in ovariectomized rats
    Yanfei L Ma
    Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana 46285, USA
    J Bone Miner Res 17:2256-64. 2002
    ..These data suggest that arzoxifene may be a useful therapeutic agent for osteoporosis in postmenopausal women...
  42. ncbi Oxidation of raloxifene to quinoids: potential toxic pathways via a diquinone methide and o-quinones
    Linning Yu
    Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, M C 781, Chicago, Illinois 60612 7231, USA
    Chem Res Toxicol 17:879-88. 2004
    ..These results suggest that raloxifene could be metabolized to electrophilic and redox active quinoids, which have the potential to cause toxicity in vivo...
  43. ncbi Differential time-dependent inactivation of P450 3A4 and P450 3A5 by raloxifene: a key role for C239 in quenching reactive intermediates
    Josh T Pearson
    Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc Seattle, WA 98119 3105, USA
    Chem Res Toxicol 20:1778-86. 2007
    ....
  44. pmc Update of the National Surgical Adjuvant Breast and Bowel Project Study of Tamoxifen and Raloxifene (STAR) P-2 Trial: Preventing breast cancer
    Victor G Vogel
    NSABP, Pittsburgh, PA 15212, USA
    Cancer Prev Res (Phila) 3:696-706. 2010
    ..These results have important public health implications and clarify that both raloxifene and tamoxifen are good preventive choices for postmenopausal women with elevated risk for breast cancer...
  45. ncbi The effect of the new SERM arzoxifene on growth and gene expression in MCF-7 breast cancer cells
    Cecilie T Freddie
    Department of Tumor Endocrinology, Institute of Cancer Biology, Danish Cancer Society, DK 2100 Copenhagen Ø, Denmark
    Mol Cell Endocrinol 219:27-36. 2004
    ..Moreover, arzoxifene displays less estrogen agonistic effects in MCF-7 cells than tamoxifen...
  46. ncbi Effects of raloxifene and estradiol on hippocampal acetylcholine release and spatial learning in the rat
    Robert B Gibbs
    Department of Pharmaceutical Sciences, University of Pittsburgh School of Pharmacy, 1004 Salk Hall, Pittsburgh, PA 15261, USA
    Psychoneuroendocrinology 29:741-8. 2004
    ....
  47. ncbi Estrogen and selective estrogen receptor modulators exert neuroprotective effects and stimulate the expression of selective Alzheimer's disease indicator-1, a recently discovered antiapoptotic gene, in human neuroblast long-term cell cultures
    Susanna Benvenuti
    Endocrine Unit, Department of Clinical Physiopathology, University of Florence, Viale Pieraccini, 6, 50139 Florence, Italy
    J Clin Endocrinol Metab 90:1775-82. 2005
    ..We found that 17beta-estradiol (17betaE(2)) and the selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen exerted neuroprotective effects, which were independent of cell ..
  48. ncbi In vitro and in vivo biologic effects of Ospemifene (FC-1271a) in breast cancer
    T L Taras
    Department of Internal Medicine, Division of Hematology/Oncology, Cancer Center, University of California, Davis, Room 3016, 4501 X Street, Sacramento, CA 95817, USA
    J Steroid Biochem Mol Biol 77:271-9. 2001
    ..In conclusion, FC-1271a appears to exert anti-estrogenic effects dependent on estrogen receptor positivity in vitro and in vivo on the growth of MCF-7 cells...
  49. pmc Tamoxifen: catalyst for the change to targeted therapy
    V Craig Jordan
    Alfred G Knudson Chair of Cancer Research, Fox Chase Cancer Center, Philadelphia, PA 19111, USA
    Eur J Cancer 44:30-8. 2008
    ..Currently, the pharmaceutical industry is exploiting the SERM concept for all members of the nuclear receptor superfamily so that medicines can now be developed for diseases once thought impossible...
  50. ncbi Randomized, double-blind, multicenter trial comparing two doses of arzoxifene (LY353381) in hormone-sensitive advanced or metastatic breast cancer patients
    J Baselga
    Vall d Hebron University Hospital, Barcelona, Spian
    Ann Oncol 14:1383-90. 2003
    ..The primary end point was to choose the best of two doses of arzoxifene based on the response rate or the clinical benefit rate (CBR). Pharmacokinetics and toxicities were also assessed...
  51. ncbi Effects of bazedoxifene/conjugated estrogens on endometrial safety and bone in postmenopausal women
    S Mirkin
    Pfizer Inc, Collegeville, PA, USA
    Climacteric 16:338-46. 2013
    ..This study evaluated the endometrial safety of BZA/CE and effects on bone mineral density (BMD) compared with CE/medroxyprogesterone acetate (MPA) and placebo...
  52. pmc Treatment with selective estrogen receptor modulators regulates myelin specific T-cells and suppresses experimental autoimmune encephalomyelitis
    Bruce F Bebo
    Neurological Sciences Institute, Oregon Health and Science University, Beaverton, Oregon, USA
    Glia 57:777-90. 2009
    ..b>Selective estrogen receptor modulators (SERMs) could provide an alternative therapeutic strategy, because they behave as estrogen ..
  53. ncbi Structure-based approach for the discovery of novel selective estrogen receptor modulators
    C Rosano
    S C Nanobiotecnologie, Istituto Nazionale per la Ricerca sul Cancro, 16132 Genova, Italy
    Curr Med Chem 18:1188-94. 2011
    ..examines the impact of Structure Based Drug Design (SBDD) on the discovery of ligands as the selective estrogen receptor modulators (SERMs) of the Estrogen Receptor (ER)α, which is involved in the regulation of several ..
  54. ncbi Efficacy of selective estrogen receptor modulators in nude mice bearing human transitional cell carcinoma
    Guru Sonpavde
    U S Oncology Research, Webster, Texas, USA
    Urology 69:1221-6. 2007
    ..To evaluate estrogen receptors as a therapeutic target for human bladder cancer...
  55. ncbi Endometrial effects of a tissue selective estrogen complex containing bazedoxifene/conjugated estrogens as a menopausal therapy
    James H Pickar
    Wyeth Research, Collegeville, Pennsylvania 19101, USA
    Fertil Steril 92:1018-24. 2009
    ..To evaluate the endometrial safety of a tissue selective estrogen complex (TSEC; pairing of a selective estrogen receptor modulator [SERM] with estrogens) composed of bazedoxifene/conjugated estrogens (BZA/CE) in postmenopausal women...
  56. ncbi Human splicing factor SPF45 (RBM17) confers broad multidrug resistance to anticancer drugs when overexpressed--a phenotype partially reversed by selective estrogen receptor modulators
    William L Perry
    Lilly Research Laboratories, Eli Lilly and Co, Indianapolis, Indiana 46285, USA
    Cancer Res 65:6593-600. 2005
    ..Thus, SPF45-mediated drug resistance in A2780 cells may result in part from effects of SPF45 on the transcription or alternate splicing of ERbeta-regulated genes...
  57. ncbi Effects of ospemifene and raloxifene on hormonal status, lipids, genital tract, and tolerability in postmenopausal women
    Janne Komi
    Hormos Medical Corporation, Turku, Finland
    Menopause 12:202-9. 2005
    ..To compare ospemifene and raloxifene regarding their effects on hormones, lipids, genital tract, and tolerability in postmenopausal women...
  58. ncbi Arzoxifene for prevention of fractures and invasive breast cancer in postmenopausal women
    Steven R Cummings
    San Francisco Coordinating Center, California Pacific Medical Center Research Institute and the University of California, San Francisco, CA 94107, USA
    J Bone Miner Res 26:397-404. 2011
    ..7%, with a 2.3-fold relative increase (95% CI 1.5-3.7). Like other SERMs, arzoxifene decreased vertebral fractures and invasive breast cancer while the risk of venous thromboembolic events increased...
  59. ncbi Transition from estrogen therapy to raloxifene in postmenopausal women: effects on treatment satisfaction and the endometrium-a pilot study
    Susan R Davis
    Jean Hailes Foundation, Melbourne, Australia
    Menopause 11:167-75. 2004
    ....
  60. ncbi Efficacy of tissue-selective estrogen complex of bazedoxifene/conjugated estrogens for osteoporosis prevention in at-risk postmenopausal women
    Robert Lindsay
    Department of Medicine, Helen Hayes Hospital, West Haverstraw, New York, New York, and Columbia University, New York, New York, USA
    Fertil Steril 92:1045-52. 2009
    ..To evaluate the efficacy of the tissue-selective estrogen complex, bazedoxifene/conjugated estrogens (BZA/CE), for postmenopausal osteoporosis prevention...
  61. ncbi Administration of raloxifene reduces sensorimotor and working memory deficits following traumatic brain injury
    Olga N Kokiko
    Restorative Neuroscience Laboratory, Department of Psychology, Southern Illinois University, Carbondale, IL 62901, USA
    Behav Brain Res 170:233-40. 2006
    ..Recent findings have shown that selective estrogen receptor modulators (SERMs) may have therapeutic benefit...
  62. ncbi Bazedoxifene/conjugated estrogens (BZA/CE): incidence of uterine bleeding in postmenopausal women
    David F Archer
    CONRAD Clinical Research Center, Eastern Virginia Medical School, Norfolk, Virginia 23507, USA
    Fertil Steril 92:1039-44. 2009
    ..To evaluate the effect of bazedoxifene/conjugated estrogens (BZA/CE), a tissue selective estrogen complex, on uterine bleeding in postmenopausal women...
  63. ncbi Relief of vasomotor symptoms with the tissue-selective estrogen complex containing bazedoxifene/conjugated estrogens: a randomized, controlled trial
    Joann V Pinkerton
    University of Virginia, Midlife Health Center and Division, Charlottesville, VA 22903, USA
    Menopause 16:1116-24. 2009
    ..The aim of this study was to assess the safety and efficacy of bazedoxifene (BZA)/conjugated estrogens (CE) treating moderate to severe vasomotor symptoms in the Selective Estrogen Menopause and Response to Therapy 2 trial...
  64. ncbi The cardiovascular effects of selective estrogen receptor modulators
    G E Christodoulakos
    Second Department of Obstetrics and Gynecology, Aretaieion Hospital, University of Athens, Athens, Greece
    Ann N Y Acad Sci 1092:374-84. 2006
    ..In the aftermath of the WHI, increased interest has been given to the action of selective estrogen receptor modulators (SERMs) and their effect on the cardiovascular system...
  65. ncbi Cognitive function in postmenopausal women treated with raloxifene
    K Yaffe
    Department of Psychiatry, University of California at San Francisco, 94121, USA
    N Engl J Med 344:1207-13. 2001
    ..CONCLUSIONS: Raloxifene treatment for three years does not affect overall cognitive scores in postmenopausal women with osteoporosis...
  66. ncbi Raloxifene is not associated with biologically relevant changes in hot flushes in postmenopausal women for whom therapy is appropriate
    Santiago Palacios
    Instituto Palacios, Madrid, Spain
    Am J Obstet Gynecol 191:121-31. 2004
    ..This study was undertaken to provide a detailed evaluation of the potential of raloxifene to induce or exacerbate hot flushes in postmenopausal women...
  67. ncbi Effects of bazedoxifene/conjugated estrogens on quality of life in postmenopausal women with symptoms of vulvar/vaginal atrophy
    G Bachmann
    Department of Obstetrics, Gynecology and Reproductive Sciences, University of Medicine and Dentistry of New Jersey Robert Wood Johnson Medical School, New Brunswick, NJ, USA
    Climacteric 13:132-40. 2010
    ..To evaluate the effects of the tissue selective estrogen complex (TSEC) pairing bazedoxifene (BZA) with conjugated estrogens (CE) on sexual function and quality of life in postmenopausal women...
  68. ncbi Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity
    Zhihui Qin
    Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, Illinois 60612 7231, USA
    J Med Chem 50:2682-92. 2007
    The regulation of estrogenic and antiestrogenic effects of selective estrogen receptor modulators (SERMs) is thought to underlie their clinical use...
  69. pmc Tamoxifen mediated estrogen receptor activation protects against early impairment of hippocampal neuron excitability in an oxygen/glucose deprivation brain slice ischemia model
    Huaqiu Zhang
    Department of Neurosurgery, Tongji Hospital, Tongji Medical College, Huazhong, University of Science and Technology, Wuhan, 430030, PR China
    Brain Res 1247:196-211. 2009
    ....
  70. ncbi Safety and tolerability of bazedoxifene in postmenopausal women with osteoporosis: results of a 5-year, randomized, placebo-controlled phase 3 trial
    T J de Villiers
    Panorama MediClinic and University of Stellenbosch, Room 118 Parow 7500, Cape Town, South Africa
    Osteoporos Int 22:567-76. 2011
    ..Overall, the results at 5 years were consistent with those seen at 3 years...
  71. ncbi Bazedoxifene effects on the reproductive tract in postmenopausal women at risk for osteoporosis
    Joann V Pinkerton
    University of Virginia, Charlottesville, VA 22908, USA
    Menopause 16:1102-8. 2009
    ..The aim of this study was to examine the endometrial, ovarian, and breast safety of bazedoxifene, a novel selective estrogen-receptor modulator, in postmenopausal women at risk for osteoporosis...
  72. pmc Signaling, physiological functions and clinical relevance of the G protein-coupled estrogen receptor GPER
    Eric R Prossnitz
    Department of Cell Biology and Physiology and UNM Cancer Center, University of New Mexico, Albuquerque, NM 87131, USA
    Prostaglandins Other Lipid Mediat 89:89-97. 2009
    ....
  73. ncbi Bioactivation of the selective estrogen receptor modulator desmethylated arzoxifene to quinoids: 4'-fluoro substitution prevents quinoid formation
    Hong Liu
    Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, M C 781, Chicago, Illinois 60612 7231, USA
    Chem Res Toxicol 18:162-73. 2005
    Although selective estrogen receptor modulators (SERMs) are useful in the treatment and prevention of breast cancer, the SERM tamoxifen has been associated with an increased risk of endometrial cancer possibly due to metabolism to ..
  74. ncbi Not all SERMs are created equal
    Steven R Goldstein
    Menopause 13:325-7. 2006
  75. ncbi Estrogenic agonist activity of ICI 182,780 (Faslodex) in hippocampal neurons: implications for basic science understanding of estrogen signaling and development of estrogen modulators with a dual therapeutic profile
    Liqin Zhao
    Molecular Pharmacology and Toxicology, Neuroscience, and Biomedical Engineering, University of Southern California, 1985 Zonal Avenue, PSC 503, Los Angeles, CA 90089, USA
    J Pharmacol Exp Ther 319:1124-32. 2006
    ....
  76. pmc Potential of selective estrogen receptor modulators as treatments and preventives of breast cancer
    Jing Peng
    Fox Chase Cancer Center, 333 Cottman Avenue, Philadelphia, PA 19111, USA
    Anticancer Agents Med Chem 9:481-99. 2009
    ..b>Selective estrogen receptor modulators (SERMs) are synthetic molecules which bind to ER and can modulate its transcriptional capabilities ..
  77. ncbi Monocyte-macrophage system as a target for estrogen and selective estrogen receptor modulators
    Pirkko L Härkönen
    Lund University, Department of Laboratory Medicine, Tumor Biology, Malmo University Hospital, CRC Entrance 72, 205 02 Malmo, Sweden
    Ann N Y Acad Sci 1089:218-27. 2006
    ....
  78. ncbi Endoxifen, a secondary metabolite of tamoxifen, and 4-OH-tamoxifen induce similar changes in global gene expression patterns in MCF-7 breast cancer cells
    Young Chai Lim
    Division of Clinical Pharmacology, Indiana University School of Medicine, 1001 West 10th Street, WD Myers Bldg, W7123, Indianapolis, IN 46202, USA
    J Pharmacol Exp Ther 318:503-12. 2006
    ..We conclude that endoxifen and 4-OH-Tam have similar effects on global gene expression patterns in MCF-7 cells and that the majority of the affected genes are estrogen-regulated genes...
  79. ncbi Additive effects of raloxifene and alendronate on bone density and biochemical markers of bone remodeling in postmenopausal women with osteoporosis
    Olof Johnell
    Department of Orthopaedics, Universiteitssjukhuset MAS, Malmø, Sweden
    J Clin Endocrinol Metab 87:985-92. 2002
    ..RLX+ALN reduced bone turnover more than either drug alone, resulting in greater BMD increment, but whether this difference reflects better fracture risk reduction was not assessed in this study...
  80. ncbi Structural modulation of reactivity/activity in design of improved benzothiophene selective estrogen receptor modulators: induction of chemopreventive mechanisms
    Bolan Yu
    Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612, USA
    Mol Cancer Ther 6:2418-28. 2007
    The benzothiophene selective estrogen receptor modulators (SERM) raloxifene and arzoxifene are in clinical use and clinical trials for chemoprevention of breast cancer and other indications...
  81. ncbi Activity of three selective estrogen receptor modulators on hormone-dependent responses in the mouse uterus and mammary gland
    Judy S Crabtree
    Endocrinology and Reproductive Disorders Division, Women s Health and Musculoskeletal Biology, Wyeth Research, Collegeville, PA 19426, USA
    Mol Cell Endocrinol 287:40-6. 2008
    b>Selective estrogen receptor modulators (SERMs) have the unique potential to provide estrogenic effects in the skeletal and cardiovascular system, while minimizing/eliminating side effects on reproductive organs...
  82. ncbi Evaluation of bazedoxifene/conjugated estrogens for the treatment of menopausal symptoms and effects on metabolic parameters and overall safety profile
    Rogerio A Lobo
    Columbia University Medical Center, New York, New York
    Fertil Steril 92:1025-38. 2009
    ..To evaluate the effects of a tissue-selective estrogen complex (TSEC) composed of bazedoxifene/conjugated estrogens (BZA/CE) on menopausal symptoms, metabolic parameters, and overall safety...
  83. ncbi Risk of ischemic stroke with tamoxifen treatment for breast cancer: a meta-analysis
    Cheryl D Bushnell
    Department of Medicine Neurology, Duke University Medical Center, Durham, NC 27710, USA
    Neurology 63:1230-3. 2004
    ..To assess the overall risk of stroke, specifically ischemic stroke, associated with tamoxifen use by performing a meta-analysis of data reported in breast cancer trials...
  84. ncbi Selective estrogen receptor modulators protect hippocampal neurons from kainic acid excitotoxicity: differences with the effect of estradiol
    Iratxe Ciriza
    Instituto Cajal, C S I C, E 28002 Madrid, Spain
    J Neurobiol 61:209-21. 2004
    ..b>Selective estrogen receptor modulators (SERMs) may represent an alternative to estrogen for the treatment or the prevention of ..
  85. ncbi Safety and efficacy results of a randomized trial comparing adjuvant toremifene and tamoxifen in postmenopausal patients with node-positive breast cancer. Finnish Breast Cancer Group
    K Holli
    Department of Oncology and Palliative Medicine, Tampere University Hospital, Tampere, Finland
    J Clin Oncol 18:3487-94. 2000
    ..In this multicenter trial, toremifene 40 mg/d was compared with tamoxifen 20 mg/d, both given orally for 3 years to postmenopausal, axillary node-positive women after breast surgery...
  86. ncbi The effects of estradiol and selective estrogen receptor modulators on gene expression and messenger RNA stability in immortalized sheep endometrial stromal cells and human endometrial adenocarcinoma cells
    Yuhua Z Farnell
    Departments of Animal Science, Faculty of Genetics, Texas A and M University, College Station, TX 77843 2471, USA
    J Steroid Biochem Mol Biol 84:453-61. 2003
    ..Its antagonism by ICI 182,780 reveals that ER protein is involved in this E2 response...
  87. ncbi Selective estrogen receptor modulators (SERMs) for the brain: current status and remaining challenges for developing NeuroSERMs
    Liqin Zhao
    Department of Molecular Pharmacology and Toxicology and the Program in Neuroscience, School of Pharmacy, University of Southern California, Pharmaceutical Sciences Center, Los Angeles, CA 90089, USA
    Brain Res Brain Res Rev 49:472-93. 2005
    ..Results of these endeavors have yielded insights into strategies for developing novel molecules with NeuroSERM potential in order to prevent brain related climacteric symptoms and neurodegenerative diseases...
  88. pmc Selective estrogen receptor modulators inhibit growth and progression of premalignant lesions in a mouse model of ductal carcinoma in situ
    Ruria Namba
    Department of Pathology and Laboratory Medicine, School of Medicine, University of California, Davis, Sacramento, CA, USA
    Breast Cancer Res 7:R881-9. 2005
    ..demonstrate the utility of a mouse transplantation model of DCIS for chemoprevention studies using selective estrogen receptor modulators (SERMs)...
  89. pmc Effect of raloxifene on stroke and venous thromboembolism according to subgroups in postmenopausal women at increased risk of coronary heart disease
    Lori Mosca
    Director, Preventive Cardiology, New York Presbyterian Hospital, 601 West 168th Street, 43, New York, NY 10032, USA
    Stroke 40:147-55. 2009
    ..The purpose of this analysis was to evaluate the effect of raloxifene on the incidence of all strokes, stroke deaths, and venous thromboembolic events according to participant subgroups...
  90. ncbi Tamoxifen, a selective estrogen receptor modulator, reduces ischemic damage caused by middle cerebral artery occlusion in the ovariectomized female rat
    Shyamal H Mehta
    Department of Physiology, Medical College of Georgia, Augusta, GA 30912, USA
    Neuroendocrinology 77:44-50. 2003
    ..These studies suggest that clinically important SERMs may have an additional unrecognized beneficial effect of protection of the female brain...
  91. ncbi Bazedoxifene, a selective estrogen receptor modulator: effects on the endometrium, ovaries, and breast from a randomized controlled trial in osteoporotic postmenopausal women
    David F Archer
    CONRAD Clinical Research Center, Eastern Virginia Medical School, Norfolk, VA 23507, USA
    Menopause 16:1109-15. 2009
    ..The aim of this study was to evaluate the endometrial, ovarian, and breast safety of bazedoxifene used as a treatment for postmenopausal osteoporosis...
  92. pmc The NSABP Study of Tamoxifen and Raloxifene (STAR) trial
    Victor G Vogel
    University of Pittsburgh Cancer Institute, Magee Womens Hospital, Pittsburgh, PA 15213 3180, USA
    Expert Rev Anticancer Ther 9:51-60. 2009
    ..The risk of other cancers, fractures, ischemic heart disease and stroke is similar for both drugs...
  93. ncbi Gender difference in the neuroendocrine regulation of growth hormone axis by selective estrogen receptor modulators
    Vita Birzniece
    Garvan Institute of Medical Research, Darlinghurst, New South Wales 2010, Australia
    J Clin Endocrinol Metab 97:E521-7. 2012
    ..Tamoxifen and raloxifene are selective estrogen receptor modulators (SERMs), drugs that block central estrogen action but exert estrogen-like effects in the liver, ..
  94. ncbi Effects of selective estrogen receptor modulators on allocentric working memory performance and on dendritic spines in medial prefrontal cortex pyramidal neurons of ovariectomized rats
    D A Velázquez-Zamora
    Laboratorio de Psicobiologia, Division de Neurociencias, CIBO, IMSS, Guadalajara, Jal, Mexico
    Horm Behav 61:512-7. 2012
    Estradiol and some selective estrogen receptor modulators (SERMs) are neuroprotective in a variety of experimental models of neurodegeneration, reduce the inflammatory response of glial cells, reduce anxiety and depression, promote ..
  95. ncbi Review on raloxifene: profile of a selective estrogen receptor modulator
    M Heringa
    Medical Department, Division of Nephrology, University of Ulm, Germany
    Int J Clin Pharmacol Ther 41:331-45. 2003
    ..5 h. Less than 0.2% of an oral dose is excreted unchanged in the urine and less than 6% is excreted in urine as glucuronide conjugates. Serious adverse event caused by raloxifene is a 3-fold increase in the risk of thromboembolic events...
  96. ncbi Effects of various selective estrogen receptor modulators with or without conjugated estrogens on mouse mammary gland
    Bryan J Peano
    Department of Women s Health and Musculoskeletal Biology, Wyeth Research, Collegeville, Pennsylvania 19426, USA
    Endocrinology 150:1897-903. 2009
    b>Selective estrogen receptor modulators (SERMs) are small molecules that, depending on the end point measured, may either function as estrogen receptor (ER) agonists or antagonize estrogens' agonist activity...
  97. ncbi Impact of the selective estrogen receptor modulator, tamoxifen, on neuronal outgrowth and survival following toxic insults associated with aging and Alzheimer's disease
    Kathleen O'Neill
    Department of Molecular Pharmacology and Toxicology, University of Southern California, Pharmaceutical Sciences Center, Los Angeles 90033, USA
    Exp Neurol 188:268-78. 2004
    We investigated the estrogen agonist/antagonist properties of the selective estrogen receptor modulators (SERMs), tamoxifen (TMX) and 4-hydroxy-tamoxifen (OHT), using an in vitro neuron model system to determine the impact of the ..
  98. 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...
  99. ncbi Selective estrogen receptor modulators
    Henry U Bryant
    Lilly Research Laboratories, Indianapolis IN, USA
    Rev Endocr Metab Disord 3:231-41. 2002
  100. ncbi [Effects of different treatments for osteoporosis on prevention of fractures: toward and individualized and economic approach]
    O Lamy
    Service de Medecine A, CHUV, Lausanne
    Praxis (Bern 1994) 93:399-405. 2004
    ..Economical analyses take into account the health care resources needed to get these benefits. At 50 years, only calcium and vitamin D are cost-effective, whereas at 70 years, bisphosphonates and raloxifene are also cost-effective...
  101. ncbi Effects of ospemifene, a novel SERM, on vascular markers and function in healthy, postmenopausal women
    Olavi Ylikorkala
    Department of Obstetrics and Gynecology, Helsinki University Central Hospital, Helsinki, Finland
    Menopause 10:440-7. 2003
    ..Ospemifene, a novel selective estrogen receptor modulator (SERM), shows promise for bone preservation in postmenopausal women. This study examined the effects of ospemifene on different vascular surrogate markers...

Research Grants63

  1. Development of VN/14-1 and Related Analogs for Breast Cancer Therapy
    VINCENT COLLINS OFUKA NJAR; Fiscal Year: 2013
    ..cancers, and also antagonize uterine hyperplasia, characteristics that are distinct from those of selective estrogen receptor modulators (SERMs), such as tamoxifen and aromatase inhibitors (AIs)...
  2. 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...
  3. 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 ..
  4. 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...
  5. Optic Nerve Aging and Glaucoma
    Thasarat Vajaranant; Fiscal Year: 2013
    ..will 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...
  6. 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. ..
  7. 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. ..
  8. Regulation of miRNA in breast cancer
    Carolyn M Klinge; Fiscal Year: 2013
    ....
  9. 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. ..
  10. 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. ..
  11. Estrogen Receptor-Coregulator Functional Interactions
    Carolyn Louise Smith; Fiscal Year: 2012
    ..4HT);the latter interactions are important for determining the relative antagonist activity of selective estrogen receptor modulators (SERMs) such as 4HT...
  12. 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. ..
  13. MOLECULAR PROBES FOR STEROID RECEPTORS
    John A Katzenellenbogen; Fiscal Year: 2012
    ..are (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 ..
  14. 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. ..
  15. 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. ..
  16. 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 ..
  17. Carcinogenic Metabolites Formed from Antiestrogen
    Judy L Bolton; Fiscal Year: 2013
    ..abstract_text> ..
  18. 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...
  19. The role of HDAC2 in hormone therapy resistance
    Pamela N Munster; Fiscal Year: 2013
    ....
  20. Epigenetic Marks of Xenoestrogen Exposure
    David J Waxman; Fiscal Year: 2010
    ....
  21. 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)...
  22. 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 ..
  23. Phytoestrogen and Endogenous Estrogen Exposure and Risk of Stroke
    Xianglan Zhang; Fiscal Year: 2013
    ..Mounting 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...
  24. UAB Rexinoids for Breast Cancer Prevention
    Donald D Muccio; Fiscal Year: 2011
    ..This SPORE project impacts public health by the development of drugs that may prevent breast cancer. ..
  25. Biointeractions of antiestrogens with nitric oxide
    Gregory R J Thatcher; Fiscal Year: 2013
    ..b>Selective estrogen receptor modulators (SERMs) could provide an alternative to HRT, but development has stalled because of the risk of ..
  26. 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...
  27. 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 ..
  28. 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. ..
  29. Ohio State University DISCOVERY PREP for Biomedical Research
    Virginia M Sanders; Fiscal Year: 2013
    ..The program will increase the likelihood of admission to, and graduation from, a highly competitive Ph.D. program in biomedical science research. ..
  30. 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 ..
  31. Actions of Endoxifen on the Skeleton
    Anne Gingery; Fiscal Year: 2013
    ....
  32. Alternative mechanisms of selective estrogen receptor modulation in cancer preven
    Chin Yo Lin; Fiscal Year: 2010
    ..b>Selective estrogen receptor modulators (SERMs) have been shown to be effective in both preventing and treating ER- positive breast ..
  33. 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. ..
  34. 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. ..
  35. 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...
  36. 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 ..
  37. 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...
  38. MODEL FOR PELVIC FLOOR DISORDERS
    Amanda Clark; Fiscal Year: 2004
    ..abstract_text> ..
  39. 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) ..
  40. 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. ..
  41. 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 ..
  42. PSYCHOBIOLOGY OF ESTROGEN RECEPTOR MODULATORS
    Mark Wilson; Fiscal Year: 2003
    ..are likely mediated through subtypes of the estrogen receptor (ER), the compounds are described as selective estrogen receptor modulators (SERMs)...
  43. Interactions between SERMs, soy and black cohosh
    Heather Shaw; Fiscal Year: 2007
    ..abstract_text> ..
  44. Phosphorylation of Estrogen Receptor and Coregulators
    BRIAN ROWAN; Fiscal Year: 2009
    ..abstract_text> ..
  45. CVD Mechanisms Associated with Phytoestrogens Use
    Donna Kritz Silverstein; Fiscal Year: 2003
    ..Given that women can expect to live one-third of their lives after menopause, it is important to know whether and how phytoestrogens may modify cardiovascular disease mechanisms. ..
  46. COGNITIVE AGING: EFFECTS OF ESTRADIOL AND RALOXIFENE
    AGNES LACREUSE; Fiscal Year: 2000
    ..These compounds called selective Estrogen Receptor Modulators(SERMs), have a well-documented efficacy in peripheral target tissues, but their effects on ..
  47. Development and use of systems to study estrogen action
    SUSAN NAGEL; Fiscal Year: 2005
    ..the identification of 1) genes regulated in individual cells where ER-ligands, both estrogens and selective estrogen receptor modulators (SERMs), exert agonist activity and 2) novel ER comodulatory proteins...
  48. Selective estrogen modulators and cognition
    James Herndon; Fiscal Year: 2005
    ..A new group of non-steroidal estrogens, deemed Selective Estrogen Receptor Modulators (SERMs) has been developed as a possible alternative to ERT but without the adverse proliferative ..
  49. WORLD CONGRESS ON OSTEOPOROSIS 2000
    Paula Stern; Fiscal Year: 2000
    ..nutrition and bone disease; estrogens and progestins; men with osteoporosis; bone forming agents; selective estrogen receptor modulators; and bisphosphonates, among others through 12 plenary sessions, 50 abstract presentations, 700-to- ..
  50. Estrogens, Paracrine Factors, and Endometrial Cancer
    David Kaufman; Fiscal Year: 2006
    ..Despite this, Selective Estrogen Receptor Modulators (SERMs) and protective, anti-proliferative phytoestrogens that influence this process have only ..
  51. SELECTIVE ESTROGEN RECEPTOR MODULATORS
    Ashraf Saeed; Fiscal Year: 1999
    The long-term goal of this proposal is to develop selective estrogen receptor modulators for the treatment of hormone dependent medical disorders such as breast cancer and osteoporosis...
  52. HTS for Androgen Receptor Antagonists that Recruit NCoR
    Steven Balk; Fiscal Year: 2006
    ..Significantly, the molecular mechanism of action for the selective estrogen receptor modulators (SERMs) appears to be that they favor recruitment of NCoR and SMRT...
  53. Estrogen Receptor Modulators and Dendritic Cell Function
    Susan Kovats; Fiscal Year: 2006
    ..or treatment of breast cancer involve partial blockade of systemic estrogen responses via selective estrogen receptor modulators (SERM)...
  54. Estrogen enhancement of endothelial vasodilatory factors
    Roshanak Rahimian; Fiscal Year: 2003
    ..The enhanced insight into these protective mechanisms is expected to eventually also be beneficial for the male population. ..
  55. LEVORMELOXIFENE EFFECTS ON CORONARY ATHEROSCLEROSIS
    James Goodrich; Fiscal Year: 1999
    ..Therefore the current hope for the future are selective estrogen receptor modulators (SERMS). The properties of this class of drug allow it to act only on certain tissues...
  56. Functional Genetic Tests for Breast Cancer Diagnosis
    GRANT BITTER; Fiscal Year: 2003
    ..abstract_text> ..
  57. BIOLOGICAL MARKERS OF BREAST CANCER & TAMOXIFEN RESPONSE
    Timothy Rebbeck; Fiscal Year: 2004
    ..In addition, we will have evaluated the potential of MRI-detected breast changes as surrogate endpoints and accumulated data on a range of histopathologic lesions that may be used as surrogate endpoints as well. ..
  58. Acceptance of Breast Cancer Chemoprevention Therapy
    MFON CYRUS DAVID; Fiscal Year: 2006
    ..are to identify the factors that influence the acceptance of breast cancer chemoprevention with selective estrogen receptor modulators (SERMs), and to increase the depth of my knowledge in this field by taking related didactic ..
  59. Anabolic Skeletal Agents for Osteoporosis
    Andrew Stewart; Fiscal Year: 2004
    ..osteoclastic bone resorption using a family of so called "anti-resorptive" drugs such as estrogen, selective estrogen receptor modulators, bisphosphonates and calcitonin...
  60. Evolution of Estrogen Receptor-Ligand Interactions
    Jennifer Fox; Fiscal Year: 2006
    ..Such an experimental system will allow the rigorous testing of hypotheses about ER-ligand structure function relationships and the dynamics of receptor-ligand coevolution. ..
  61. RALOXIFENE EFFECTS ON COGNITION IN EARLY MENOPAUSE
    MARGARET UPCHURCH; Fiscal Year: 2001
    ..Digit span and Trail-Making Test performance, skills for which there is little evidence of an estrogen effect, will also be measured. ..
  62. FRET-based HTS Assay for Estrogen Receptor Modulators
    SID DE; Fiscal Year: 2003
    ....
  63. Fas/FasL System In Normal Mammary Gland Development
    Gil Mor; Fiscal Year: 2003
    ..and FasL expression and function; and 4) Study the regulation of FasL expression by estrogen and selective estrogen receptor modulators (SERMs). A thin line separates normal from neoplastic development...