estrone

Summary

Summary: An aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from ANDROSTENEDIONE directly, or from TESTOSTERONE via ESTRADIOL. In humans, it is produced primarily by the cyclic ovaries, PLACENTA, and the ADIPOSE TISSUE of men and postmenopausal women.

Top Publications

  1. pmc Kidney-targeted Birt-Hogg-Dube gene inactivation in a mouse model: Erk1/2 and Akt-mTOR activation, cell hyperproliferation, and polycystic kidneys
    Masaya Baba
    Urologic Oncology Branch, National Cancer Institute Frederick, Frederick, MD 21702, USA
    J Natl Cancer Inst 100:140-54. 2008
  2. ncbi Predicted-no-effect concentrations for the steroid estrogens estrone, 17β-estradiol, estriol, and 17α-ethinylestradiol
    Daniel J Caldwell
    Johnson and Johnson, New Brunswick, New Jersey, USA
    Environ Toxicol Chem 31:1396-406. 2012
  3. ncbi Association of CYP1A1 polymorphisms with differential metabolic activation of 17beta-estradiol and estrone
    Pyotr Kisselev
    Institute of Clinical Pharmacology, Charite Campus Mitte, University Medicine Berlin, Berlin, Germany
    Cancer Res 65:2972-8. 2005
  4. ncbi Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver
    G A Kullak-Ublick
    Division of Clinical Pharmacology and Toxicology, Department of Medicine, University Hospital, Zurich, Switzerland
    Gastroenterology 120:525-33. 2001
  5. ncbi Polymorphisms associated with circulating sex hormone levels in postmenopausal women
    Alison M Dunning
    Cancer Research UK, Department of Oncology, University of Cambridge, Strangeways Research Laboratory, Cambridge, UK
    J Natl Cancer Inst 96:936-45. 2004
  6. ncbi Endometrial and myometrial secretion of androgens and estrone during early pregnancy and luteolysis in pigs
    Anita Franczak
    Department of Animal Physiology, University of Warmia and Mazury in Olsztyn, Oczapowski 1A, 10 718 Olsztyn, Poland
    Reprod Biol 8:213-28. 2008
  7. ncbi Effects of estrone on N-methyl-D-aspartic acid- and staurosporine-induced changes in caspase-3-like protease activity and lactate dehydrogenase-release: time- and tissue-dependent effects in neuronal primary cultures
    M Kajta
    Department of Endocrinology, Institute of Pharmacology, Polish Academy of Sciences, Smetna 12, 31 343 Krakow, Poland
    Neuroscience 123:515-26. 2004
  8. ncbi 17β-Estradiol, but not estrone, increases the survival and activation of new neurons in the hippocampus in response to spatial memory in adult female rats
    Robyn E S McClure
    Department of Psychology, Graduate Program in Neuroscience, Brain Research Centre, University of British Columbia, Vancouver, BC, Canada
    Horm Behav 63:144-57. 2013
  9. ncbi Docking, synthesis, and in vitro evaluation of antimitotic estrone analogs
    Andre Stander
    Department of Physiology, University of Pretoria, Pretoria, South Africa
    Chem Biol Drug Des 77:173-81. 2011
  10. ncbi Differential role of organic anion-transporting polypeptides in estrone-3-sulphate uptake by breast epithelial cells and breast cancer cells
    Nilasha Banerjee
    Department of Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy, University of Toronto, 144 College Street, Toronto, ON, Canada M5S 3M2
    J Pharmacol Exp Ther 342:510-9. 2012

Detail Information

Publications348 found, 100 shown here

  1. pmc Kidney-targeted Birt-Hogg-Dube gene inactivation in a mouse model: Erk1/2 and Akt-mTOR activation, cell hyperproliferation, and polycystic kidneys
    Masaya Baba
    Urologic Oncology Branch, National Cancer Institute Frederick, Frederick, MD 21702, USA
    J Natl Cancer Inst 100:140-54. 2008
    ..BHD encodes folliculin, a protein that may interact with the energy- and nutrient-sensing 5'-AMP-activated protein kinase-mammalian target of rapamycin (AMPK-mTOR) signaling pathways...
  2. ncbi Predicted-no-effect concentrations for the steroid estrogens estrone, 17β-estradiol, estriol, and 17α-ethinylestradiol
    Daniel J Caldwell
    Johnson and Johnson, New Brunswick, New Jersey, USA
    Environ Toxicol Chem 31:1396-406. 2012
    The authors derive predicted-no-effect concentrations (PNECs) for the steroid estrogens (estrone [E1], 17β-estradiol [E2], estriol [E3], and 17α-ethinylestradiol [EE2]) appropriate for use in risk assessment of aquatic organisms...
  3. ncbi Association of CYP1A1 polymorphisms with differential metabolic activation of 17beta-estradiol and estrone
    Pyotr Kisselev
    Institute of Clinical Pharmacology, Charite Campus Mitte, University Medicine Berlin, Berlin, Germany
    Cancer Res 65:2972-8. 2005
    ..common allelic variants of human CYP1A1 towards both endogenously occurring estrogens, 17beta-estradiol (E2) and estrone (E1). We expressed and purified CYP1A1.1 (wild-type), CYP1A1.2 (Ile(462)Val), and CYP1A1...
  4. ncbi Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver
    G A Kullak-Ublick
    Division of Clinical Pharmacology and Toxicology, Department of Medicine, University Hospital, Zurich, Switzerland
    Gastroenterology 120:525-33. 2001
    ..We aimed to characterize the novel OATP-B with respect to tissue distribution and hepatocellular localization and to compare its substrate specificity with those of OATP-A, OATP-C, and OATP8...
  5. ncbi Polymorphisms associated with circulating sex hormone levels in postmenopausal women
    Alison M Dunning
    Cancer Research UK, Department of Oncology, University of Cambridge, Strangeways Research Laboratory, Cambridge, UK
    J Natl Cancer Inst 96:936-45. 2004
    ..We investigated the association between levels of sex hormones and single nucleotide polymorphisms (SNPs) in genes coding for the enzymes that regulate them...
  6. ncbi Endometrial and myometrial secretion of androgens and estrone during early pregnancy and luteolysis in pigs
    Anita Franczak
    Department of Animal Physiology, University of Warmia and Mazury in Olsztyn, Oczapowski 1A, 10 718 Olsztyn, Poland
    Reprod Biol 8:213-28. 2008
    ..whether porcine endometrium and myometrium secrete androgens - androstenedione (A(4)), testosterone (T) and estrone (E(1)) during early pregnancy and luteolysis (Days 14-16) in pigs...
  7. ncbi Effects of estrone on N-methyl-D-aspartic acid- and staurosporine-induced changes in caspase-3-like protease activity and lactate dehydrogenase-release: time- and tissue-dependent effects in neuronal primary cultures
    M Kajta
    Department of Endocrinology, Institute of Pharmacology, Polish Academy of Sciences, Smetna 12, 31 343 Krakow, Poland
    Neuroscience 123:515-26. 2004
    ..In the present study we compared effects of estrone (100 and 500 nM) on N-methyl-D-aspartic acid (NMDA) (1 mM)- and staurosporine (1 microM)-induced caspase-3-like ..
  8. ncbi 17β-Estradiol, but not estrone, increases the survival and activation of new neurons in the hippocampus in response to spatial memory in adult female rats
    Robyn E S McClure
    Department of Psychology, Graduate Program in Neuroscience, Brain Research Centre, University of British Columbia, Vancouver, BC, Canada
    Horm Behav 63:144-57. 2013
    Estrogens fluctuate across the lifespan in women, with circulating 17β-estradiol levels higher pre-menopause than estrone and circulating estrone levels higher postmenopause than 17β-estradiol...
  9. ncbi Docking, synthesis, and in vitro evaluation of antimitotic estrone analogs
    Andre Stander
    Department of Physiology, University of Pretoria, Pretoria, South Africa
    Chem Biol Drug Des 77:173-81. 2011
    ..Modifications at position 2' of estrone were made to include moieties that are known to improve the antimitotic activity of estradiol analogs...
  10. ncbi Differential role of organic anion-transporting polypeptides in estrone-3-sulphate uptake by breast epithelial cells and breast cancer cells
    Nilasha Banerjee
    Department of Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy, University of Toronto, 144 College Street, Toronto, ON, Canada M5S 3M2
    J Pharmacol Exp Ther 342:510-9. 2012
    ..b>Estrone-3-sulfate (E3S), a substrate for 7 of 11 OATPs, is a predominant source of tumor estrogen in postmenopausal, ..
  11. ncbi Characterization of common UGT1A8, UGT1A9, and UGT2B7 variants with different capacities to inactivate mutagenic 4-hydroxylated metabolites of estradiol and estrone
    Jean Thibaudeau
    Oncology and Molecular Endocrinology Research Center, Faculty of Pharmacy, Laval University, Quebec, Canada
    Cancer Res 66:125-33. 2006
    The oxidative metabolism of estrone (E1) and estradiol (E2) to form carcinogenic 4-hydroxy-catecholestrogens (4-OHCE) is associated with uterine and breast carcinogenesis...
  12. pmc Reexamination of testosterone, dihydrotestosterone, estradiol and estrone levels across the menstrual cycle and in postmenopausal women measured by liquid chromatography-tandem mass spectrometry
    Micol S Rothman
    Department of Medicine, University of Colorado Denver, Aurora, CO 80045, USA
    Steroids 76:177-82. 2011
    ..LC-MS/MS) assays to determine testosterone (T) and dihydrotestosterone (DHT) along with estradiol (E2) and estrone (E1) levels across the menstrual cycle of 31 healthy premenopausal females and in 19 postmenopausal females...
  13. ncbi Polymorphisms in human organic anion-transporting polypeptide 1A2 (OATP1A2): implications for altered drug disposition and central nervous system drug entry
    Wooin Lee
    Division of Clinical Pharmacology, Department of Medicine, Vanderbilt University, Nashville Tennessee 37232, USA
    J Biol Chem 280:9610-7. 2005
    ..A516C and A404T variants had markedly reduced capacity for mediating the cellular uptake of OATP1A2 substrates, estrone 3-sulfate and two delta-opioid receptor agonists, deltorphin II, and [D-penicillamine(2,5)]-enkephalin...
  14. ncbi Role of polymorphic human cytochrome P450 enzymes in estrone oxidation
    Alastair E Cribb
    Department of Biomedical Sciences, Atlantic Veterinary College, University of Prince Edward Island, 550 University Avenue, Charlottetown, Prince Edward Island, Canada C1A 4P3
    Cancer Epidemiol Biomarkers Prev 15:551-8. 2006
    ..Therefore, we assessed the human cytochrome P450-dependent oxidation of estrone using substrate concentrations that more closely approximate the maximum expected concentrations in breast tissue...
  15. ncbi Endogenous steroid hormone concentrations and risk of breast cancer: does the association vary by a woman's predicted breast cancer risk?
    A Heather Eliassen
    Channing Laboratory, Brigham and Women s Hospital, Boston, MA 02115, USA
    J Clin Oncol 24:1823-30. 2006
    ....
  16. ncbi Acute regulation of OAT3-mediated estrone sulfate transport in isolated rabbit renal proximal tubules
    S Soodvilai
    Dept of Physiology, College of Medicine, University of Arizona, Tucson, AZ 85724, USA
    Am J Physiol Renal Physiol 287:F1021-9. 2004
    ..PMA, a PKC activator, inhibited uptake of estrone sulfate (ES), a prototypic substrate for OAT3, in a dose- and time-dependent manner...
  17. ncbi Plasma estrone sulfate assay in men: Comparison of radioimmunoassay, mass spectrometry coupled to gas chromatography (GC-MS), and liquid chromatography-tandem mass spectrometry (LC-MS/MS)
    Frank Giton
    AP HP CIB GHU Sud, Hopital Henri Mondor, Faculte de Medecine, 8 rue du General Sarrail, 94010 Creteil, France
    Clin Chim Acta 411:1208-13. 2010
    Estrogens are involved in the natural history of the prostate cancer and estrone sulfate, the quantitatively main circulating plasma estrogen in men, has been associated with an aggressive form of this cancer...
  18. ncbi pH-Dependent transport of pemetrexed by breast cancer resistance protein
    Li Li
    Department of Pharmaceutics, University of Minnesota, 308 Harvard Street SE, Minneapolis, MN 55455, USA
    Drug Metab Dispos 39:1478-85. 2011
    ..the study presented here, we examine the pH dependence of BCRP using methothrexate (MTX), pemetrexed (PMX), and estrone sulfate (ES) as model substrates...
  19. pmc Uremic toxins inhibit transport by breast cancer resistance protein and multidrug resistance protein 4 at clinically relevant concentrations
    Henricus A M Mutsaers
    Department of Pharmacology and Toxicology, Radboud University Nijmegen Medical Centre, Nijmegen, The Netherlands
    PLoS ONE 6:e18438. 2011
    ..5 mM, 1 mM, 25 µM, respectively) and BCRP-mediated [(3)H]-estrone sulfate ([(3)H]-E1S) uptake (Ki values: 4 mM, 500 µM and 50 µM, respectively), whereas indole-3-acetic acid and ..
  20. ncbi Recent data on intratumor estrogens in breast cancer
    Per E Lønning
    Section of Oncology, Institute of Medicine, University of Bergen, Norway
    Steroids 76:786-91. 2011
    ..Novel data on tissue estrogen levels confirm a positive normal breast tissue to plasma concentration gradient for estrone, and to a smaller extent estradiol. Remarkably, this gradient is similar for pre- and post-menopausal women...
  21. ncbi A novel cancer targeting approach based on estrone anchored stealth liposome for site-specific breast cancer therapy
    Shivani Rai Paliwal
    Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Dr H S Gour Viswavidyalaya, Sagar M P, India
    Curr Cancer Drug Targets 10:343-53. 2010
    ..b>Estrone (ES) was anchored as ligand on to stealth liposome (ES-SL-DOX) for targeting to ERs...
  22. ncbi Analysis of the phylogenetic diversity of estrone-degrading bacteria in activated sewage sludge using microautoradiography-fluorescence in situ hybridization
    Kaisai Zang
    Department of Urban Engineering, Graduate School of Engineering, University of Tokyo, 7 3 1 Hongo, Bunkyo ku, Tokyo, Japan
    Syst Appl Microbiol 31:206-14. 2008
    In situ uptake of [2,4,6,7-3H(N)]estrone ([3H]E1) by the major phylogenetic groups present in activated sludge samples from two different municipal wastewater treatment plants was investigated using microautoradiography-fluorescence in ..
  23. ncbi Comparative study on the in vitro/in vivo estrogenic potencies of 17beta-estradiol, estrone, 17alpha-ethynylestradiol and nonylphenol
    K Van den Belt
    VITO Flemish Institute for Technological Research, Expertisecenter Environmental Toxicology, Boeretang 200 B 2400 MOL, Belgium
    Aquat Toxicol 66:183-95. 2004
    ..Compounds tested were 17beta-estradiol (E2), estrone (E1), 17alpha-ethynylestradiol (EE2) and the alkylphenolic compound nonylphenol (NP)...
  24. pmc Adiposity and sex hormones in postmenopausal breast cancer survivors
    Anne McTiernan
    Cancer Prevention Research Program, MP 900, Fred Hutchinson Cancer Research Center, 1100 Fairview Ave N, Seattle, WA 98109, USA
    J Clin Oncol 21:1961-6. 2003
    ..This study examined the association between adiposity and concentrations of estrogens, androgens, and sex hormone-binding globulin (SHBG) in a population-based sample of postmenopausal women with breast cancer...
  25. pmc Alterations in the production rate and the metabolism of oestrone and oestrone sulphate in breast cancer patients treated with aminoglutethimide
    P E Lønning
    Department of Therapeutic Oncology and Radiophysics, University of Bergen, Norway
    Br J Cancer 60:107-11. 1989
    ..The possibility that such effects might be partly responsible for the mechanism of action of aminoglutethimide in advanced breast cancer should be considered...
  26. ncbi Estradiol and estrone C-16 derivatives as inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: blocking of ER+ breast cancer cell proliferation induced by estrone
    Yannick Laplante
    Medicinal Chemistry Division, Oncology and Molecular Endocrinology Research Center, CHUQ Pavillon CHUL and Université Laval, Que, Canada G1V 4G2
    Bioorg Med Chem 16:1849-60. 2008
    ..study identifying 16beta-benzyl-E2 (1) as a lead compound for developing inhibitors of the transformation of estrone (E1) into E2, we modified the benzyl group of 1 to improve its inhibitory activity...
  27. pmc Disruption of Fnip1 reveals a metabolic checkpoint controlling B lymphocyte development
    Heon Park
    The Department of Comparative Medicine, University of Washington, Seattle, WA 98195 7190, USA
    Immunity 36:769-81. 2012
    ....
  28. ncbi Relative involvement of three 17beta-hydroxysteroid dehydrogenases (types 1, 7 and 12) in the formation of estradiol in various breast cancer cell lines using selective inhibitors
    Yannick Laplante
    Oncology and Molecular Endocrinology Laboratory Medicinal Chemistry Division, CHUQ CHUL Research Center and Université Laval, 2705 Laurier Boulevard, Quebec, Quebec G1V 4G2, Canada
    Mol Cell Endocrinol 301:146-53. 2009
    ..and JEG-3 cells, a 17beta-HSD1 inhibitor almost completely inhibited the formation of E2 at 1microM from 60nM of estrone (E1) (98%, 91% and 90%, respectively), whereas no significant inhibition of E2 formation was obtained using ..
  29. ncbi Body mass index, circulating levels of sex-steroid hormones, IGF-I and IGF-binding protein-3: a cross-sectional study in healthy women
    A Lukanova
    Hormones and Cancer Group, International Agency for Research on Cancer, Lyon, France
    Eur J Endocrinol 150:161-71. 2004
    ..with circulating androgens (testosterone, androstenedione and dehydroepiandrosterone sulfate (DHEAS)), estrogens (estrone and estradiol), sex hormone-binding globulin (SHBG), IGF-I and IGF-binding protein (IGFBP)-3, and the ..
  30. ncbi Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C
    I Tamai
    Faculty of Pharmaceutical Sciences, Kanazawa University, Japan
    Pharm Res 18:1262-9. 2001
    ..OATP-B or -C was expressed in HEK293 cells or Xenopus oocytes, and uptakes of estradiol-17beta-glucuronide and estrone-3-sulfate were measured using radiolabeled compounds...
  31. ncbi CYP3A variation, premenopausal estrone levels, and breast cancer risk
    Nichola Johnson
    The Breakthrough Breast Cancer Research Centre, Division of Breast Cancer Research, Institute of Cancer Research, London, UK
    J Natl Cancer Inst 104:657-69. 2012
    ..Our aim was to identify common variants in genes involved in sex steroid synthesis or metabolism that are associated with hormone levels and the risk of breast cancer in premenopausal women...
  32. pmc The contribution of 17beta-hydroxysteroid dehydrogenase type 1 to the estradiol-estrone ratio in estrogen-sensitive breast cancer cells
    Chen Yan Zhang
    Laboratory of Molecular Endocrinology and Oncology, Centre Hospitalier de Université Laval Research Center CHUL, CHUQ and Laval University, Quebec City, Quebec, Canada
    PLoS ONE 7:e29835. 2012
    b>Estrone and estradiol are both estrogens with estrone being the less potent form and estradiol being the most potent estrogen. The binding of the latter to cellular regulatory elements stimulates the proliferation of breast cancer cells...
  33. ncbi Dehydroepiandrosterone sulfate and estrone sulfate reduce GABA-recurrent inhibition in the hippocampus via muscarinic acetylcholine receptors
    Scott C Steffensen
    Department of Psychology, Brigham Young University, Provo, Utah 846022, USA
    Hippocampus 16:1080-90. 2006
    ..In this study, we evaluated the role of muscarinic receptors in mediating the effects of DHEAS and estrone sulfate (ES), the principal circulating estrogen in humans, on short-latency-evoked potential responses, paired-..
  34. ncbi Obesity, estrone, and coronary artery disease in postmenopausal women
    T C B F Silva
    Heart Institute InCor, University of Sao Paulo Medical School, 05468 000 São Paulo, Brazil
    Maturitas 59:242-8. 2008
    ..In this prospective study we analyzed the association of body mass index (BMI) and blood levels of estrone in postmenopausal women with known CAD or with a high risk factor score for CAD.
  35. ncbi Novel estrone mimetics with high 17beta-HSD1 inhibitory activity
    Alexander Oster
    Pharmaceutical and Medicinal Chemistry, Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, PO Box 15 11 50, D 66041 Saarbrucken, Germany
    Bioorg Med Chem 18:3494-505. 2010
    17Beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) catalyzes the reduction of estrone into estradiol, which is the most potent estrogen in humans...
  36. ncbi Identification of steroid sulfate transport processes in the human mammary gland
    F Pizzagalli
    Division of Clinical Pharmacology and Toxicology, Department of Internal Medicine, University Hospital of Zurich, Switzerland
    J Clin Endocrinol Metab 88:3902-12. 2003
    ..b>Estrone-3-sulfate (E(1)S) is an important estrogenic form in premenopausal women, and dehydroepiandrosterone sulfate (..
  37. ncbi A novel spreadsheet method for calculating the free serum concentrations of testosterone, dihydrotestosterone, estradiol, estrone and cortisol: with illustrative examples from male and female populations
    Norman A Mazer
    Section of Endocrinology, Diabetes and Nutrition, Boston University School of Medicine, Boston, MA, United States
    Steroids 74:512-9. 2009
    In humans, testosterone (T), dihydrotestosterone (DHT), estradiol (E2), estrone (E1) and cortisol (C) bind to the serum proteins sex hormone-binding globulin (SHBG), albumin (Alb) and corticosteroid-binding globulin (CBG)...
  38. ncbi Specificity and regioselectivity of the conjugation of estradiol, estrone, and their catecholestrogen and methoxyestrogen metabolites by human uridine diphospho-glucuronosyltransferases expressed in endometrium
    Johanie Lepine
    Department of Molecular Endocrinology and Oncology, G1V 4G2 Quebec, Canada
    J Clin Endocrinol Metab 89:5222-32. 2004
    ..Six UGTs, namely 1A1, 1A3, 1A8, 1A9, 1A10, and 2B7, were found to glucuronidate estradiol (E(2)) and estrone (E(1)), their hydroxyls (OH), and their methoxy derivatives (MeO)...
  39. ncbi Identification of a novel human organic anion transporting polypeptide as a high affinity thyroxine transporter
    F Pizzagalli
    Division of Clinical Pharmacology and Toxicology, Department of Medicine, University Hospital, CH 8091 Zurich, Switzerland
    Mol Endocrinol 16:2283-96. 2002
    ..Substrates less well transported by OATP-F include T(3), bromosulfophthalein, estrone-3-sulfate, and estradiol-17beta-glucuronide...
  40. ncbi Organic anion transporting polypeptide 2B1 is a high-affinity transporter for atorvastatin and is expressed in the human heart
    Markus Grube
    Research Center of Pharmacology and Experimental Therapeutics and Department of Pharmacology, Ernst Moritz Arndt University, Greifswald, Germany
    Clin Pharmacol Ther 80:607-20. 2006
    ..In this study we examine OATP2B1 expression in the human heart and describe statins as inhibitors and substrates of OATP2B1...
  41. ncbi A model to estimate influent and effluent concentrations of estradiol, estrone, and ethinylestradiol at sewage treatment works
    Andrew C Johnson
    Centre for Ecology and Hydrology, Wallingford, Oxon OXIO 8BB, United Kingdom
    Environ Sci Technol 38:3649-58. 2004
    To predict sewage influent and effluent concentrations of the steroid estrogens 17beta-estradiol, estrone, and 17alpha-ethinylestradiol, a review of human excretion was carried out...
  42. ncbi Endogenous sex hormones and breast cancer in postmenopausal women: reanalysis of nine prospective studies
    T Key
    Cancer Research U K Epidemiology Unit, University of Oxford, Radcliffe Infirmary, Oxford, UK
    J Natl Cancer Inst 94:606-16. 2002
    ..We reanalyzed the worldwide data from prospective studies to examine the relationship between the levels of endogenous sex hormones and breast cancer risk in postmenopausal women...
  43. ncbi Substrate-dependent drug-drug interactions between gemfibrozil, fluvastatin and other organic anion-transporting peptide (OATP) substrates on OATP1B1, OATP2B1, and OATP1B3
    Johannes Noe
    F Hoffmann La Roche Ltd, Non Clinical Development Drug Safety, Basel, Switzerland
    Drug Metab Dispos 35:1308-14. 2007
    ..of 63 microM), pravastatin, simvastatin, and taurocholate was inhibited by gemfibrozil, whereas the transport of estrone-3-sulfate and troglitazone sulfate (both used at 3 microM) was not affected...
  44. pmc Short-term oleoyl-estrone treatment affects capacity to manage lipids in rat adipose tissue
    Anna Salas
    Departament de Nutrició i Bromatologia, Facultat de Biologia, Universitat de Barcelona, Av, Diagonal 645, 08028 Barcelona, Spain
    BMC Genomics 8:292. 2007
    Short-term OE (oleoyl-estrone) treatment causes significant decreases in rat weight mainly due to adipose tissue loss...
  45. pmc Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3
    Chunshan Gui
    Department of Pharmacology, Toxicology and Therapeutics, The University of Kansas Medical Center, Kansas City, Kansas, USA
    Eur J Pharmacol 584:57-65. 2008
    ..Transport of estrone-3-sulfate was hardly affected while all other substrates tested were inhibited...
  46. ncbi Tissue estradiol is selectively elevated in receptor positive breast cancers while tumour estrone is reduced independent of receptor status
    P E Lønning
    Section of Oncology, Institute of Medicine, University of Bergen, Jonas Lies vei 26, N 5021 Bergen, Norway
    J Steroid Biochem Mol Biol 117:31-41. 2009
    ..We detected similar concentrations of each of the three major estrogens estradiol (E(2)), estrone (E(1)) and E(1)S in tumour-bearing versus non-tumour-bearing quadrants...
  47. pmc Human oestrogenic 17beta-hydroxysteroid dehydrogenase specificity: enzyme regulation through an NADPH-dependent substrate inhibition towards the highly specific oestrone reduction
    A Gangloff
    Oncology and Molecular Endocrinology Research Center, Laval University Medical Center (CHUL, 2705 Boulevard Laurier, , G1V 4G2, Canada
    Biochem J 356:269-76. 2001
    ....
  48. ncbi Interrelationships of serum estradiol, estrone, and estrone sulfate, adiposity, biochemical bone markers, and leptin in post-menopausal women
    V Daniel Castracane
    Department of Obstetrics and Gynecology, Texas Tech University Health Sciences Center, Amarillo, USA
    Maturitas 53:217-25. 2006
    ..The aim of this study was to examine the relationships between endogenous estrogens and adiposity, bone markers, and leptin in post-menopausal (PM) women...
  49. ncbi Mutations in a novel gene lead to kidney tumors, lung wall defects, and benign tumors of the hair follicle in patients with the Birt-Hogg-Dubé syndrome
    Michael L Nickerson
    Laboratory of Immunobiology, Center for Cancer Research, SAIC Frederick, Inc, National Center for Cancer Research, Frederick, MD 21702, USA
    Cancer Cell 2:157-64. 2002
    ....
  50. ncbi Combined effects of oleoyl-estrone and a beta3-adrenergic agonist (CL316,243) on lipid stores of diet-induced overweight male Wistar rats
    Raquel Ferrer-Lorente
    Department of Nutrition and Food Science Faculty of Biology, University of Barcelona, Av Diagonal, 645, E 08028 Barcelona, Spain
    Life Sci 77:2051-8. 2005
    Oleoyl-estrone (OE) decreases appetite, induces adipose tissue wasting and resets the ponderostat setting, sparing glucose and protein. The beta3-adrenergic agonists increase energy expenditure and lipolysis...
  51. ncbi Targeted delivery of doxorubicin via estrone-appended liposomes
    Shivani Rai
    Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Dr H S Gour Vishwavidyalaya, Sagar, MP, India
    J Drug Target 16:455-63. 2008
    b>Estrone-appended liposomal formulation of doxorubicin was designed to enhance the capability of clinically used liposomal doxorubicin formulation with the added advantage of delivery of doxorubicin to its destination site, i.e...
  52. ncbi Involvement of tyrosine kinase and PI3K in the regulation of OAT3-mediated estrone sulfate transport in isolated rabbit renal proximal tubules
    S Soodvilai
    Dept of Physiology, Faculty of Science, Mahidol University, Bangkok, Thailand 10400
    Am J Physiol Renal Physiol 289:F1057-64. 2005
    ..Genistein, a tyrosine kinase inhibitor, and wortmannin, a PI3K inhibitor, inhibited transport of estrone sulfate, a prototypic substrate for OAT3, in a dose-dependent manner...
  53. ncbi Binary and ternary crystal structure analyses of a novel inhibitor with 17beta-HSD type 1: a lead compound for breast cancer therapy
    Mausumi Mazumdar
    Laboratory of Molecular Endocrinology and Oncology, CHUL Research Center Centre Hospitalier de Université Laval, CHUQ and Laval University, Quebec, Canada, G1V 4G2
    Biochem J 424:357-66. 2009
    ..Such inhibitors that block oestrogen synthesis to suppress the sulfatase pathway producing oestradiol can be used in adjuvant therapies with oestrogen receptor blockade, opening a new orientation of breast cancer treatment...
  54. ncbi Combined effects of oral oleoyl-estrone and limited food intake on body composition of young overweight male rats
    M M Romero
    Departament de Nutrició i Bromatologia, Facultat de Biologia, Universitat de Barcelona, Barcelona, Spain
    Int J Obes (Lond) 30:1149-56. 2006
    ..Two levels of dietary limitation at 50 and 25% of a standard intake were established, roughly corresponding to the human LCDs and VLCDs...
  55. ncbi Endogenous estrogen, androgen, and progesterone concentrations and breast cancer risk among postmenopausal women
    Stacey A Missmer
    Channing Laboratory, Brigham and Women s Hospital and Harvard Medical School, 181 Longwood Avenue, Boston, MA 02115, USA
    J Natl Cancer Inst 96:1856-65. 2004
    ..Nor has the relation between breast cancer risk and postmenopausal progesterone levels been investigated. We prospectively investigated these relations in a case-control study nested within the Nurses' Health Study...
  56. ncbi pH dependence of organic anion-transporting polypeptide 2B1 in Caco-2 cells: potential role in antiretroviral drug oral bioavailability and drug-drug interactions
    Olena Kis
    Department of Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy, University of Toronto, Toronto, Canada
    J Pharmacol Exp Ther 334:1009-22. 2010
    ..b>Estrone-3-sulfate (E3S) uptake demonstrated biphasic saturation kinetics in Caco-2 cells, with dissociation constants (K(..
  57. ncbi Peripartum changes in plasma estrone sulfate and estradiol-17beta profiles associated with and without the retention of fetal membranes in holstein-friesian cattle
    Kapil Deo Shah
    Graduate School of Biosphere Science, Hiroshima University, Higashi Hiroshima, Japan
    J Reprod Dev 53:279-88. 2007
    The aim of this study was to evaluate the changes in plasma concentrations of estrone sulfate (E(1)S) and estradiol-17beta (E(2)beta) during the peripartum period (from day 10 prepartum to day 1 postpartum) associated with and without ..
  58. ncbi Sorption of bisphenol A, 17alpha-ethynylestradiol and estrone to mineral surfaces
    Ali Shareef
    Colloid and Environmental Chemistry Laboratory, La Trobe University, P O Box 199, Bendigo, Victoria 3552, Australia
    J Colloid Interface Sci 297:62-9. 2006
    Sorption of the endocrine disrupting chemicals (EDCs) bisphenol A (BPA), 17alpha-ethynylestradiol (EE2) and estrone (E1) from 3 microM aqueous solutions in 10 mM KNO3 to goethite, kaolinite and montmorillonite was investigated at 25 ..
  59. ncbi Estrone sulfate is a major source of local estrogen formation in human bone
    Mischa Muir
    Department of Internal Medicine, Division of Endocrinology, University of Bonn, Wilhelmstrasse 35 37, 53111 Bonn, Germany
    J Clin Endocrinol Metab 89:4685-92. 2004
    b>Estrone sulfate (E1S) is the most abundant estrogen in the circulation of adults...
  60. ncbi An optimised, highly sensitive radioimmunoassay for the simultaneous measurement of estrone, estradiol and estrone sulfate in the ultra-low range in human plasma samples
    Jurgen Geisler
    Institute of Medicine, Section of Oncology, University of Bergen, Norway
    J Steroid Biochem Mol Biol 109:90-5. 2008
    ..We describe here an optimised radioimmunoassay suitable for the simultaneous measurement of plasma estrone (E1), estradiol (E2) and estrone sulfate (E1S) levels in the ultra-low range...
  61. ncbi Hybrid molecules of estrone: new compounds with potential antibacterial, antifungal, and antiproliferative activities
    J Adamec
    Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, Hradec Kralove, 500 05, Czech Republic
    Bioorg Med Chem 15:2898-906. 2007
    New hybrid molecules of estrone were synthesized as compounds indicating promising biological activity (antibacterial, antimycobacterial, antifungal, and antiproliferative)...
  62. ncbi Antioxidant effects of a grapeseed procyanidin extract and oleoyl-estrone in obese Zucker rats
    Vanessa M Castrillejo
    Department of Biochemistry and Biotechnology, Rovira i Virgili University, Tarragona, Spain
    Nutrition 27:1172-6. 2011
    ..beneficial properties of a grapeseed proanthocyanidin extract (GSPE), the amelioration of obesity with oleoyl-estrone (OE), and the possible combined effect of GSPE and OE on the hepatic and renal antioxidant enzyme system in ..
  63. ncbi Inhibition of estrone sulfatase and proliferation of human breast cancer cells by nonsteroidal (p-O-sulfamoyl)-N-alkanoyl tyramines
    K W Selcer
    Department of Biological Sciences, Duquesne University, Pittsburgh, Pennsylvania 15282, USA
    Cancer Res 57:702-7. 1997
    ..The major source of estrogen in breast cancer cells may be the conversion of estrone sulfate to estrone by the enzyme estrone sulfatase...
  64. ncbi Characterization of structural and functional properties of human 17 beta-hydroxysteroid dehydrogenase type 1 using recombinant enzymes and site-directed mutagenesis
    T Puranen
    Biocenter Oulu, University of Oulu, Finland
    Mol Endocrinol 11:77-86. 1997
    Human 17 beta-hydroxysteroid dehydrogenase (17-HSD) type 1 catalyzes the conversion of the low activity estrogen, estrone, into highly active estradiol, both in the gonads and in target tissues...
  65. ncbi Gene expression of 3beta-hydroxysteroid dehydrogenase and 17beta-hydroxysteroid dehydrogenase in relation to androstenone, testosterone, and estrone sulphate in gonadally intact male and castrated pigs
    G Chen
    Department of Food Science, Swedish University of Agricultural Sciences, PO Box 7051, SE 750 07 Uppsala, Sweden
    J Anim Sci 85:2457-63. 2007
    ..were determined by real-time PCR analysis and related to the concentrations of androstenone, testosterone, and estrone sulphate (E1S)...
  66. pmc Identification of amino acids essential for estrone-3-sulfate transport within transmembrane domain 2 of organic anion transporting polypeptide 1B1
    Nan Li
    College of Life Science, South China Agricultural University, Guangzhou, China
    PLoS ONE 7:e36647. 2012
    ....
  67. ncbi Effects of single pesticides and binary pesticide mixtures on estrone production in H295R cells
    Wiebke Prutner
    Institute for Food Toxicology and Analytical Chemistry, University of Veterinary Medicine Hannover, Bischofsholer Damm 15, 30173, Hannover, Germany
    Arch Toxicol 87:2201-14. 2013
    ..line H295R can be used as an in vitro test system to investigate the effects of binary pesticide combinations on estrone production as biological endpoint...
  68. pmc Long-term prospective study of the influence of estrone levels on events in postmenopausal women with or at high risk for coronary artery disease
    Antonio de Padua Mansur
    Heart Institute InCor, University of Sao Paulo Medical School, 05403 000 Sao Paulo, SP, Brazil
    ScientificWorldJournal 2012:363595. 2012
    ..We analyzed the association between death and blood levels of estrone in postmenopausal women with known coronary artery disease (CAD) or with a high-risk factor score for CAD.
  69. pmc Age trends in estradiol and estrone levels measured using liquid chromatography tandem mass spectrometry in community-dwelling men of the Framingham Heart Study
    Guneet Kaur Jasuja
    Department of Mathematics, Boston University, Massachusetts, Boston, MA 02118, USA
    J Gerontol A Biol Sci Med Sci 68:733-40. 2013
    Age trends in estradiol and estrone levels in men and how lifestyle factors, comorbid conditions, testosterone, and sex hormone-binding globulin affect these age trends remain poorly understood, and were examined in men of the Framingham ..
  70. ncbi Purification, characterization and crystallization of human placental estrone/dehydroepiandrosterone sulfatase, a membrane-bound enzyme of the endoplasmic reticulum
    F G Hernandez-Guzman
    Department of Molecular and Cellular Biophysics, Roswell Park Cancer Institute, Elm and Carlton Streets, Buffalo, NY 14263, USA
    J Steroid Biochem Mol Biol 78:441-50. 2001
    b>Estrone (E1)/dehydroepiandrosterone (DHEA) sulfatase (ES/DHEAS) catalyzes the hydrolysis of E1 and DHEA-sulfates releasing unconjugated steroids...
  71. pmc Plasma estrone sulfate concentrations and genetic variation at the CYP19A1 locus in postmenopausal women with early breast cancer treated with letrozole
    G Lunardi
    Oncology Unit, Ospedale Sacro Cuore Don Calabria, Via Sempreboni, 5, 37024 Negrar, VR, Italy
    Breast Cancer Res Treat 137:167-74. 2013
    ..We assessed the association between plasma estrone sulfate (ES), letrozole treatment, and four SNPs of CYP19A1 gene (rs10046 C>T, rs4646 G>T, rs749292 C>T, ..
  72. ncbi Atheroprotective effect of estriol and estrone sulfate on human vascular smooth muscle cells
    N Kikuchi
    Department of Obstetrics and Gynecology, Kyoto Prefectural University of Medicine, Kawaramachi Hirokoji, Kamigyo ku, Kyoto, Japan
    J Steroid Biochem Mol Biol 72:71-8. 2000
    ..There have been few reports about the atheroprotective effect of estriol (E(3)). Estrone sulfate (E(1)-S) is the predominant estrogen of conjugated equiline estrogens, which is commonly used in hormone ..
  73. ncbi An assessment of the bioaccumulation of estrone in Daphnia magna
    Rachel L Gomes
    Environmental Processes and Water Technology Research Group, Department of Environmental Science and Technology, Imperial College London, Exhibition Road, London SW7 2BP, United Kingdom
    Environ Toxicol Chem 23:105-8. 2004
    The bioaccumulation of estrone by Daphnia magna was determined. Direct uptake via the aqueous medium occurred within the first 16 h. A bioconcentration factor of 228 was established over all temporal periods...
  74. ncbi Estrone sulfatase activity in patients with advanced ovarian cancer
    Justin C Chura
    Department of Obstetrics, Division of Gynecologic Oncology, University of Minnesota, Minneapolis, MN 55455, USA
    Gynecol Oncol 112:205-9. 2009
    ..We sought to identify whether the sulfatase pathway was present in ovarian cancer specimens and then to determine whether a clinical correlation existed between sulfatase activity and survival...
  75. ncbi Inhibition of placental estrone sulfatase activity and MCF-7 breast cancer cell proliferation by estrone-3-amino derivatives
    K W Selcer
    Department of Biological Sciences, Duquesne University, Pittsburgh, PA 15282, USA
    J Steroid Biochem Mol Biol 59:83-91. 1996
    ..lines of evidence indicate that the major source of estrogen in breast cancer cells may be from conversion of estrone sulfate to estrone by the enzyme estrone sulfatase...
  76. ncbi Letrozole suppresses plasma estradiol and estrone sulphate more completely than anastrozole in postmenopausal women with breast cancer
    J Michael Dixon
    Edinburgh Breast Unit, Western General Hospital, Edinburgh EH4 2XU, United Kingdom
    J Clin Oncol 26:1671-6. 2008
    To compare the effects of anastrozole and letrozole on plasma estradiol (E2) and estrone sulfate (E1S) levels.
  77. ncbi Liquid chromatography-tandem mass spectrometry assay for simultaneous measurement of estradiol and estrone in human plasma
    Robert E Nelson
    Department of Laboratory Medicine and Pathology, Mayo Clinic and Foundation, Rochester, MN 55905, USA
    Clin Chem 50:373-84. 2004
    Estradiol (E2) and estrone (E1) measurements form an integral part of the assessment of female reproductive function and have expanding roles in other fields...
  78. ncbi Removal of the natural hormone estrone from aqueous solutions using nanofiltration and reverse osmosis
    A I Schafer
    Centre for Water and Waste Technology, School of Civil and Environmental Engineering The University of New South Wales, Sydney, New South Wales 2052, Australia
    Environ Sci Technol 37:182-8. 2003
    The ability of a variety of nanofiltration and reverse osmosis membranes to retain the natural hormone estrone are examined here as a function of solution conditions...
  79. pmc A prospective study of urinary oestrogen excretion and breast cancer risk
    T J Key
    Imperial Cancer Research Fund, Cancer Epidemiology Unit, Radcliffe Infirmary, Oxford, UK
    Br J Cancer 73:1615-9. 1996
    ..016). We conclude that high levels of endogenous oestrogens in post-menopausal women are associated with increased breast cancer risk, but that the relationship of oestrogens in premenopausal women with risk is unclear...
  80. ncbi Concentration-dependent response of estrone-degrading bacterial community in activated sludge analyzed by microautoradiography-fluorescence in situ hybridization
    Parinda Thayanukul
    Department of Urban Engineering, The University of Tokyo, 7 3 1 Hongo, Bunkyo ku, Tokyo 113 8656, Japan
    Water Res 44:4878-87. 2010
    Inefficient removal of estrone (E1) in wastewater treatment plants (WWTPs) causes feminizing effects in male aquatic creatures...
  81. ncbi Peripheral changes in estrone sulfate concentration during the first trimester of gestation in cattle: comparison with unconjugated estrogens and relationship to fetal number
    Makoto Hirako
    Department of Animal Breeding and Reproduction, National Institute of Livestock and Grassland Science, Nishinasuno, Tochigi, Japan
    Theriogenology 57:1939-47. 2002
    b>Estrone sulfate originates mainly in the conceptus during gestation in cattle. Its concentration in maternal body fluids is a useful indicator of placental function...
  82. ncbi Longitudinal evaluation of serum estradiol and estrone in male patients infected with the human immunodeficiency virus
    J Teichmann
    Medizinische Klinik und Poliklinik III, Universistätsklinikum der Justus Liebig Universistät Giessen, Germany
    Eur J Med Res 8:77-80. 2003
    ..Follicle stimulating hormone (FSH), luteinizing hormone (LH), prolactin, estrone, estradiol, and testosterone were measured in serum by commercially available radioimmunoassays...
  83. ncbi Modification of OATP2B1-mediated transport by steroid hormones
    Markus Grube
    Department of Pharmacology, Research Center of Pharmacology and Experimental Therapeutics, Friedrich Loeffler Str 23d, 17487 Greifswald, Germany
    Mol Pharmacol 70:1735-41. 2006
    ..in those tissues because only a limited number of compounds, such as dehydroepiandrosterone-sulfate (DHEAS) and estrone-3-sulfate (E3S), have been characterized as OATP2B1 substrates...
  84. ncbi Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors
    L W Lawrence Woo
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK
    Bioorg Med Chem 20:2506-19. 2012
    b>Estrone sulfamate (EMATE) is a potent irreversible inhibitor of steroid sulfatase (STS). In order to further expand SAR, the compound was substituted at the 2- and/or 4-positions and its 17-carbonyl group was also removed...
  85. ncbi The effects of estrone, estradiol and estriol on platelet aggregation induced by adrenaline and adenosine diphosphate
    Pravit Akarasereenont
    Department of Pharmacology, Faculty of Medicine Siriraj Hospital, Mahidol University, Prannok Rd, Bangkok 10700, Thailand
    Platelets 17:441-7. 2006
    ..Here, we investigated the effects of various forms of estrogen, including estrone (E1), estradiol (E2) and estriol (E3), on platelet aggregation induced by standard agonists (adrenaline and ..
  86. ncbi Futile cycling of estrone sulfate and estrone in the recirculating perfused rat liver preparation
    E Tan
    Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Toronto, 19 Russell Street, Toronto, Ontario M5S 2S2, Canada
    J Pharmacol Exp Ther 297:423-36. 2001
    The futile cycling of estrone sulfate (E(1)S) and estrone (E1) was investigated in the recirculating, perfused, rat liver preparation...
  87. ncbi Effect of oral oleoyl-estrone on adipose tissue composition in male rats
    X Remesar
    Centre Especial de Recerca en Nutricio i Ciencia dels Aliments, Universitat de Barcelona, Barcelona, Spain
    Int J Obes Relat Metab Disord 26:1092-102. 2002
    To determine whether the oral administration of oleoyl-estrone has similar mass-decreasing effects on the main different sites of white adipose tissue (WAT).
  88. ncbi Organic anion transporting polypeptide (Oatp) 1a1-mediated perfluorooctanoate transport and evidence for a renal reabsorption mechanism of Oatp1a1 in renal elimination of perfluorocarboxylates in rats
    Ching Hui Yang
    DuPont Haskell Global Centers for Health and Environmental Sciences, Newark, DE 19714, USA
    Toxicol Lett 190:163-71. 2009
    ..The Oatp1a1-expressing CHO cells have been validated by their Oatp1a1 gene expression, estrone-3-sulfate (E3S) uptake kinetics, and the correlation between Oatp1a1 gene expression and E3S uptake activity that ..
  89. ncbi Involvement of human organic anion transporting polypeptide OATP-B (SLC21A9) in pH-dependent transport across intestinal apical membrane
    Daisuke Kobayashi
    Department of Molecular Biopharmaceutics, Faculty of Pharmaceutical Sciences, Tokyo University of Science, Tokyo, Japan
    J Pharmacol Exp Ther 306:703-8. 2003
    ..Localization of OATP-B was determined by immunohistochemical analysis. Transport properties of estrone-3-sulfate and the 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor pravastatin by OATP-B-transfected human ..
  90. ncbi Glutathione stimulates sulfated estrogen transport by multidrug resistance protein 1
    Y M Qian
    Cancer Research Laboratories, Queen's University, Kingston, Ontario, Canada K7L 3N6
    J Biol Chem 276:6404-11. 2001
    ..We found that estradiol and estrone 3-sulfate alone were poor competitors of MRP1-mediated transport of the cysteinyl leukotriene, leukotriene C(4)...
  91. ncbi Chemical reactivity as a tool to study carcinogenicity: reaction between estradiol and estrone 3,4-quinones ultimate carcinogens and guanine
    Ph Huetz
    Laboratoire de Physique Moleculaire, UMR CNRS 6624, Faculte des Sciences et Techniques, La Bouloie, Universite de Franche Comte, 25030 Besancon, France
    J Chem Inf Comput Sci 44:310-4. 2004
    ..study the chemical reactions between guanine and two ultimate carcinogens, the 3,4-quinone forms of the estrogens estrone (E1) and estradiol (E2). DNA was truncated to guanine, i.e. no deoxyribose moiety was included...
  92. pmc Role of transmembrane domain 10 for the function of organic anion transporting polypeptide 1B1
    Chunshan Gui
    Department of Pharmacology, Toxicology and Therapeutics, University of Kansas Medical Center, Kansas City, Kansas 66160, USA
    Protein Sci 18:2298-306. 2009
    ..However, at low concentrations OATP1B1 shows substrate selectivity for estrone-3-sulfate...
  93. ncbi Contribution of organic anion transporting polypeptide OATP-C to hepatic elimination of the opioid pentapeptide analogue [D-Ala2, D-Leu5]-enkephalin
    Takashi Nozawa
    Department of Pharmaceutical Biology, Faculty of Pharmaceutical Sciences, Kanazawa University, Kanazawa, Japan
    J Pharm Pharmacol 55:1013-20. 2003
    ..Moreover, the inhibitory effects of various compounds, including some peptides, on [(3)H]estrone-3-sulfate uptake by OATP-C were similar to those observed in [(3)H]DADLE uptake by rat isolated hepatocytes...
  94. ncbi The development of a sensitive enzyme immunoassay for the determination of estrone and estradiol-17beta in bovine blood plasma based on the same homologous combination with antiserum and steroid-enzyme conjugate
    Naoki Takenouchi
    National Agricultural Research Center for Tohoku Region
    J Vet Med Sci 66:1315-21. 2004
    The development of a sensitive enzymeimmunoassay (EIA) for the determination of estrone (E1) and estradiol-17beta (E2 beta) in bovine plasma is described...
  95. ncbi Influence of oleoyl-estrone treatment on circulating testosterone. Role of 17beta-hydroxysteroid dehydrogenase isoenzymes
    M M Romero
    Department of Nutrition and Food Science, Faculty of Biology, University of Barcelona, Barcelona, Spain
    J Physiol Pharmacol 60:181-90. 2009
    Overweight male rats received oral oleoyl-estrone (OE) for 10 days, and were compared with controls...
  96. ncbi Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms
    Anthony J Lee
    Department of Basic Pharmaceutical Sciences, College of Pharmacy, University of South Carolina, Columbia, South Carolina 29208, USA
    Endocrinology 144:3382-98. 2003
    We systematically characterized the oxidative metabolites of 17beta-estradiol and estrone formed by 15 human cytochrome P450 (CYP) isoforms...
  97. ncbi Distribution of estrogens, 17beta-estradiol and estrone, in Canadian municipal wastewater treatment plants
    M R Servos
    Department of Biology, University of Waterloo, 200 University Ave W Waterloo, Ontario, Canada N2L 3G1
    Sci Total Environ 336:155-70. 2005
    The distribution of female hormones, 17beta-estradiol and estrone, was determined in effluents of 18 selected municipal treatment plants across Canada...
  98. ncbi The eighth and ninth transmembrane domains in organic anion transporting polypeptide 1B1 affect the transport kinetics of estrone-3-sulfate and estradiol-17beta-D-glucuronide
    Mayuko Miyagawa
    Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo, Japan
    J Pharmacol Exp Ther 329:551-7. 2009
    ..which some TMs of OATP1B1 were substituted with those of OATP1B3, and we investigated the transport kinetics of estrone-3-sulfate (E-sul; a substrate preferentially accepted by OATP1B1) and estradiol-17beta-D-glucuronide (EG; a ..
  99. ncbi Oleoyl-estrone increases adrenal corticosteroid synthesis gene expression in overweight male rats
    Maria Del Mar Romero
    Department of Nutrition and Food Science, Faculty of Biology, University of Barcelona, Av Diagonal, 645, 08028 Barcelona, Spain
    Steroids 75:20-6. 2010
    Oleoyl-estrone (OE) induces a marked loss of body fat in rats by maintaining energy expenditure, body protein and blood glucose despite decreasing food intake. OE increases glucocorticoids, but they arrest OE lipid-mobilization...
  100. ncbi Transcellular transport of organic anions across a double-transfected Madin-Darby canine kidney II cell monolayer expressing both human organic anion-transporting polypeptide (OATP2/SLC21A6) and Multidrug resistance-associated protein 2 (MRP2/ABCC2)
    Makoto Sasaki
    Department of Biopharmaceutics, School of Pharmaceutical Sciences, The University of Tokyo, 7 3 1 Hongo, Bunkyo ku, Tokyo 113 0033, Japan
    J Biol Chem 277:6497-503. 2002
    ..In contrast, basal-to-apical transport of estrone-3-sulfate and dehydroepiandrosterone sulfate, which are significantly transported by OATP2, but not by MRP2, was ..
  101. ncbi Transport of estrone 3-sulfate mediated by organic anion transporter OATP4C1: estrone 3-sulfate binds to the different recognition site for digoxin in OATP4C1
    Hiroaki Yamaguchi
    Department of Pharmaceutical Sciences, Tohoku University Hospital, 1 1 Seiryo machi, Aoba ku, Sendai, Japan
    Drug Metab Pharmacokinet 25:314-7. 2010
    ..However, little is known about the characteristics of OATP4C1-madiated transport. We examined the transport of estrone 3-sulfate, which is known as a substrate for other OATPs, by OATP4C1-expressing cells...

Research Grants63

  1. A Soft Topical Antiandrogenic Drug
    Wei Chu Xu; Fiscal Year: 2013
    ..Circulating T and DHT also serve as precursors of estrogens through their conversion to estradiol and estrone by aromatase...
  2. Novel treatment of menopausal hot flushes with an estradiol prodrug
    Laszlo Prokai; Fiscal Year: 2012
    ..We have shown earlier that para-quinol of estrone (Q-E1) functions as a pro-drug and following its absorption its is converted in selective tissues to E1 via an ..
  3. Green Tea and Reduction of Breast Cancer Risk
    MINDY SUSAN KURZER; Fiscal Year: 2013
    ..of breast cancer risk: mammographic density;plasma insulin-like growth factor 1 (IGF-1), IGF binding protein 3, estrone, estradiol, androstenedione and sex hormone binding globulin...
  4. Fnip1 Function in Lymphocyte Development, Activation and Metabolism
    Brian M Iritani; Fiscal Year: 2013
    ..abstract_text> ..
  5. Preconception Nutrition, Endocrine Disruptors, Reproductive Outcomes
    Xiaobin Wang; Fiscal Year: 2013
    ..obtained data critical to this proposal, including (1) Reproductive Hormones: pregnanediol-3-glucuronide (PdG), estrone conjugate (E1C), and human chorionic gonadotropin (b-hCG) assessed in daily first void urine samples of ..
  6. Role of the Sex Hormones and Insulin/IGF-Axes in Endometrial Cancer Recurrence
    Howard D Strickler; Fiscal Year: 2012
    ..EA recurrence with: (i) fasting serum levels of insulin, total and free IGF-I, IGF-II, IGFBP-1 and -3, estradiol, estrone, progesterone and sex hormone binding globulin (SHBG);(ii) tumor expression of IGF-I, IGF-II, IGFBP-1 and -3 mRNA ..
  7. Population-Based Reference Ranges for Estradiol and Estrone in Men
    VASAN S RAMACHANDRAN; Fiscal Year: 2013
    DESCRIPTION (provided by applicant): The role of estradiol 17[unreadable] (E2) and estrone (E1) - the two most abundant estrogens in humans - in men's health and disease remains poorly understood...
  8. Variations in Hormones During Menopause: Effects on Cognitive and Brain Aging
    Heather A Bimonte-Nelson; Fiscal Year: 2013
    ..Since Andro is directly converted to estrone, and we have shown estrone-induced memory impairments, we hypothesize that Andro's conversion to estrone ..
  9. Medications Development for the Pregnant Opiate Addict
    Mahmoud S Ahmed; Fiscal Year: 2010
    ..6. Determine the effects of BUP and methadone on the biosynthesis of estrogens (estrone, estradiol and estriol) by CYP19 during pregnancy...
  10. Estrogen-Derived Para-Quinol Intervention in Alzheimer's Disease
    Mary A Ottinger; Fiscal Year: 2010
    ..We will evaluate para-quinols derived chemically from estrone (E1-quinol) and 17b-estradiol (E2-quinol), respectively in a murine AD model...
  11. Role of folliculin (FLCN) in lung cell survival
    Vera P Krymskaya; Fiscal Year: 2013
    ....
  12. Effects of the circadian clock and light on the production of estrogens
    Steven W Lockley; Fiscal Year: 2010
    ..We have gathered some preliminary evidence to suggest that there is an endogenous circadian rhythm in urinary estrone-3-glucuronide with a day-time peak that is 12 hours out of phase with the urinary 6- sulphatoxymelatonin rhythm, ..
  13. Gender Disparity in Bladder Cancer and Chemopreventive Intervention
    Yuesheng Zhang; Fiscal Year: 2013
    ..of liver UGT1A3 may be desirable, since this enzyme may be physiologically important, such as metabolizing estrone. SF is a promising cancer-preventive agent and is selectively delivered to bladder tissue through urinary ..
  14. Phytoestrogen and Endogenous Estrogen Exposure and Risk of Stroke
    Xianglan Zhang; Fiscal Year: 2013
    ..levels of isoflavonoids, a biomarker of systemic exposure to phytoestrogens, and with blood levels of estradiol, estrone, testosterone, and sex hormone- binding globulin...
  15. The effects of randomized, low-dose hormone therapy on mammographic density in KE
    Rulla M Tamimi; Fiscal Year: 2013
    ..We will also examine if baseline mammographic density or circulating biomarkers including estradiol, estrone, and estrone sulfate, modify or mediate changes in breast density with HT...
  16. Molecular mechanisms that match lysosome function to cellular demand
    Shawn Ferguson; Fiscal Year: 2013
    ....
  17. SYNTHESIS OF STABLE ISOTOPE-LABELED STEROIDS FOR THE MEASUREMENT OF ENDOGENOUS S
    SCOTT LANDVATTER; Fiscal Year: 2011
    ..stable-isotope labeled key steroid hormones including 2-, 3-, and 4-methoxyestrogens, estriol, testosterone, estrone, estradiol, and androstenedione and dehydroepiandrosterone...
  18. SYNTHESIS OF STABLE ISOTOPE-LABELED STEROIDS FOR THE MEASUREMENT OF ENDOGENOUS S
    SCOTT LANDVATTER; Fiscal Year: 2009
    ..stable-isotope labeled key steroid hormones including 2-, 3-, and 4-methoxyestrogens, estriol, testosterone, estrone, estradiol, and androstenedione and dehydroepiandrosterone...
  19. BIOMEDICAL (BASIC)
    MARC JAMES GUNTER; Fiscal Year: 2009
    ..proposed investigation is, therefore, to evaluate the association of incident colorectal cancer with estradiol, estrone, progesterone and sex hormone binding globulin among women enrolled in the untreated arms of the WHI-CT (women ..
  20. The role of Folliculin, tumor suppressor mutated in BHD, in mTOR nutrient sensing
    Zhi Yang Tsun; Fiscal Year: 2013
    ..These insights will shed light on the pathogenesis of BHD and may lead to the rational development of novel therapies for cancer. ..
  21. Validation of Human Vaginal Tissue Assay for Endocrine Disruptors
    Seyoum Ayehunie; Fiscal Year: 2013
    ..The production of estrone by the tissue model and changes to tissue morphology and gene expression will be monitored as biomarkers of ED...
  22. STEROID METABOLISM AND ACTION IN CANCER
    Mortimer Levitz; Fiscal Year: 1993
    ..androst-5-ene-3 beta, 16 alpha, 17 beta-triol, 16 alpha--hydroxyestrone and the classical estrogens: estrone, estradiol, and estriol...
  23. Isomeric HRT estrogen-DNA adducts: Structure and Repair
    Nicholas Geacintov; Fiscal Year: 2009
    ..prescriptions in 2003 alone) contains the conjugated equine estrogens equilenin (EN), equilin, and 8,9-dehydro-estrone (total ~ 54% composition), and the endogenous estrone and 1713-estradiol...
  24. Bone Content and Metabolism of Sex Steroid Hormones
    STEPHEN BORST; Fiscal Year: 2009
    ..While bone estradiol is low, estrone and estrone sulfate are abundant...
  25. Estrogen Metabolism and Action in Prostate Cancer Etiology in PCPT
    Ashraful Hoque; Fiscal Year: 2007
    ..Our overall hypothesis is that increased serum androstenedione, estradiol and estrone and variations in genes that metabolize estrogens are associated with the finasteride-associated risk of high-..
  26. Effects of Soy on Estrogens in Breast Fluid and Urine
    Gertraud Maskarinec; Fiscal Year: 2010
    ..Estradiol and estrone will be measured in NAF and serum with an ultrasensitive radioimmunoassay, urinary estrogen metabolites by GC-MS, ..
  27. MENSTRUAL FUNCTION AND PHYSICAL AND MENTAL JOB STRESS
    Maureen Hatch; Fiscal Year: 1993
    ..To evaluate ovulatory and luteal function, urine samples will be analyzed for estrone-3-glucuronide (E1G), pregnanediol-3-glucuronide (pdG), luteinizing hormone (LH) and creatinine (Cr)...
  28. EPIDEMIOLOGY OF HORMONES AND OSTEOPOROSIS
    Lewis Kuller; Fiscal Year: 1991
    ..There was little relationship between androgen hormones, testosterone and androstenedione to cortical bone. Estrone concentrations, the primary postmenopausal estrogen were, however, significant predictors of cortical bone in ..
  29. EFFECT OF ETHANOL ON SEX HORMONES & HDL METABOLISM
    JEROME HOJNACKI; Fiscal Year: 1991
    ..2) to evaluate whether 12% ETOH consumed during a binge drinking cycle adversely affects LP's and sex huormones (estrone/T); 3) to determine if concurrent use of oral NIC negates the anti-atherogenic LP effect of 12% ETOH and how ..
  30. METABOLIC TRANSFORMATION OF STEROIDS IN BREAST CELLS
    Rajeshwari Mehta; Fiscal Year: 1992
    ..in the development and progression of breast cancer is well documented, but direct measurement of total plasma, estrone and estradiol does not show significantly higher estrogen levels in breast cancer patients than in controls...
  31. Male Reproductive Effects from Exposure to Boron
    Wendie Robbins; Fiscal Year: 2005
    ..markers including testosterone, free testosterone, serum hormone binding globulin, dihydrotestosterone, LH, FSH, estrone, estradiol, estriol; (2) describe the relationship between boron exposure and indirect measures of toxicity on ..
  32. STRUCTURE OF MICROSOMAL ENZYMES--ESTROGEN BIOSYN
    Debashis Ghosh; Fiscal Year: 2000
    ..cells are Cytochrome P450 Aromatase (P450arom), Type 1 17beta- Hydroxysteroid Dehydrogenase (17beta-HSD1) and Estrone/DHEA Sulfatase (ES)...
  33. FERTILE PERIOD PREDICTION WITH A TRIF BIOSENSOR
    JUDITH ERB; Fiscal Year: 1992
    ..This research would develop a fertile period prediction system based upon the presence of an increase in urinary estrone-3-glucuronide (E1-g) 72 hours prior to ovulation and an increase in pregnanediol glucuronide (Pd-g) following ..
  34. NEW YORK UNIVERSITY WOMENS HEALTH STUDY
    Paolo Toniolo; Fiscal Year: 2002
    ..initial observations of the NYU Women's Health Study showing a strong association between endogenous estrogens (estrone and estradiol) and post-menopausal breast cancer...
  35. Relationship Between AD Clinicopathological Changes and CNS Sex Steroid Hormones
    Jeremiah Kelly; Fiscal Year: 2009
    ..The study will quantify levels of testosterone, estradiol, androstenedione and estrone by high sensitivity radioimmunoassay and will quantify expression of cytochrome P450 aromatase using real-time RT-..
  36. STRUCTURE-FUNCTION OF STEROIDOGENIC CYTOCHROMES P-450
    John Shively; Fiscal Year: 1990
    ..One focus of our studies will be aromatase, the enzyme responsible for the conversion of androstenedione to estrone and testosterone to estradiol...
  37. Hormones During Weight Loss in Breast Cancer Survivors
    Cheryl Rock; Fiscal Year: 2004
    ..Obesity is associated with increased circulating concentrations of estrone and estradiol in postmenopausal women, and it also is associated with decreased levels of sex-hormone binding ..
  38. EPIDEMIOLOGY OF MENOPAUSE AND DEMENTIA IN DOWN SYNDROME
    Nicole Schupf; Fiscal Year: 2009
    ..e. serum estradiol, bioavailable estradiol, estrone, sex-hormone binding globulin, dehydroepiandrostcrone, follicle stimulating hormone and progesterone);(2) are ..
  39. OBESITY AND INFERTILITY IN THE LETHAL YELLOW MOUSE
    Maureen Diggins; Fiscal Year: 1991
    ..The contribution of body fat to blood estrone levels leading to chronically elevated estrogens in the obese mice will be determined by calculating the ratio of ..
  40. OVARIAN FUNCTION IN MARES CHRONICALLY TREATED WITH PZP
    Jay Kirkpatrick; Fiscal Year: 1992
    ..Urinary estrone conjugates (E1C) will be measured by enzyme immunoassay (EIA) in order to reflect plasma E2 concentrations...
  41. ESTROGEN AND INSULIN LIKE GROWTH FACTORS IN BREAST CANCE
    Herbert Yu; Fiscal Year: 2000
    ..Plasma samples of these 400 women will be measured for estradiol, estrone, estrone sulfate, testosterone, dehydroepiandrosterone sulfate (DHEA-S) IGF-I, IGF-II and IGFBP-3 using ..
  42. REPRODUCTIVE PHYSIOLOGY OF OVARIAN FAILURE
    Nanette Santoro; Fiscal Year: 1992
    ..by performing a long-term (12 month) longitudinal assessment of the daily urinary excretion of LH, FSH, estrone conjugates and pregnanediol glucuronide in 3 groups of women; two designed to represent the beginning (..
  43. PROSTATIC CANCER: GENETIC AND ENDOCRINE RISK FACTORS
    A Meikle; Fiscal Year: 1980
    ..We will determine whether (1) the plasma concentrations of sex steroids (estradiol-17beta, estrone, testosterone and dihydrotestosterone) and prolactin are abnormal in probands and first-order relatives as ..
  44. LEAD, ENDOCRINE DISRUPTION AND REPRODUCTIVE OUTCOMES
    Xiping Xu; Fiscal Year: 2000
    ..monitored by urinary hormone metabolites, including follicle-stimulating hormone (FSH), leutinizing hormone (LH), estrone conjugates (E1C), and pregnanediol-3-glucuronide (PdG)...
  45. EXERCISE EFFECT ON SEX HORMONES IN POSTMENOPAUSAL WOMEN
    Anne McTiernan; Fiscal Year: 2000
    ..Serum hormones will be assayed at baseline and at end-of-study. These hormones include: total estrone, total estradiol, free estradiol, percent bioavailable estradiol, estrone sulfate, sex hormone binding globulin, ..
  46. ENDOGENOUS ESTROGENS AND ENDOMETRIAL CANCER
    Anne Zeleniuch Jacquotte; Fiscal Year: 1999
    ..Serum samples will be assayed for estrone, estradiol, percent estradiol bound to sex hormone binding globulin and percent free estradiol...
  47. MRI OF BODY FAT, OVULATION AND ESTROGEN METABOLISM
    ROSE FRISCH; Fiscal Year: 1990
    ..Impedance Analysis; 3) Ovarian function will be monitored by urinary pregnanediol glucuronide, urinary estrone glucuronide, salivary progesterone and basal body temperature; 4) The extent of 2-hydroxylation of 17 beta-..
  48. SEX STEROID HORMONES AND RISK OF CHD IN WOMEN
    Kathryn Rexrode; Fiscal Year: 2002
    ..design, the investigators will measure baseline sex steroid hormone levels (serum total and free estradiol, estrone sulfate, total and free testosterone, dehydroepiandrosterone sulfate) and sex hormone binding globulin to ..
  49. MAMMARY ESTROGEN METABOLISM AND BREAST CANCER RISK
    Fritz Parl; Fiscal Year: 2004
    ..leads to the formation of catechol estrogens, the 2-OH and 4-OH derivatives of 17beta-estradiol (E2) and estrone (E1)...
  50. HORMONES AND RISK OF PROSTATIC HYPERLASIA
    Lois Monteiro; Fiscal Year: 1991
    ..and 400 controls will be retrieved and analyzed for testosterone, dihydrotestosterone, delta4-androstenedione, estrone, and estradiol...
  51. HORMONES IN THE EPIDEMIOLOGY OF PROSTATIC HYPERPLASIA
    Wendy Verhoek Oftedahl; Fiscal Year: 1992
    ..will be pooled and analyzed for free and bound testosterone, dehydrotestosterone, free and bound estradiol, estrone, delta4-androstenedione, androstanediol, and prolactin...
  52. Intra-Subject Hormone Variation
    Donald Brambilla; Fiscal Year: 2006
    ..SHBG, LH, prolactin, DHEA, DHEAS, cortisol, androstenedione, androstanediol glucoronide (3-alpha-diol G) and estrone) are included because of rapidly growing interest in their actions, and because it's cost-efficient also to ..
  53. RAPID METHOD FOR ANALYSIS OF ESTROGEN METABOLITES
    MINDY KURZER; Fiscal Year: 2000
    In addition to the major endogenous estrogens, specific estrogen metabolites (including 16alpha(OH) estrone, 4-(OH) estrone and 4-(OH) estradiol) are thought to be genotoxic and potentially carcinogenic in humans...
  54. ESTROGEN, CORTICOID, AND GONADOTROPIN IN OBESITY
    Barnett Zumoff; Fiscal Year: 1980
    ..3) Plasma estrogen levels are elevated in obese men and women, but the elevation is predominantly of estrone in men and of estradiol in women; this is hypothesized to be due to a sex difference in the set-point of the E2 ..
  55. CATECHOL ESTROGENS: PRODUCTION ACTION METABOLISM
    Christopher Longcope; Fiscal Year: 1980
    The catechol estrogens have been isolated from human urine as major metabolites of estrone and estradiol. They have been shown to possess biological activity both in vivo and in vitro in several animal systems...
  56. A-RING SUBSTITUTED ESTROGENS AS BREAST TUMOR INHIBITORS
    SAMUEL BROOKS; Fiscal Year: 1990
    ..Four-substitution on estrone by either nitro- or amine groups imparts carcinostatic properties to the molecule while diminishing the ..
  57. Modulation by dioxin of ovarian estrogen synthesis
    REINHOLD HUTZ; Fiscal Year: 2002
    ..will evaluate levels of mRNAs for ovarian CYP1A1 and 1B1, which preferentially catalyze estrogens (estradiol and estrone) to their 2-OH- and 4-OH metabolites, respectively; and separate any products chromatographically, in order to ..
  58. ESTROGEN METABOLITES EFFECTS ON BONE
    Russell Turner; Fiscal Year: 2002
    ..b>Estrone (E1) and its metabolites, 16alpha-Hydroxyl estrone ( (16alpha-OHE1) and 2-hydroxyesterone (2-OHE1), are the most ..
  59. GROWTH FACTORS AND THE BPH CHIMPANZEE MODEL
    Mitchell Steiner; Fiscal Year: 2001
    ..I and type II (TGFb RI and RII)] and their relationship to androgens (testosterone) and estrogens (estradiol and estrone) should provide important clues about the etiology and natural history of BPH...
  60. PROSTAGLANDIN F2ALPHA LUTEOTROPIC & LUTEOLYTIC EFFECTS
    JAMES HIXON; Fiscal Year: 1980
    ..The number of estrone implants will be increased between 230 and 250 days of gestation to mimic the increase in estrogen concentrations ..
  61. GENETIC HORMONAL AND BEHAVIORAL DETERMINANTS OF OBESITY
    Jennifer Hays; Fiscal Year: 2000
    ..1 (IGF-1) and its major binding protein (BP-3), dehydroepiandrosterone DHEA) and its sulfated conjugate (DHEAS), estrone, estradiol, and sex hormone-binding globulin (SHBG);and (iii) behavioral determinants of obesity, including ..
  62. URINARY ESTROGEN METABOLITES AND BREAST CANCER RISK
    Susan Hankinson; Fiscal Year: 2001
    ..As part of this project, we will evaluate a number of plasma estrogens (e.g., estradiol, estrone, estrone sulfate) and other hormones in relation to breast cancer risk in postmenopausal women...
  63. ESTROGEN/DNA ADDUCT ANALYSIS IN URINE
    MINDY KURZER; Fiscal Year: 2000
    In addition to the major endogenous estrogens, specific estrogen metabolites (including 16alpha(OH) estrone, 4-(OH) estrone, and 4-(OH) estradiol) are thought to be genotoxic and potentially carcinogenic in humans...