mifepristone

Summary

Summary: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME.

Top Publications

  1. ncbi Mifepristone, a glucocorticoid receptor antagonist, produces clinical and metabolic benefits in patients with Cushing's syndrome
    Maria Fleseriu
    Northwest Pituitary Center, Department of Medicine, Oregon Health and Science University, Portland, Oregon 97239, USA
    J Clin Endocrinol Metab 97:2039-49. 2012
  2. ncbi Monocyte chemoattractant protein-1 (CCL-2) integrates mechanical and endocrine signals that mediate term and preterm labor
    Oksana Shynlova
    Samuel Lunenfeld Research Institute, Mount Sinai Hospital, Toronto, Ontario, Canada
    J Immunol 181:1470-9. 2008
  3. pmc Antiprogestin mifepristone inhibits the growth of cancer cells of reproductive and non-reproductive origin regardless of progesterone receptor expression
    Chelsea R Tieszen
    Division of Basic Biomedical Sciences, Sanford School of Medicine of the University of South Dakota, Vermillion, SD, USA
    BMC Cancer 11:207. 2011
  4. ncbi RU486 (mifepristone): mechanisms of action and clinical uses
    F Cadepond
    INSERM U33, , France
    Annu Rev Med 48:129-56. 1997
  5. pmc A conditional tissue-specific transgene expression system using inducible GAL4
    T Osterwalder
    Department of Molecular, Cellular, and Developmental Biology, and Pharmacology Department, Yale University, P O Box 208103, New Haven, CT 06511, USA
    Proc Natl Acad Sci U S A 98:12596-601. 2001
  6. pmc Mifepristone prevents repopulation of ovarian cancer cells escaping cisplatin-paclitaxel therapy
    Carlos D Gamarra-Luques
    Division of Basic Biomedical Sciences, Sanford School of Medicine of the University of South Dakota, 414 East Clark Street, Vermillion, SD, USA
    BMC Cancer 12:200. 2012
  7. pmc Progesterone is essential for maintenance and growth of uterine leiomyoma
    Hiroshi Ishikawa
    Division of Reproductive Biology Research, Northwestern University Feinberg School of Medicine, Department of Obstetrics and Gynecology, 4th Floor, Suite 4 127, 303 East Superior Street, Chicago, Illinois 60611, USA
    Endocrinology 151:2433-42. 2010
  8. ncbi Mifepristone for the treatment of uterine leiomyomas: a randomized controlled trial
    Josep Lluis Carbonell Esteve
    Clinica Mediterrania Medica, Valencia, Spain
    Obstet Gynecol 112:1029-36. 2008
  9. pmc Mifepristone inhibits ovarian cancer cell growth in vitro and in vivo
    Alicia A Goyeneche
    Division of Basic Biomedical Sciences, Sanford School of Medicine, The University of South Dakota, Vermillion, South Dakota 57069, USA
    Clin Cancer Res 13:3370-9. 2007
  10. ncbi Differential localization and activity of the A- and B-forms of the human progesterone receptor using green fluorescent protein chimeras
    C S Lim
    Laboratory of Receptor Biology and Gene Expression, National Cancer Institute, Bethesda, Maryland 20892 5055, USA
    Mol Endocrinol 13:366-75. 1999

Research Grants

Detail Information

Publications340 found, 100 shown here

  1. ncbi Mifepristone, a glucocorticoid receptor antagonist, produces clinical and metabolic benefits in patients with Cushing's syndrome
    Maria Fleseriu
    Northwest Pituitary Center, Department of Medicine, Oregon Health and Science University, Portland, Oregon 97239, USA
    J Clin Endocrinol Metab 97:2039-49. 2012
    ..Cushing's syndrome (CS) is a disorder associated with significant morbidity and mortality due to prolonged exposure to high cortisol concentrations...
  2. ncbi Monocyte chemoattractant protein-1 (CCL-2) integrates mechanical and endocrine signals that mediate term and preterm labor
    Oksana Shynlova
    Samuel Lunenfeld Research Institute, Mount Sinai Hospital, Toronto, Ontario, Canada
    J Immunol 181:1470-9. 2008
    ....
  3. pmc Antiprogestin mifepristone inhibits the growth of cancer cells of reproductive and non-reproductive origin regardless of progesterone receptor expression
    Chelsea R Tieszen
    Division of Basic Biomedical Sciences, Sanford School of Medicine of the University of South Dakota, Vermillion, SD, USA
    BMC Cancer 11:207. 2011
    b>Mifepristone (MF) has been largely used in reproductive medicine due to its capacity to modulate the progesterone receptor (PR)...
  4. ncbi RU486 (mifepristone): mechanisms of action and clinical uses
    F Cadepond
    INSERM U33, , France
    Annu Rev Med 48:129-56. 1997
    RU486 (mifepristone) has proved to be a remarkably active antiprogesterone and antiglucocorticosteroid agent in human beings...
  5. pmc A conditional tissue-specific transgene expression system using inducible GAL4
    T Osterwalder
    Department of Molecular, Cellular, and Developmental Biology, and Pharmacology Department, Yale University, P O Box 208103, New Haven, CT 06511, USA
    Proc Natl Acad Sci U S A 98:12596-601. 2001
    ..that its transcriptional activity within the target tissues depends on the presence of the activator RU486 (mifepristone)...
  6. pmc Mifepristone prevents repopulation of ovarian cancer cells escaping cisplatin-paclitaxel therapy
    Carlos D Gamarra-Luques
    Division of Basic Biomedical Sciences, Sanford School of Medicine of the University of South Dakota, 414 East Clark Street, Vermillion, SD, USA
    BMC Cancer 12:200. 2012
    ..In this work we questioned whether the synthetic steroid mifepristone, which as monotherapy inhibits the growth of ovarian cancer cells, is capable of preventing repopulation of ..
  7. pmc Progesterone is essential for maintenance and growth of uterine leiomyoma
    Hiroshi Ishikawa
    Division of Reproductive Biology Research, Northwestern University Feinberg School of Medicine, Department of Obstetrics and Gynecology, 4th Floor, Suite 4 127, 303 East Superior Street, Chicago, Illinois 60611, USA
    Endocrinology 151:2433-42. 2010
    ..Taken together, our findings define that volume maintenance and growth of human UL are progesterone dependent...
  8. ncbi Mifepristone for the treatment of uterine leiomyomas: a randomized controlled trial
    Josep Lluis Carbonell Esteve
    Clinica Mediterrania Medica, Valencia, Spain
    Obstet Gynecol 112:1029-36. 2008
    To estimate the efficacy of daily administration of 5 mg compared with 10 mg of mifepristone for the treatment of uterine myomas.
  9. pmc Mifepristone inhibits ovarian cancer cell growth in vitro and in vivo
    Alicia A Goyeneche
    Division of Basic Biomedical Sciences, Sanford School of Medicine, The University of South Dakota, Vermillion, South Dakota 57069, USA
    Clin Cancer Res 13:3370-9. 2007
    These studies were designed to determine whether the synthetic steroid mifepristone inhibits ovarian cancer growth in vitro and in vivo and the molecular mechanisms involved.
  10. ncbi Differential localization and activity of the A- and B-forms of the human progesterone receptor using green fluorescent protein chimeras
    C S Lim
    Laboratory of Receptor Biology and Gene Expression, National Cancer Institute, Bethesda, Maryland 20892 5055, USA
    Mol Endocrinol 13:366-75. 1999
    ..The causes for and implications of this differential localization of the A and B forms of the human PR are discussed...
  11. ncbi Low-dose mifepristone in treatment of uterine leiomyoma: a randomised double-blind placebo-controlled clinical trial
    Madhu Bagaria
    Department of Obstetrics and Gynaecology, University College of Medical Sciences, Delhi, India
    Aust N Z J Obstet Gynaecol 49:77-83. 2009
    To evaluate the effect of low-dose mifepristone on leiomyoma-related symptoms, uterine and leiomyoma in women with symptomatic leiomyomata.
  12. ncbi Effect of RU486 on hepatic and adipocyte gene expression improves diabetes control in obesity-type 2 diabetes
    A I Taylor
    The SAAD Centre for Pharmacy and Diabetes, School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Horm Metab Res 41:899-904. 2009
    ..001). These data demonstrate wide-ranging effects of glucocorticoid receptor antagonism on gene expression and metabolism, illustrating the therapeutic potential of specific glucocorticoid receptor antagonists in obesity-related diabetes...
  13. ncbi Clinical utility of progesterone receptor modulators and their effect on the endometrium
    Irving M Spitz
    Institute of Hormone Research and Ben Gurion University of the Negev, Jerusalem, Israel
    Curr Opin Obstet Gynecol 21:318-24. 2009
    In view of the spate of recent publications related to mifepristone and some second generation progesterone receptor modulators (PRMs), this appears to be an opportune time to view the clinical status of these compounds.
  14. ncbi Effects of mifepristone on invasive and metastatic potential of human gastric adenocarcinoma cell line MKN-45 in vitro and in vivo
    Da qiang Li
    State Key Laboratory of Ultrasound Engineering in Medicine, Chongqing Medical University PO Box 153, Chongqing 400016, China
    World J Gastroenterol 10:1726-9. 2004
    To investigate the effects of mifepristone on the invasive and metastatic potential of human gastric adenocarcinoma cell line MKN-45 and its mechanisms.
  15. ncbi The transcriptional response to chronic stress and glucocorticoid receptor blockade in the hippocampal dentate gyrus
    Nicole A Datson
    Division of Medical Pharmacology, Leiden Amsterdam Center for Drug Research, Leiden University Medical Center, Leiden, The Netherlands
    Hippocampus 22:359-71. 2012
    ..studies demonstrated that glucocorticoid receptor (GR) blockade by a brief treatment with the GR antagonist mifepristone (RU486) rapidly reverses the stress and glucocorticoid effects on neurogenesis...
  16. ncbi Advances in medical therapies for Cushing's syndrome
    Nicholas A Tritos
    Neuroendocrine Unit, Massachusetts General Hospital and Harvard Medical School, Boston, Massachusetts 02114, USA
    Discov Med 13:171-9. 2012
    ..b>Mifepristone, a type 2 glucocorticoid receptor antagonist, was recently approved by the FDA as a new therapy for CS...
  17. pmc p38 and p42/44 MAPKs differentially regulate progesterone receptor A and B isoform stabilization
    Junaid A Khan
    Institut National de la Santé et de la Recherche Médicale Unité 693, Universite Paris Sud, Faculte de Medecine Paris Sud, Le Kremlin Bicetre, France
    Mol Endocrinol 25:1710-24. 2011
    ..Imbalance in PRA/PRB ratio frequently associated with carcinogenesis might be a direct consequence of disorders in MAPK signaling that might switch cellular responses to hormonal stimuli and contribute towards pathogenesis...
  18. ncbi The androgen receptor recruits nuclear receptor CoRepressor (N-CoR) in the presence of mifepristone via its N and C termini revealing a novel molecular mechanism for androgen receptor antagonists
    Myles C Hodgson
    Division of Hematology Oncology and Endocrinology, Department of Medicine, Beth Israel Deaconess Medical Center and Harvard Medical School, Boston, Massachusetts 02215, USA
    J Biol Chem 280:6511-9. 2005
    ..as bicalutamide that are currently in use for prostate cancer treatment can also mediate NCoR recruitment, but mifepristone (RU486) at nanomolar concentrations is unique in its ability to markedly enhance the AR-NCoR interaction...
  19. pmc Acute glucocorticoid administration rapidly suppresses basal and stress-induced hypothalamo-pituitary-adrenal axis activity
    Marcus H Andrews
    Henry Wellcome Laboratories for Integrative Neuroscience and Endocrinology, University of Bristol, Bristol BS1 3NY, United Kingdom
    Endocrinology 153:200-11. 2012
    ..Thus, in rats, glucocorticoid receptor activation rapidly suppresses basal and stress-induced HPA activity that operates, at least in part, through a central mechanism of action...
  20. ncbi Improvements in neurocognitive function and mood following adjunctive treatment with mifepristone (RU-486) in bipolar disorder
    Allan H Young
    Stanley Research Centre, School of Neurology, Neurobiology and Psychiatry, University of Newcastle upon Tyne, UK
    Neuropsychopharmacology 29:1538-45. 2004
    ..this hypothesis, 20 bipolar patients were treated with 600 mg/day of the corticosteroid receptor antagonist mifepristone (RU-486) or placebo for 1 week in a double-blind crossover design...
  21. pmc Comparative effectiveness, safety and acceptability of medical abortion at home and in a clinic: a systematic review
    Thoai D Ngo
    Department of Epidemiology and Population Health, London School of Hygiene and Tropical Medicine, England, UK
    Bull World Health Organ 89:360-70. 2011
    ..To compare medical abortion practised at home and in clinics in terms of effectiveness, safety and acceptability...
  22. pmc Transcription factor KLF11 integrates progesterone receptor signaling and proliferation in uterine leiomyoma cells
    Ping Yin
    Division of Reproductive Biology Research, Department of Obstetrics and Gynecology, Feinberg School of Medicine at Northwestern University, Chicago, IL 60611, USA
    Cancer Res 70:1722-30. 2010
    ..Taken together, using a ChIP-cloning approach, we uncovered KLF11 as an integrator of PR signaling and proliferation in uterine leiomyoma cells...
  23. pmc Regulation of bim in glucocorticoid-mediated osteoblast apoptosis
    B Espina
    The Botnar Research Centre, Oxford Institute of Musculoskeletal Sciences, Nuffield Department of Orthopaedic Surgery, Oxford, UK
    J Cell Physiol 215:488-96. 2008
    ..These findings suggest that Bim is a novel regulator of osteoblast apoptosis and may be a therapeutic target...
  24. ncbi Progestin-dependent progression of human breast tumor xenografts: a novel model for evaluating antitumor therapeutics
    Yayun Liang
    Dalton Cardiovascular Research Center, Veterinary Pathobiology, and Department of Biomedical Sciences, University of Missouri, Columbia, Missouri 65211, USA
    Cancer Res 67:9929-36. 2007
    ..Such a model could potentially be used to screen for safer antiprogestins, antiangiogenic agents, or for compounds that reactivate mutant p53 and prevent progestin-dependent progression of breast disease...
  25. pmc Mifepristone in the central nucleus of the amygdala reduces yohimbine stress-induced reinstatement of ethanol-seeking
    Jeffrey A Simms
    Preclinical Development Group, Ernest Gallo Clinic and Research Center at University of California San Francisco, Emeryville, CA 94608, USA
    Neuropsychopharmacology 37:906-18. 2012
    ..The objective of this study was to determine whether mifepristone, a glucocorticoid receptor antagonist, plays a role in ethanol self-administration and reinstatement...
  26. ncbi Cisplatin cytotoxicity is increased by mifepristone in cervical carcinoma: an in vitro and in vivo study
    Rafael Jurado
    Laboratorio de Farmacologia, Subdireccion de Investigacion Basica, Instituto Nacional de Cancerología INCan, Mexico D F, Mexico
    Oncol Rep 22:1237-45. 2009
    We investigated the ability of mifepristone, an anti-progestin drug, to modulate the cytotoxic effect of cisplatin in two cervical cancer cell lines and in human xenograft cervical tumors...
  27. ncbi Antiandrogen effects of mifepristone on coactivator and corepressor interactions with the androgen receptor
    Liang Nian Song
    Department of Oncology, Lombardi Cancer Center, Georgetown University, 3800 Reservoir Road, Northwest, Washington, D C 20057, USA
    Mol Endocrinol 18:70-85. 2004
    b>Mifepristone is a potent antagonist of steroid hormone receptors such as glucocorticoid and progesterone receptors...
  28. ncbi Effect of mifepristone for symptomatic leiomyomata on quality of life and uterine size: a randomized controlled trial
    Kevin Fiscella
    Department of Family Medicine, Obstetrics and Gynecology, School of Medicine and Dentistry, University of Rochester, Rochester, New York 14620, USA
    Obstet Gynecol 108:1381-7. 2006
    To assess the effect of low-dose mifepristone on quality of life, pain, bleeding, and uterine size among women with symptomatic leiomyomata.
  29. ncbi Mifepristone for treatment of uterine leiomyoma. A prospective randomized placebo controlled trial
    M Engman
    Department of Woman and Child Health, Division of Obstetrics and Gynaecology, Karolinska Institutet, Karolinska University Hospital, 171 76 Stockholm, Sweden
    Hum Reprod 24:1870-9. 2009
    ..Uterine leiomyomas are widely prevalent and frequently cause menorrhagia. The major therapeutic option today is hysterectomy. Medical options are of highest interest...
  30. ncbi Brief treatment with the glucocorticoid receptor antagonist mifepristone normalizes the reduction in neurogenesis after chronic stress
    Charlotte A Oomen
    SILS Centre for Neuroscience, University of Amsterdam, Kruislaan 320, 1098 SM, Amsterdam, The Netherlands
    Eur J Neurosci 26:3395-401. 2007
    ..In the present study, we therefore questioned whether glucocorticoid receptor blockade by mifepristone can normalize the effects of chronic stress on adult neurogenesis...
  31. ncbi Mifepristone induced progesterone withdrawal reveals novel regulatory pathways in human endometrium
    R D Catalano
    Department of Pathology, University of Cambridge, Cambridge, UK
    Mol Hum Reprod 13:641-54. 2007
    In women, a single dose of the antiprogestin mifepristone (RU486) in the secretory phase rapidly renders the endometrium unreceptive and is followed by endometrial breakdown and menstruation within 72 h...
  32. ncbi The steroid hormone receptor EcR finely modulates Drosophila lifespan during adulthood in a sex-specific manner
    Herve Tricoire
    Unité BFA EAC 7059, Université Paris Diderot Paris7 CNRS, 4 rue Marie Andrée Lagroua Weill Hallé, Paris, France
    Mech Ageing Dev 130:547-52. 2009
    ..These results reveal a complex adult and sex-specific control of lifespan by steroid signalling in Drosophila...
  33. pmc Preventing local regeneration of glucocorticoids by 11beta-hydroxysteroid dehydrogenase type 1 enhances angiogenesis
    Gary R Small
    Centre for Cardiovascular Science, Queen s Medical Research Institute, University of Edinburgh, Edinburgh EH16 4TJ, Scotland, UK
    Proc Natl Acad Sci U S A 102:12165-70. 2005
    ....
  34. ncbi Corticosterone acutely prolonged N-methyl-d-aspartate receptor-mediated Ca2+ elevation in cultured rat hippocampal neurons
    Taiki Takahashi
    Department of Biophysics and Life Sciences, Graduate School of Arts and Sciences, University of Tokyo at Komaba, Meguro, Tokyo, Japan
    J Neurochem 83:1441-51. 2002
    ..These results imply that high levels of CORT induce a rapid and non-genomic prolongation of NMDA receptor-mediated Ca2+ elevation, probably via putative membrane surface receptors for CORT in the hippocampal neurons...
  35. ncbi Brain aging and Aβ₁₋₄₂ neurotoxicity converge via deterioration in autophagy-lysosomal system: a conditional Drosophila model linking Alzheimer's neurodegeneration with aging
    Daijun Ling
    Department of Neuroscience, Beckman Research Institute of City of Hope, Duarte, CA 91010, USA
    Acta Neuropathol 121:183-91. 2011
    ..A chronic deterioration of the neuronal autophagy-lysosomal system is likely to be a key event in transitioning from normal brain aging to pathological aging leading to Alzheimer's neurodegeneration...
  36. ncbi Dynamics of the action of dFOXO on adult mortality in Drosophila
    Maria E Giannakou
    Centre for Research on Ageing, Department of Biology, University College London, London, UK
    Aging Cell 6:429-38. 2007
    ..The decreased mortality and increased lifespan of dFOXO overexpressing flies was uncoupled from any effect on female fecundity and from expression levels of Drosophila insulin-like peptides in the brain...
  37. ncbi Mifepristone-induced amenorrhoea is associated with an increase in microvessel density and glucocorticoid receptor and a decrease in stromal vascular endothelial growth factor
    Nitish Narvekar
    Contraceptive Development Network, Centre for Reproductive Biology, Edinburgh, UK
    Hum Reprod 21:2312-8. 2006
    We have previously shown that the progesterone antagonist mifepristone is a contraceptive when given in a dose of 2 or 5 mg per day...
  38. ncbi Brief treatment with the glucocorticoid receptor antagonist mifepristone normalises the corticosterone-induced reduction of adult hippocampal neurogenesis
    J L Mayer
    Swammerdam Institute for Life Sciences, Centre for Neuroscience, University of Amsterdam, Amsterdam, The Netherlands
    J Neuroendocrinol 18:629-31. 2006
    The glucocorticoid receptor antagonist mifepristone has been shown to rapidly and effectively ameliorate symptoms of psychotic major depression...
  39. pmc RU486 did not exacerbate cytokine release in mice challenged with LPS nor in db/db mice
    Baichun Yang
    Department of Metabolic Molecular Pharmacology, Research and Development, GlaxoSmithKline, Research Triangle Park, USA
    BMC Pharmacol 8:7. 2008
    ..We investigated the effects of RU486 on serum cytokines in db/db mice and on lipopolysaccharide (LPS)-induced circulating TNFalpha levels in both normal AKR mice and diet-induced obese (DIO) C57BL/6 mice...
  40. ncbi Daily low-dose mifepristone has contraceptive potential by suppressing ovulation and menstruation: a double-blind randomized control trial of 2 and 5 mg per day for 120 days
    Audrey Brown
    Contraceptive Development Network, Centre for Reproductive Biology, University of Edinburgh, Edinburgh, EH3 9ET, United Kingdom
    J Clin Endocrinol Metab 87:63-70. 2002
    ..double-blind randomized trial, we have explored the contraceptive potential of two doses of the P antagonist mifepristone in healthy volunteers in Edinburgh and Shanghai...
  41. pmc Human glucocorticoid receptor beta binds RU-486 and is transcriptionally active
    Laura J Lewis-Tuffin
    Laboratory of Signal Transduciton, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, NC 27709, USA
    Mol Cell Biol 27:2266-82. 2007
    ....
  42. pmc A single-day treatment with mifepristone is sufficient to normalize chronic glucocorticoid induced suppression of hippocampal cell proliferation
    Pu Hu
    Swammerdam Institute for Life Sciences, Center for Neuroscience, University of Amsterdam, Amsterdam, The Netherlands
    PLoS ONE 7:e46224. 2012
    ..Earlier we showed that administration of the glucocorticoid receptor antagonist mifepristone during the final 4 days of a 21 days period of corticosterone treatment fully normalized the number of newborn ..
  43. pmc Mifepristone abrogates repopulation of ovarian cancer cells in between courses of cisplatin treatment
    Elizabeth M Freeburg
    Sanford School of Medicine, The University of South Dakota, Vermillion, SD 57069, USA
    Int J Oncol 34:743-55. 2009
    ..In this study, we tested the hypothesis that mifepristone (MF), a steroid compound with demonstrated growth inhibition activity in ovarian cancer, should be efficacious ..
  44. ncbi Postnatal glucocorticoid excess due to pituitary glucocorticoid receptor deficiency: differential short- and long-term consequences
    Mathias V Schmidt
    Max Planck Institute of Psychiatry, Munich, Germany
    Endocrinology 150:2709-16. 2009
    ..Postnatal glucocorticoid excess results in an altered stress-coping behavior in adult animals, with no effects on anxiety like behavior or cognition...
  45. pmc Blocking mineralocorticoid receptors prior to retrieval reduces contextual fear memory in mice
    Ming Zhou
    Center for Neuroscience, Swammerdam Institute for Life Sciences, University of Amsterdam, Amsterdam, The Netherlands
    PLoS ONE 6:e26220. 2011
    ..We tested here whether blockade of MRs or GRs during retrieval also affects subsequent expression of fear memory...
  46. pmc Progesterone and mifepristone regulate L-type amino acid transporter 2 and 4F2 heavy chain expression in uterine leiomyoma cells
    Xia Luo
    Division of Reproductive Biology Research, Department of Obstetrics and Gynecology, Feinberg School of Medicine, Northwestern University, Chicago, Illinois 60611, USA
    J Clin Endocrinol Metab 94:4533-9. 2009
    ..Until now, little is known about the roles of LAT2/4F2hc in the regulation of the growth of human uterine leiomyoma...
  47. ncbi Mifepristone: pharmacology and clinical impact in reproductive medicine, endocrinology and oncology
    Annie Im
    University of Pittsburgh, Division of Hematology Oncology, Department of Medicine, 5150 Centre Avenue, Pittsburgh, PA 15232, USA
    Expert Opin Pharmacother 11:481-8. 2010
    b>Mifepristone is a synthetic selective progesterone-receptor modulator (SPRM) that is widely used around the globe in the field of reproductive medicine...
  48. pmc Distinguishing features of endometrial pathology after exposure to the progesterone receptor modulator mifepristone
    Julietta Fiscella
    Department of Pathology, School of Medicine and Dentistry, University of Rochester School of Medicine, Rochester, NY 14620, USA
    Hum Pathol 42:947-53. 2011
    There is growing interest in the use of progesterone receptor modulators such as mifepristone for treatment of gynecologic and other conditions, but interest in progesterone receptor modulators is dampened by the effects of the agents on ..
  49. pmc Revealing a steroid receptor ligand as a unique PPARγ agonist
    Shengchen Lin
    State Key Laboratory for Cellular Stress Biology, School of Life Sciences, Xiamen University, Fujian, China
    Cell Res 22:746-56. 2012
    ..Our findings together indicate that steroid compounds may represent an alternative approach for designing non-TZD PPARγ ligands in the treatment of insulin resistance...
  50. pmc A distinct modulating domain in glucocorticoid receptor monomers in the repression of activity of the transcription factor AP-1
    S Heck
    Kernforschungszentrum Karlsruhe, Institut fur Genetik, Germany
    EMBO J 13:4087-95. 1994
    ..While DNA binding and activation of glucocorticoid-regulated promoters require GR dimerization, we present data that suggest that repression is a function of GR monomers...
  51. ncbi Progestin regulation of vascular endothelial growth factor in human breast cancer cells
    S M Hyder
    Department of Integrative Biology, Pharmacology and Physiology, University of Texas Health Sciences Center Houston, 77225, USA
    Cancer Res 58:392-5. 1998
    ....
  52. ncbi Dexamethasone has a central antiemetic mechanism in decerebrated cats
    Chiu Ming Ho
    Department of Anesthesiology, National Defense Medical Center Tri Service General Hospital, Rm 8113, No 161, Sec 6, Minchiuan E Rd, Taipei 114, Taiwan
    Anesth Analg 99:734-9, table of contents. 2004
    ..4, P < 0.05; 0.1 microg, 2.9 +/- 0.9 versus 0.3 +/- 0.5, P < 0.05) induced by xylazine. Pretreatment with mifepristone, a glucocorticoid receptor antagonist, blocked the antiemetic effect of dexamethasone in the bilateral nuclei ..
  53. ncbi Systematic review of mifepristone for the treatment of uterine leiomyomata
    Jody Steinauer
    Department of Obstetrics, Gynecology, and Reproductive Sciences, San Francisco General Hospital, 1001 Potrero Avenue, Ward 6D 14, San Francisco, CA 94110, USA
    Obstet Gynecol 103:1331-6. 2004
    To systematically review the effect of mifepristone on uterine leiomyoma size and symptoms and to summarize its adverse effects.
  54. ncbi Low-dose mifepristone inhibits endometrial proliferation and up-regulates androgen receptor
    Nitish Narvekar
    Contraceptive Development Network, Center for Reproductive Biology, Edinburgh, United Kingdom EH16 4SB
    J Clin Endocrinol Metab 89:2491-7. 2004
    b>Mifepristone in daily low doses has contraceptive potential by inhibiting ovulation. Follicular development is maintained, and although the endometrium is exposed to unopposed estrogen, there are no signs of hyperplasia or atypia...
  55. ncbi A randomized trial to examine the effect of mifepristone on neuropsychological performance and mood in patients with bipolar depression
    Stuart Watson
    Academic Psychiatry, Newcastle University, Newcastle upon Tyne, United Kingdom
    Biol Psychiatry 72:943-9. 2012
    ..We have previously demonstrated a beneficial effect on spatial working memory (SWM) of treatment for 1 week with the progesterone and glucocorticoid receptor antagonist mifepristone, evident 2 weeks after the cessation of treatment.
  56. ncbi Progesterone receptor plays a major antiinflammatory role in human myometrial cells by antagonism of nuclear factor-kappaB activation of cyclooxygenase 2 expression
    Daniel B Hardy
    Department of Biochemistry, The University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Boulevard, Dallas, Texas 75390 9038, USA
    Mol Endocrinol 20:2724-33. 2006
    ..Based on these findings, we propose that PR may inhibit NF-kappaB activation of COX-2 gene expression and uterine contractility via ligand-dependent and ligand-independent mechanisms...
  57. pmc Glucocorticoid receptor and sequential P53 activation by dexamethasone mediates apoptosis and cell cycle arrest of osteoblastic MC3T3-E1 cells
    Hui Li
    Department of Orthopaedic Surgery, Peking Union Medical College Hospital, Chinese Academy of Medical Science and Peking Union Medical College, Beijing, China
    PLoS ONE 7:e37030. 2012
    ..These data demonstrate that proliferation of MC3T3-E1 cell was significantly and directly inhibited by dexamethasone treatment via aberrant GR activation and subsequently P53 activation...
  58. ncbi Mifepristone treatment improves length and quality of survival of mice with spontaneous lung cancer
    Jerome H Check
    The University of Medicine and Dentistry of New Jersey, Robert Wood Johnson Medical School at Camden, Cooper Hospital University Medical Center, Department of Obstetrics and Gynecology, Division of Reproductive Endocrinology and Infertility, Camden, NJ, USA
    Anticancer Res 30:119-22. 2010
    ..b>Mifepristone has not only been shown to down-regulate PIBF expression by human leukemic cell lines but has also been shown ..
  59. ncbi Clinical pharmacokinetics of mifepristone
    O Heikinheimo
    Department of Biomedicine, University of Helsinki, Finland
    Clin Pharmacokinet 33:7-17. 1997
    b>Mifepristone is a steroidal antiprogestin and antiglucocorticoid acting at the receptor level...
  60. ncbi Hormonal regulation and localization of estrogen, progestin and androgen receptors in the endometrium of nonhuman primates: effects of progesterone receptor antagonists
    Ov D Slayden
    Division of Reproductive Sciences, Oregon National Primate Research Center, 505 NW 185th Ave, Beaverton, OR 97006, USA
    Arch Histol Cytol 67:393-409. 2004
    ..This endometrial antiproliferative effect is the basis of the clinical use of PA to control various diseases such as endometriosis...
  61. ncbi Treatment of uterine myoma with 5 or 10mg mifepristone daily during 6 months, post-treatment evolution over 12 months: double-blind randomised clinical trial
    Josep Ll Carbonell Esteve
    Mediterránea Médica Clinic, Valencia, Castello, Valencian Country, Spain
    Eur J Obstet Gynecol Reprod Biol 161:202-8. 2012
    To evaluate the efficacy and safety of 5 and 10mg doses of mifepristone for 6 months for the treatment of uterine fibroids and to check those results at 1 year post-treatment.
  62. pmc Growth inhibition induced by antiprogestins RU-38486, ORG-31710, and CDB-2914 in ovarian cancer cells involves inhibition of cyclin dependent kinase 2
    Alicia A Goyeneche
    Division of Basic Biomedical Sciences, Sanford School of Medicine of the University of South Dakota, Vermillion, SD, USA
    Invest New Drugs 30:967-80. 2012
    ..Our results suggest that, as a consequence of their cytostatic and lethal effects, antiprogestin steroids of well-known contraceptive properties emerge as attractive new agents to be repositioned for ovarian cancer therapeutics...
  63. pmc Mifepristone prevents stress-induced apoptosis in newborn neurons and increases AMPA receptor expression in the dentate gyrus of C57/BL6 mice
    María Llorens-Martín
    CSIC, Madrid, Spain
    PLoS ONE 6:e28376. 2011
    ..Furthermore, we evaluated the effects of the glucocorticoid receptor (GR) antagonist mifepristone on the cell death induced by the Porsolt test...
  64. ncbi The effect of mifepristone on breast cell proliferation in premenopausal women evaluated through fine needle aspiration cytology
    M Engman
    Division of Obstetrics and Gynecology, Department of Woman and Child Health, Karolinska Institutet, Karolinska University Hospital, 171 76 Stockholm, Sweden
    Hum Reprod 23:2072-9. 2008
    Progestins as well as estrogens have a role in breast cell proliferation and the development of breast cancer. Here, the effect of mifepristone on cell proliferation in human breast tissue in vivo was studied in premenopausal women.
  65. ncbi Effects of mifepristone on endometrial receptivity
    Kristina Gemzell Danielsson
    Department of Woman and Child Health, Division for Obstetrics and Gynecology, Karolinska Hospital Institute, Stockholm S 171 76, Sweden
    Steroids 68:1069-75. 2003
    ..The effect of various doses and regimens of mifepristone on endometrial development and markers of receptivity has been studied...
  66. pmc Ligand-specific dynamics of the progesterone receptor in living cells and during chromatin remodeling in vitro
    Geetha V Rayasam
    Laboratory of Receptor Biology and Gene Expression, Building 41, B602, National Cancer Institute, National Institutes of Health, 41 Library Dr, Bethesda, MD 20892 5055, USA
    Mol Cell Biol 25:2406-18. 2005
    ....
  67. ncbi Glucocorticoid-induced skeletal muscle atrophy is associated with upregulation of myostatin gene expression
    Kun Ma
    Division of Endocrinology, Metabolism, and Molecular Medicine, Charles R Drew University of Medicine and Science, Los Angeles, CA 90059, USA
    Am J Physiol Endocrinol Metab 285:E363-71. 2003
    ..We propose that dexamethasone-induced muscle loss is mediated, at least in part, by the upregulation of myostatin expression through a glucocorticoid receptor-mediated pathway...
  68. ncbi Anti-progestins suppress the growth of established tumors induced by 7,12-dimethylbenz(a)anthracene: comparison between RU486 and a new 21-substituted-19-nor-progestin
    Ronald D Wiehle
    Repros Therapeutics Inc, The Woodlands, TX 77380, USA
    Oncol Rep 18:167-74. 2007
    ..These results indicate that anti-progestins should be developed for the chemoprevention and treatment of hormone-responsive breast cancer...
  69. ncbi Effect of low-dose mifepristone administration on day 2 after ovulation on transcript profiles in implantation-stage endometrium of rhesus monkeys
    D Ghosh
    Department of Physiology, All India Institute of Medical Sciences, New Delhi, India
    Reproduction 138:357-70. 2009
    ..effect, we have compared transcript profiles for 409 known genes between control receptive stage (n=13), and mifepristone-induced desynchronized and non-receptive stage (n=12) monkey endometrial samples collected on days 4 (n=12) and ..
  70. ncbi Arousal and stress effects on consolidation and reconsolidation of recognition memory
    Mouna Maroun
    Department of Neurobiology and Etiology, The Brain and Behavior Research Center, University of Haifa, Haifa, Israel
    Neuropsychopharmacology 33:394-405. 2008
    ....
  71. ncbi Dexamethasone inhibits proliferation of adult hippocampal neurogenesis in vivo and in vitro
    Jong Bin Kim
    Department of Biochemistry, Hanyang University College of Medicine, 17 Haengdang dong, Sungdong gu, Seoul 133 791, Republic of Korea
    Brain Res 1027:1-10. 2004
    ..Taken these in vitro and in vivo results together, it is concluded that glucocorticoid receptor activation blocks only proliferation, but not differentiation, in hippocampal neurogenesis...
  72. ncbi Neuroprotective effect of mifepristone involves neuron depolarization
    A M Ghoumari
    INSERM UMR788 and University Paris XI, Bicetre, France
    FASEB J 20:1377-86. 2006
    ..the mechanism of this developmental apoptosis, we took advantage of its inhibition by the steroid analog mifepristone. This effect did not involve the classical steroid nuclear receptors...
  73. ncbi Medical abortion in early pregnancy: experience in China
    Linan Cheng
    Shanghai Institute of Family Planning Technical Instruction, International Peace Maternity and Child Health Hospital, China Welfare Institute, Shanghai 200030, People s Republic of China
    Contraception 74:61-5. 2006
    ..b>Mifepristone is now produced in three companies in China and is commonly used with PGs for medical abortion.
  74. pmc Mapracorat, a novel selective glucocorticoid receptor agonist, inhibits hyperosmolar-induced cytokine release and MAPK pathways in human corneal epithelial cells
    Megan E Cavet
    Pharmaceutical R and D, Bausch and Lomb, Inc, Rochester, NY 14609, USA
    Mol Vis 16:1791-800. 2010
    ..This study assessed the anti-inflammatory effects of mapracorat in an in vitro osmotic stress model which mimics some of the pathophysiological changes seen in dry eye...
  75. pmc A screen of apoptosis and senescence regulatory genes for life span effects when over-expressed in Drosophila
    Jie Shen
    Molecular and Computational Biology Program, Department of Biological Sciences, University of Southern California, Los Angeles, CA 90089, USA
    Aging (Albany NY) 1:191-211. 2009
    ..expression of transgenes in Drosophila was produced using the Geneswitch system, wherein feeding the drug RU486/Mifepristone activates the artificial transcription factor Geneswitch...
  76. ncbi Successful long-term treatment of refractory Cushing's disease with high-dose mifepristone (RU 486)
    J W Chu
    Department of Medicine, Stanford University School of Medicine, Stanford, California 94305, USA
    J Clin Endocrinol Metab 86:3568-73. 2001
    ..surgical, medical, and radiotherapeutic approaches, he responded dramatically to high-dose long-term mifepristone therapy (up to 25 mg/kg x d)...
  77. pmc Pathways involved in gut mucosal barrier dysfunction induced in adult rats by maternal deprivation: corticotrophin-releasing factor and nerve growth factor interplay
    Frederick Barreau
    Neuro Gastroenterology and Nutrition Unit, INRA, 180 chemin de Tournefeuille, BP 3, 31931 Toulouse Cedex 9, France
    J Physiol 580:347-56. 2007
    ..At 12 weeks of age, adult rats were treated with mifepristone (an antagonist of corticoid receptors), alpha-helical CRF((9-41)) (a non-specific CRF receptor antagonist), or ..
  78. ncbi Low-dose mifepristone for uterine leiomyomata
    Steven H Eisinger
    Department of Family Medicine, School of Medicine, University of Rochester, Rochester, New York, USA
    Obstet Gynecol 101:243-50. 2003
    To compare the effect of 5 and 10 mg of mifepristone on uterine leiomyoma size and symptoms, and to measure side effects.
  79. ncbi The glucocorticoid agonist activities of mifepristone (RU486) and progesterone are dependent on glucocorticoid receptor levels but not on EC50 values
    Shimin Zhang
    Division of Molecular Pathobiology, Department of Environmental and Infectious Disease Sciences, American Registry of Pathology, Armed Forces Institute of Pathology, Washington, DC 20306, USA
    Steroids 72:600-8. 2007
    b>Mifepristone is an antagonist of the glucocorticoid receptor (GR) that also has significant agonist activity in some cell types...
  80. ncbi Preterm and term cervical ripening in CD1 Mice (Mus musculus): similar or divergent molecular mechanisms?
    Juan M Gonzalez
    Maternal and Child Health Research Program, Department of Obstetrics and Gynecology, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    Biol Reprod 81:1226-32. 2009
    ..Our results indicate that the molecular mechanisms governing preterm and term cervical ripening are distinctly different...
  81. ncbi Mifepristone (RU486): a review
    D K Mahajan
    Department of Obstetrics and Gynecology, Louisiana State University School of Medicine, Shreveport 71130, USA
    Fertil Steril 68:967-76. 1997
    To review the literature concerning the mechanism of action and pharmacodynamics of mifepristone (RU486), potential new uses of RU486, and its current use not only as an abortifacient but also as therapy for endometriosis, leiomyoma, ..
  82. ncbi Corticosterone reduces dendritic complexity in developing hippocampal CA1 neurons
    Deborah N Alfarez
    Swammerdam Institute for Life Sciences, Center for Neuroscience, Universiteit van Amsterdam, Amsterdam, The Netherlands
    Hippocampus 19:828-36. 2009
    ..These findings suggest that it is relevant to maintain plasma corticosterone levels low during hippocampal development...
  83. ncbi Induction of antiproliferation and apoptosis in estrogen receptor negative MDA-231 human breast cancer cells by mifepristone and 4-hydroxytamoxifen combination therapy: a role for TGFbeta1
    Yayun Liang
    Department of Surgery, Medical College of Georgia, Augusta, GA, USA
    Int J Oncol 23:369-80. 2003
    b>Mifepristone (MIF) is an antiprogestin with potent anti-glucocorticoid and anti-androgen activity. MIF also appears to have anti-tumor activity independent of its ability to bind to nuclear receptors...
  84. ncbi Mifepristone-misoprostol abortion: a trial in rural and urban Maharashtra, India
    Kurus Coyaji
    K E M Hospital, Pune, India
    Contraception 66:33-40. 2002
    ..the use of medical abortion in developing countries, we investigated the safety, efficacy, and acceptability of mifepristone-misoprostol abortion in the outpatient family planning departments of two urban hospitals and one rural ..
  85. ncbi Antiviral effects of mifepristone on human immunodeficiency virus type-1 (HIV-1): targeting Vpr and its cellular partner, the glucocorticoid receptor (GR)
    Elizabeth A Schafer
    Department of Infectious Diseases and Microbiology, University of Pittsburgh, Graduate School of Public Health, 130 DeSoto Street, Pittsburgh, PA 15261, USA
    Antiviral Res 72:224-32. 2006
    ..the HIV-1 LTR through glucocorticoid response element (GRE), an event that can be blocked by the GR antagonist, mifepristone. Results demonstrated that Vpr-induced transactivation of the HIV-1 LTR was inhibited by mifepristone in a dose-..
  86. ncbi Effect of long-term treatment with low-dose mifepristone on the endometrium
    D T Baird
    Contraceptive Development Network, Centre for Reproductive Biology, University of Edinburgh, Academic Centre, 49 Little France Crescent, Old Dalkeith Road, Edinburgh EH16 4SB, UK
    Hum Reprod 18:61-8. 2003
    b>Mifepristone in low daily doses has contraceptive potential by inhibiting ovulation and menstruation. Because follicular development is maintained, the endometrium is exposed to estrogen for prolonged periods unopposed by progesterone.
  87. ncbi Glucocorticoids inhibit developmental stage-specific osteoblast cell cycle. Dissociation of cyclin A-cyclin-dependent kinase 2 from E2F4-p130 complexes
    E Smith
    Department of Orthopaedic Surgery, Institute for Genetic Medicine, University of Southern California Keck School of Medicine, Los Angeles, California 90033, USA
    J Biol Chem 275:19992-20001. 2000
    ..Thus, glucocorticoids induce premature attenuation of the osteoblast cell cycle, possibly contributing to the osteoporosis induced by these drugs in vivo...
  88. ncbi Mifepristone treatment of olanzapine-induced weight gain in healthy men
    Coleman Gross
    Corcept Therapeutics, Menlo Park, CA 94025, USA
    Adv Ther 26:959-69. 2009
    ..The objective of this study was to determine if mifepristone, a glucocorticoid receptor antagonist, could prevent olanzapine-induced weight gain.
  89. ncbi Differential response of progesterone receptor isoforms in hormone-dependent and -independent facilitation of female sexual receptivity
    Shaila K Mani
    Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, Texas 77030, USA
    Mol Endocrinol 20:1322-32. 2006
    ..The data reveal the selective contributions of individual isoforms to the signaling pathways mediating female reproductive behavior...
  90. ncbi Menstrual-like changes in mice are provoked through the pharmacologic withdrawal of progesterone using mifepristone following induction of decidualization
    X B Xu
    Department of Cell Biology, National Research Institute for Family Planning, Beijing 100081, People s Republic of China
    Hum Reprod 22:3184-91. 2007
    ..Since progesterone action ablated pharmacologically may provide more insight into the mechanism of action, a mouse menstruation model using mifepristone was established.
  91. pmc Mifepristone (RU486) protects Purkinje cells from cell death in organotypic slice cultures of postnatal rat and mouse cerebellum
    A M Ghoumari
    Institut National de la Santé et de la Recherche Médicale U488, Batiment Gregory Pincus, 80 rue du General Leclerc, 94276 Kremlin Bicêtre, France
    Proc Natl Acad Sci U S A 100:7953-8. 2003
    b>Mifepristone (RU486), which binds with high affinity to both progesterone and glucocorticosteroid receptors (PR and GR), is well known for its use in the termination of unwanted pregnancy, but other activities including neuroprotection ..
  92. ncbi ABCA1 redistributes membrane cholesterol independent of apolipoprotein interactions
    Ashley M Vaughan
    Department of Medicine, University of Washington, Seattle, WA 98195 6426, USA
    J Lipid Res 44:1373-80. 2003
    ..These studies show that ABCA1 redistributes cholesterol to cell-surface domains, where it becomes accessible for removal by apolipoproteins, consistent with a direct role of ABCA1 in cholesterol transport...
  93. ncbi A phase II study of mifepristone (RU-486) in castration-resistant prostate cancer, with a correlative assessment of androgen-related hormones
    Mary Ellen Taplin
    Dana Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA
    BJU Int 101:1084-9. 2008
    To evaluate mifepristone (RU-486) in patients with castration-resistant prostate cancer (CRPC), with a correlative assessment of serum androgens and androgen metabolites
  94. ncbi Mifepristone (RU 486) in Cushing's syndrome
    Sarah Johanssen
    Endocrine and Diabetes Unit, Department of Internal Medicine I, University of Wuerzburg, Josef Schneider Street 2, 97080 Wuerzburg, Germany
    Eur J Endocrinol 157:561-9. 2007
    b>Mifepristone (RU 486) blocks the action of cortisol by binding to the glucocorticoid receptor and, therefore, is of potential therapeutic value in Cushing's syndrome...
  95. ncbi Mifepristone: where do we come from and where are we going? Clinical development over a quarter of a century
    Irving M Spitz
    Institute of Hormone Research and Ben Gurion University of the Negev, Jerusalem 92548, Israel
    Contraception 82:442-52. 2010
    Administration of mifepristone followed by the prostaglandin, misoprostol, has been used successfully in the medical termination of pregnancy for over 25 years, and the method is registered in 35 countries...
  96. pmc Mifepristone decreases depression-like behavior and modulates neuroendocrine and central hypothalamic-pituitary-adrenocortical axis responsiveness to stress
    Aynara C Wulsin
    Department of Psychiatry, University of Cincinnati, College of Medicine, Cincinnati, OH 45267, USA
    Psychoneuroendocrinology 35:1100-12. 2010
    ..The current study was designed to test the efficacy of mifepristone, a GR antagonist, in mitigating behavioral, neuroendocrine and central nervous system (CNS) responses to an ..
  97. ncbi Reversal of antiprogestin resistance and progesterone receptor isoform ratio in acquired resistant mammary carcinomas
    Victoria Wargon
    Laboratory of Hormonal Carcinogenesis, Institute of Experimental Biology and Medicine National Research Council of Argentina CONICET, Obligado 2490, 1428 Buenos Aires, Argentina
    Breast Cancer Res Treat 116:449-60. 2009
    ....
  98. ncbi Selective transcriptional regulation of aromatase gene by vitamin D, dexamethasone, and mifepristone in human glioma cells
    Josue G Yague
    Instituto Cajal, CSIC, Avenida Doctor Arce 37, 28002 Madrid, Spain
    Endocrine 35:252-61. 2009
    ..We assessed whether vitamin D, dexamethasone, and the glucocorticoid receptor antagonist mifepristone regulate the aromatase gene in human glioma, neuroblastoma, and breast cancer cells...
  99. ncbi Vaginal misoprostol administered 1, 2, or 3 days after mifepristone for early medical abortion: A randomized trial
    E A Schaff
    Reproductive Health Program, Department of Family Medicine, University of Rochester School of Medicine, 1000 South Ave, Box 101, Rochester, NY 14620, USA
    JAMA 284:1948-53. 2000
    The conventional timing of misoprostol administration after mifepristone for medical abortion is 2 days, but more flexible intervals, which may make the regimen more convenient, have not been studied.
  100. ncbi [Effects of mifepristone on expression of estrogen receptor and progesterone receptor in cultured human eutopic and ectopic endometria]
    J Jiang
    Department of Obstetrics and Gynecology, Second Hospital of Hebei Medical University, Shijiazhuang 050000, China
    Zhonghua Fu Chan Ke Za Zhi 36:218-21. 2001
    OBJECTIVE: To investigate the effects of mifepristone on expression of estrogen receptor (ER) and progesterone receptor (PR) in cultured human eutopic and ectopic endometria...
  101. ncbi Mifepristone treatment improves length and quality of survival of mice with spontaneous leukemia
    Jerome H Check
    Department of Obstetrics and Gynecology, The University of Medicine and Dentistry of New Jersey, Robert Wood Johnson Medical School at Camden, Cooper Hospital University Medical Center, Camden, New Jersey, USA
    Anticancer Res 29:2977-80. 2009
    b>Mifepristone was found to suppress expression of the progesterone-induced blocking factor (PIBF). Progesterone-induced blocking factor suppresses natural killer cell activity...

Research Grants63

  1. Mifepristone for Prevention of Breakthrough Bleeding
    John Jain; Fiscal Year: 2004
    ..b>Mifepristone is a competitive progesterone receptor antagonist...
  2. Chronic Nicotine's Activation of the HPA Axis
    Theodore Friedman; Fiscal Year: 2005
    ..abstract_text> ..
  3. Suppression of Breakthrough Bleeding in LNG-IUS Users
    Ov Slayden; Fiscal Year: 2006
    ..using subcutaneous Norplant contraception, BTB can be suppressed by intermittent antiprogestin therapy with mifepristone. NICHD has a new antiprogestin, CDB-2914, that is more potent than mifepristone...
  4. Individual differences in anxiety in females
    Mohamed Kabbaj; Fiscal Year: 2006
    ..Male rats will be used as positive controls. ..
  5. Ethanol Regulation of Serum Glucocorticoid Kinase I
    BLAIR N COSTIN; Fiscal Year: 2012
    ..The work proposed here could shed light on molecular mechanisms underlying alcoholism and eventually have implications in the development of novel pharmacological agents for alcoholism or alcohol-related neurological disorders. ..
  6. Endocrine Targets for Prevention of Lung Cancer
    Robert M Bigsby; Fiscal Year: 2012
    ..On the other hand, using the antiprogestin, mifepristone, we will determine the role of PR in tumor progression...
  7. Glucocorticoids, Stress and Blood Pressure Regulation
    Deborah A Scheuer; Fiscal Year: 2013
    ..The pellets will be composed of the following steroids: Cort, Mifepristone (a GR receptor antagonist), eplerenone (an MR receptor antagonist) and/or cholesterol...
  8. BRCA1 and progesterone receptors in breast cancer
    Eva Y Lee; Fiscal Year: 2013
    ..Consistently, treatment of these mice with the anti-progesterone, mifepristone (RU486), significantly delays or prevents mammary tumorigenesis...
  9. Novel Therapeutics in PTSD: A Randomized Clinical Trial of Mifepristone
    Gerardo Villarreal; Fiscal Year: 2013
    ..manipulation of the body's major stress system (the hypothalamic-pituitary-adrenal (HPA) axis) with mifepristone. At high doses mifepristone is a glucocorticoid receptor (GR) antagonist with peripheral and central nervous ..
  10. GCs, CRF and Stressor-Induced Relapse
    John R Mantsch; Fiscal Year: 2013
    ..The ability of a rat model of excessive drug use to enhance CRF regulation of drug-seeking behavior in a manner that depends on secretion of glucocorticoid hormones will be tested. ..
  11. Antiprogestin therapy for ovarian cancer
    CARLOS MARCELO TELLERIA; Fiscal Year: 2012
    ..Our laboratory demonstrated that single therapy with the prototypical antiprogestin mifepristone inhibits growth of ovarian cancer cells in vitro as well as in a preclinical in vivo animal model of ovarian ..
  12. MOLECULAR MECHANISM OF LEIOMYOMA GROWTH AND REGRESSION
    GREGORY SCOTT SCHULTZ; Fiscal Year: 2011
    ..This proposal will investigate how fibroids are developed and grow, and ways to prevent them, including their symptoms. ..
  13. Role of misoprostol in Clostridium sordellii endometritis in a rodent model
    David M Aronoff; Fiscal Year: 2012
    DESCRIPTION (provided by applicant): The combination oral regimen of mifepristone (MFP;also known as RU-486) and misoprostol was FDA approved in 2000 to induce abortion medically...
  14. Extra / Intra-cellular Signaling in Novel 3-Dimensional Human Leiomyoma Cultures
    WILLIAM HENRY CATHERINO; Fiscal Year: 2013
    ..One such medical therapy, mifepristone, decreases tumor size, although the mechanism is unclear...
  15. Mifepristone Treatment for Cocaine Dependence
    WILFRED NOEL RABY; Fiscal Year: 2013
    ..Its goal is to test if mifepristone, a central and peripheral glucocorticoid receptor (GR) antagonist, can decrease relapse to cocaine use and ..
  16. Growth Inhibition Induced by Mifepristone in Ovarian Cancer
    Carlos Telleria; Fiscal Year: 2009
    ..goal of this application is to study the feasibility of using the prototypical progesterone receptor modulator mifepristone, also known as "RU486," for ovarian cancer therapeutics...
  17. Comparative Effectiveness of Pregnancy Failure Management Regimens (Pre-Fai-R)
    Courtney A Schreiber; Fiscal Year: 2013
    ..b>Mifepristone, a competitive progesterone and glucocorticoid receptor antagonist, blocks the cellular effects of progesterone ..
  18. Hormonal Regulation of the Cervix During Pregnancy
    ORRIN SHERWOOD; Fiscal Year: 2006
    ..Treatment with RU 486 alone and in combination with exogenous relaxin will be done at term with relaxin-deficient rats. ..
  19. ANTIPROGESTINS IN ENDOMETRIUM
    RONALD WIEHLE; Fiscal Year: 2000
    ..Such compounds could fill Zonagen's developmental pipeline with drugs for those diseases and, potentially, other indications. ..
  20. NEUROENDOCRINE CONTROL OF ANTERIOR PITUITARY HORMONES
    RHONDA KINEMAN; Fiscal Year: 2006
    ..The current application centers on the interrelationship between changes in metabolic function and the GH axis. ..
  21. MYOMETRIAL GAP JUNCTION MODULATION IN PRETERM LABOR
    WILLIAM LARSEN; Fiscal Year: 1990
    ..Data obtained in these studies should provide a fundamental basis for the development of new preventative therapies and risk assessment for preterm labor...
  22. SPECIALIZED CENTER OF RESEARCH IN HEART FAILURE
    Douglas Mann; Fiscal Year: 2004
    ..These studies elucidate further the molecular foundations of cardiac hypertrophy and failure and should provide a rational basis for more effective therapy. ..
  23. Antiprogestins in Cynomolgus Endometriosis
    RONALD WIEHLE; Fiscal Year: 2003
    ..The tertiary outcome parameters will be the assessment of the impact of our compound on inflammation markers, on cycling and on liver function. ..
  24. ANTIPROGESTINS AND ACTIVE CELL DEATH IN BREAST CANCER
    M El Etreby; Fiscal Year: 2001
    ..an additive antitumor activity and to clarify the intracellular mechanism of action of the antiprogestin mifepristone, and the antiestrogen tamoxifen, in inhibition of growth of established tumors (chemotherapy) and in prevention ..
  25. TSH SECRETION--ROLE OF GLUCOCORTICOIDS
    Mary Samuels; Fiscal Year: 1999
    ..2) Administration of mifepristone. Healthy subjects will receive mifepristone, a competitive glucocorticoid antagonist, which will permit a ..
  26. CSF-1R EXPRESSION IN HUMAN BREAST CARCINOMA
    BARRY KACINSKI; Fiscal Year: 2000
    ..They also propose to determine whether glucocorticoids and their antagonists modulate the expression of CSF-1R in human breast carcinoma specimens maintained ex vivo in short-term organ culture and in vivo in nude mice. ..
  27. HTS for Androgen Receptor Antagonists that Recruit NCoR
    Steven Balk; Fiscal Year: 2006
    ..AR can interact with co-repressor proteins, including NCoR and SMRT, and that this interaction is enhanced by mifepristone (RU486), demonstrating that drug induced conformational changes in the AR can enhance co-repressor recruitment...
  28. Steroid As Cytoprotectants against Oxidative Toxicity
    Qin Chen; Fiscal Year: 2007
    ..The glucocorticoid receptor antagonist mifepristone prevented CT from inducing a cell survival response...
  29. Collagen-binding proteins in softening of uterine cervix
    Robert Kokenyesi; Fiscal Year: 2003
    ..in cervical softening will be tested by the induction of preterm delivery with the antiprogesterone agent Mifepristone (RU-486)...
  30. Control of menstrual bleeding disturbances in women
    Ian Fraser; Fiscal Year: 2006
    ..There is preliminary evidence that a short course of an antiprogesterone (Mifepristone) may also stabilize the endometrium, and it is postulated that a combination of an antiprogesterone with ..
  31. PHYSIOLOGIC BASIS OF FA GENE RECESSIVITY
    GARY TRUETT; Fiscal Year: 1999
    ..2) fa genotype effects can be altered from recessive to codominant by blocking the glucocorticoid receptor with mifepristone early in life from day 8- 16 of life, B...
  32. Breast Tumor Inhibition by Antiprogestins
    RONALD WIEHLE; Fiscal Year: 2002
    ..New antiprogestins discovered by NICHD and realized as drugs through this proposed SBIR, satisfy the need to bring the results of government-sponsored science into the public domain. ..
  33. HYPOGLYCEMIA AND AUTONOMIC NERVOUS SYSTEM FUNCTION
    Roy Freeman; Fiscal Year: 2007
    ..In addition, we will determine whether administration of a glucocorticoid receptor antagonist, mifepristone, prior to antecedent hypoglycemia improves the autonomic and neuroendocrine response to subsequent hypoglycemia ..
  34. TARGETED OVEREXPRESSION OF PTH-RELATED PEPTIDE
    ARTHUR BROADUS; Fiscal Year: 2007
    ..This aim too is based on preliminary evidence of such an effect in vitro. The model to be created will be a collagen gene-driven Cre under the control of PR1 (RU-486). ..
  35. METABOLIC CONSEQUENCES OF ANTIRETROVIRAL THERAPY
    DAVID WEIGLE; Fiscal Year: 2003
    ..Future trials of these medications, along with a great deal more basic research, are clearly justified by the increasing and sustained use of HAART to deal with the worldwide epidemic of HIV infection. ..
  36. CALCIUM AND SALT INTAKE
    MICHAEL TORDOFF; Fiscal Year: 1999
    ..For each model, corticosterone and/or RU-486 (a corticosterone antagonist) will be given and several behavioral and physiological parameters assessed. ..
  37. IMMUNOLOGIC PROBES FOR STUDY OF PROGESTERONE RECEPTOR
    Dean Edwards; Fiscal Year: 1991
    ..The overall goal of this proposal is to attempt to relate specific structural features of steroid receptors that might be responsible for regulating functional activities...
  38. ATF3 in Beta cell signaling, expression & destruction
    Tsonwin Hai; Fiscal Year: 2006
    ..The mifepristone-inducible system will be used to generate transgenic mice expressing ATF3 in the islets in an inducible manner...
  39. Steroid resistance: Experimental Autoimmune Encephalomyelitis/Multiple Sclerosis
    Thomas G Forsthuber; Fiscal Year: 2010
    ..Furthermore, EAE is substantially exacerbated in MIF-/- mice treated with the glucocorticoid receptor inhibitor Mifepristone (RU-486)...
  40. MYOCARDIAL PROTEIN SYNTHESIS AFTER ALCOHOL INTOXICATION
    Charles H Lang; Fiscal Year: 2010
    ..Overall, the research design will establish the mechanism by which myocardial protein synthesis is reduced in response to alcohol abuse. ..
  41. Antiretroviral-Induced Defects in Muscle Protein Synthesis
    Charles H Lang; Fiscal Year: 2010
    ..Such data is needed to both realize the full potential and avoid possible pitfalls of this drug in the long-term treatment of HIV-infected individuals. ..
  42. Myocardial Protein Synthesis After Thermal Injury
    Charles Lang; Fiscal Year: 2005
    ..Overall, the research will elucidate the mechanisms by which myocardial protein synthesis is reduced after thermal injury, leading to the better understanding and treatment of the resulting cardiomyopathy. - ..
  43. Progesterone regulation of human luteal cell viability
    John Peluso; Fiscal Year: 2006
    ..Such selective manipulation of the P4's actions could have far reaching effects on the treatment for infertility, contraception and certain types of cancers. [unreadable] [unreadable]..
  44. Protein Kinase G Regulation of Granulosa Cell Viability
    John Peluso; Fiscal Year: 2006
    ..We now propose to test this hypothesis using biochemical, genetic, imaging and cell biological techniques. [unreadable] [unreadable]..
  45. The effect of nonoxynol-9 on human endometrium
    John Jain; Fiscal Year: 2005
    ..The results of this study will provide important preliminary information on the role of microbicides on endometrial toxicity and may help guide future research priorities. ..
  46. RCT of a Novel Oral Contraceptive Initiation Method
    Carolyn Westhoff; Fiscal Year: 2004
    ..We will also assess dual method use for STD prevention in the study to adoption of and adherence to oral contraceptives. We will also assess dual method use for STD prevention in the study population. ..
  47. Regulation of Oocyte Viability by Granulosa Cell Contact
    John Peluso; Fiscal Year: 2004
    ..abstract_text> ..
  48. MECHANISMS OF REPRODUCTIVE AGING
    Darrell Brann; Fiscal Year: 2004
    ..As a whole, the proposed studies will provide important insights as to why glutamate signaling is compromised in the hypothalamus of the middle-aged rat, and will advance our understanding of reproductive aging. ..
  49. Obesity, Oral Contraception and Ovarian Suppression
    Carolyn Westhoff; Fiscal Year: 2007
    ..This study will have very good power to detect clinically important differences. Results could directly and immediately affect contraceptive practice. ..
  50. ASTROCYTE-NEURON INTERACTIONS AND GNRH NEURONAL FUNCTION
    Darrell Brann; Fiscal Year: 2005
    ....
  51. NEUROENDOCRINE REGULATION OF BEHAVIOR
    JEFFREY BLAUSTEIN; Fiscal Year: 2006
    ....
  52. Pharmacotherapy for Minor Depression
    Robert Howland; Fiscal Year: 2004
    ..The results of this study will have profound public health implications by improving our understanding of the efficacy of SJW and standard antidepressants for the treatment of MinorD. ..
  53. LONG-TERM LORAZEPAM USE AND ACUTE TOXICITY IN THE AGED
    Nunzio Pomara; Fiscal Year: 2005
    ..index of brain white matter organization) contribute most strongly to the acute effects of lorazepam on cognitive/motor performance or postural sway in elderly individuals receiving long-term lorazepam treatment for GAD? ..
  54. Low birth weight, uterine infection, and nitric oxide
    Chandrasekhar Yallampalli; Fiscal Year: 2007
    ..2 will test the hypothesis that NO donor can reverse the increases in DAF expression in uteroplacental and vascular tissues and in fetal growth restriction ..
  55. Estrogen receptor activation in the CNS
    JEFFREY BLAUSTEIN; Fiscal Year: 2005
    ..This initial research is essential for future work on the molecular consequences of ligand independent activation of ERs in the brain of males and females, which can then be studied in an unprecedented way. ..
  56. Northeast Under/Grad Research Organization for Neuroscience
    Cheryl Frye; Fiscal Year: 2008
    ..Both of these outcomes are congruous with the Public Health Service's mission to ensure that there is a resource of well-trained scientists and health-care providers in the United States. [unreadable] [unreadable] [unreadable]..
  57. Arginine and Ovine Model for Fetal Growth Restriction
    Guoyao Wu; Fiscal Year: 2007
    ..This will ultimately promote favorable pregnancy outcomes while saving billions of healthcare dollars in the U.S. and worldwide. [unreadable] [unreadable] [unreadable]..
  58. Do Reporting Biases Mitigate Disparity Estimates?
    Kevin Fiscella; Fiscal Year: 2004
    ..abstract_text> ..
  59. Progestin Regulation of VEGF in Breast Cancer Cells
    SALMAN HYDER; Fiscal Year: 2005
    ..abstract_text> ..
  60. Podocyte Protein Alterations Induced by Glucocorticoids
    Richard Ransom; Fiscal Year: 2005
    ..Identification of a potential mechanism for glucocorticoid action in the treatment of NS would permit the development of more highly targeted and less toxic therapies for this very common form of kidney disease. ..
  61. SYMPATHETIC NEURAL FUNCTION AND GLUCOCORTICOIDS
    DEBORAH SCHEUER; Fiscal Year: 2001
    ..The results will provide fundamental new knowledge of the mechanisms of glucocorticoid-mediated modulation of arterial pressure regulation. ..
  62. Simplified Tai Chi for Reducing Fibromyalgia Pain
    CHRISTY SHERMAN; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..