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. Vila R, Cabot C, Villarreal L, Monegal A, Ayet E, Romero M, et al. Oleoyl-estrone is a precursor of an estrone-derived ponderostat signal. J Steroid Biochem Mol Biol. 2011;124:99-111 pubmed publisher
    Oleoyl-estrone (OE) is a powerful anti-obesity compound that decreases food intake, decreases insulin resistance and circulating cholesterol...
  2. Castrillejo V, Romero M, Esteve M, Ardevol A, Blay M, Bladé C, et al. Antioxidant effects of a grapeseed procyanidin extract and oleoyl-estrone in obese Zucker rats. Nutrition. 2011;27:1172-6 pubmed publisher
    ..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 ..
  3. Isabelle M, Villemur R, Juteau P, Lepine F. Isolation of estrogen-degrading bacteria from an activated sludge bioreactor treating swine waste, including a strain that converts estrone to ?-estradiol. Can J Microbiol. 2011;57:559-68 pubmed publisher
    ..consortium from a swine wastewater biotreatment was enriched in the presence of low concentrations (1 mg/L) of estrone (E1), 17?-estradiol (?E2), and equol (EQO) as sole carbon sources...
  4. Izumi S, Nozaki Y, Komori T, Maeda K, Takenaka O, Kusano K, et al. Substrate-dependent inhibition of organic anion transporting polypeptide 1B1: comparative analysis with prototypical probe substrates estradiol-17?-glucuronide, estrone-3-sulfate, and sulfobromophthalein. Drug Metab Dispos. 2013;41:1859-66 pubmed publisher
    ..on the OATP1B1-mediated uptake of the prototypical substrates [³H]estradiol-17?-glucuronide (E?G), [³H]estrone-3-sulfate (E?S), and [³H]sulfobromophthalein (BSP) were studied in OATP1B1-transfected cells...
  5. Jasuja G, Travison T, Davda M, Rose A, Zhang A, Kushnir M, et al. Circulating estrone levels are associated prospectively with diabetes risk in men of the Framingham Heart Study. Diabetes Care. 2013;36:2591-6 pubmed publisher
    ..murine models, estrogen administration reduces diabetes risk; however, the relationship of estradiol and estrone to diabetes in men is poorly understood...
  6. Thayanukul P, Zang K, Janhom T, Kurisu F, Kasuga I, Furumai H. Concentration-dependent response of estrone-degrading bacterial community in activated sludge analyzed by microautoradiography-fluorescence in situ hybridization. Water Res. 2010;44:4878-87 pubmed publisher
    Inefficient removal of estrone (E1) in wastewater treatment plants (WWTPs) causes feminizing effects in male aquatic creatures...
  7. Rothman M, Carlson N, Xu M, Wang C, Swerdloff R, Lee P, et al. Reexamination of testosterone, dihydrotestosterone, estradiol and estrone levels across the menstrual cycle and in postmenopausal women measured by liquid chromatography-tandem mass spectrometry. Steroids. 2011;76:177-82 pubmed publisher
    ..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...
  8. Park H, Staehling K, Tsang M, Appleby M, Brunkow M, Margineantu D, et al. Disruption of Fnip1 reveals a metabolic checkpoint controlling B lymphocyte development. Immunity. 2012;36:769-81 pubmed publisher
  9. Li L, Sham Y, Bikadi Z, Elmquist W. pH-Dependent transport of pemetrexed by breast cancer resistance protein. Drug Metab Dispos. 2011;39:1478-85 pubmed publisher
    ..the study presented here, we examine the pH dependence of BCRP using methothrexate (MTX), pemetrexed (PMX), and estrone sulfate (ES) as model substrates...

More Information

Publications62

  1. Li N, Hong W, Huang H, Lu H, Lin G, Hong M. Identification of amino acids essential for estrone-3-sulfate transport within transmembrane domain 2 of organic anion transporting polypeptide 1B1. PLoS ONE. 2012;7:e36647 pubmed publisher
  2. Zhang C, Chen J, Yin D, Lin S. The contribution of 17beta-hydroxysteroid dehydrogenase type 1 to the estradiol-estrone ratio in estrogen-sensitive breast cancer cells. PLoS ONE. 2012;7:e29835 pubmed publisher
    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...
  3. Kis O, Zastre J, Ramaswamy M, Bendayan R. pH dependence of organic anion-transporting polypeptide 2B1 in Caco-2 cells: potential role in antiretroviral drug oral bioavailability and drug-drug interactions. J Pharmacol Exp Ther. 2010;334:1009-22 pubmed publisher
    ..b>Estrone-3-sulfate (E3S) uptake demonstrated biphasic saturation kinetics in Caco-2 cells, with dissociation constants (K(..
  4. Atkinson S, Marlatt V, Kimpe L, Lean D, Trudeau V, Blais J. Environmental factors affecting ultraviolet photodegradation rates and estrogenicity of estrone and ethinylestradiol in natural waters. Arch Environ Contam Toxicol. 2011;60:1-7 pubmed publisher
    ..To determine patterns of UV photodegradation for estrone (E1) and 17?-ethinylestradiol (EE2), water samples containing these compounds were exposed to levels of UVB ..
  5. Mazumdar M, Fournier D, Zhu D, Cadot C, Poirier D, Lin S. Binary and ternary crystal structure analyses of a novel inhibitor with 17beta-HSD type 1: a lead compound for breast cancer therapy. Biochem J. 2009;424:357-66 pubmed publisher
    ..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. ..
  6. Prutner W, Nicken P, Haunhorst E, Hamscher G, Steinberg P. Effects of single pesticides and binary pesticide mixtures on estrone production in H295R cells. Arch Toxicol. 2013;87:2201-14 pubmed publisher
    ..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...
  7. Strugała A, Jagodziński P. Conversion of estrone to 17 beta-estradiol in Jurkat acute T cell leukemia Hut-78 T- and Raji B lymphoma cell lines in vitro. Biomed Pharmacother. 2013;67:299-303 pubmed publisher
    ..type 1 (HSD17B1) transcript and protein and the production of 17 beta-estradiol (E2) from estrone (E1) in human Jurkat acute T cell leukemia, Hut-78 and Raji B lymphoma cells...
  8. Banerjee N, Allen C, Bendayan R. Differential role of organic anion-transporting polypeptides in estrone-3-sulphate uptake by breast epithelial cells and breast cancer cells. J Pharmacol Exp Ther. 2012;342:510-9 pubmed publisher
    ..b>Estrone-3-sulfate (E3S), a substrate for 7 of 11 OATPs, is a predominant source of tumor estrogen in postmenopausal, ..
  9. de Padua Mansur A, Silva T, Takada J, Avakian S, Strunz C, Machado César L, et al. Long-term prospective study of the influence of estrone levels on events in postmenopausal women with or at high risk for coronary artery disease. ScientificWorldJournal. 2012;2012:363595 pubmed publisher
    ..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...
  10. Lunardi G, Piccioli P, Bruzzi P, Notaro R, Lastraioli S, Serra M, et al. Plasma estrone sulfate concentrations and genetic variation at the CYP19A1 locus in postmenopausal women with early breast cancer treated with letrozole. Breast Cancer Res Treat. 2013;137:167-74 pubmed publisher
    ..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, ..
  11. Berényi A, Minorics R, Iványi Z, Ocsovszki I, Ducza E, Thole H, et al. Synthesis and investigation of the anticancer effects of estrone-16-oxime ethers in vitro. Steroids. 2013;78:69-78 pubmed publisher
    ..The aim of this study was to describe the cytotoxic effects of 63 newly synthetized estrone-16-oxime ethers on human cancer cell lines (cervix carcinoma HeLa, breast carcinoma MCF7 and skin epidermoid ..
  12. Stander A, Joubert F, Joubert A. Docking, synthesis, and in vitro evaluation of antimitotic estrone analogs. Chem Biol Drug Des. 2011;77:173-81 pubmed publisher
    ..Modifications at position 2' of estrone were made to include moieties that are known to improve the antimitotic activity of estradiol analogs...
  13. Giton F, Caron P, Bérubé R, Belanger A, Barbier O, Fiet J. 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). Clin Chim Acta. 2010;411:1208-13 pubmed publisher
    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...
  14. Bagot C, Marsh M, Whitehead M, Sherwood R, Roberts L, Patel R, et al. The effect of estrone on thrombin generation may explain the different thrombotic risk between oral and transdermal hormone replacement therapy. J Thromb Haemost. 2010;8:1736-44 pubmed publisher
    ..women, respectively, on thrombin generation, standard markers of thrombophilia, estradiol level and estrone level...
  15. Glaeser H, Mandery K, Sticht H, Fromm M, Konig J. Relevance of conserved lysine and arginine residues in transmembrane helices for the transport activity of organic anion transporting polypeptide 1B3. Br J Pharmacol. 2010;159:698-708 pubmed publisher
    Organic anion transporting polypeptide 1B3 (OATP1B3) (SLCO1B3) mediates the uptake of endogenous substrates (e.g. estrone-3-sulphate) and drugs (e.g. pravastatin) from blood into hepatocytes...
  16. Johnson N, Walker K, Gibson L, Orr N, Folkerd E, Haynes B, et al. CYP3A variation, premenopausal estrone levels, and breast cancer risk. J Natl Cancer Inst. 2012;104:657-69 pubmed publisher
    ..We measured urinary levels of estrone glucuronide (E1G) using a protocol specifically developed to account for cyclic variation in hormone levels ..
  17. Folkerd E, Dixon J, Renshaw L, A Hern R, Dowsett M. Suppression of plasma estrogen levels by letrozole and anastrozole is related to body mass index in patients with breast cancer. J Clin Oncol. 2012;30:2977-80 pubmed publisher
    To investigate whether suppression of plasma estradiol and estrone sulfate levels by the aromatase inhibitors (AIs) anastrozole and letrozole is related to body mass index (BMI) in postmenopausal women with early estrogen receptor (ER) -..
  18. Lønning P, Haynes B, Straume A, Dunbier A, Helle H, Knappskog S, et al. Recent data on intratumor estrogens in breast cancer. Steroids. 2011;76:786-91 pubmed publisher
    ..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...
  19. Mutsaers H, van den Heuvel L, Ringens L, Dankers A, Russel F, Wetzels J, et al. Uremic toxins inhibit transport by breast cancer resistance protein and multidrug resistance protein 4 at clinically relevant concentrations. PLoS ONE. 2011;6:e18438 pubmed publisher
    ..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. Lawrence Woo L, Leblond B, Purohit A, Potter B. Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors. Bioorg Med Chem. 2012;20:2506-19 pubmed publisher
    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...
  21. McClure R, Barha C, Galea L. 17?-Estradiol, but not estrone, increases the survival and activation of new neurons in the hippocampus in response to spatial memory in adult female rats. Horm Behav. 2013;63:144-57 pubmed publisher
    Estrogens fluctuate across the lifespan in women, with circulating 17?-estradiol levels higher pre-menopause than estrone and circulating estrone levels higher postmenopause than 17?-estradiol...
  22. Yamaguchi H, Sugie M, Okada M, Mikkaichi T, Toyohara T, Abe T, et al. Transport of estrone 3-sulfate mediated by organic anion transporter OATP4C1: estrone 3-sulfate binds to the different recognition site for digoxin in OATP4C1. Drug Metab Pharmacokinet. 2010;25:314-7 pubmed
    ..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...
  23. Caldwell D, Mastrocco F, Anderson P, Lange R, Sumpter J. Predicted-no-effect concentrations for the steroid estrogens estrone, 17?-estradiol, estriol, and 17?-ethinylestradiol. Environ Toxicol Chem. 2012;31:1396-406 pubmed publisher
    The authors derive predicted-no-effect concentrations (PNECs) for the steroid estrogens (estrone [E1], 17?-estradiol [E2], estriol [E3], and 17?-ethinylestradiol [EE2]) appropriate for use in risk assessment of aquatic organisms...
  24. Oster A, Klein T, Werth R, Kruchten P, Bey E, Negri M, et al. Novel estrone mimetics with high 17beta-HSD1 inhibitory activity. Bioorg Med Chem. 2010;18:3494-505 pubmed publisher
    17Beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) catalyzes the reduction of estrone into estradiol, which is the most potent estrogen in humans...
  25. Paliwal S, Paliwal R, Mishra N, Mehta A, Vyas S. A novel cancer targeting approach based on estrone anchored stealth liposome for site-specific breast cancer therapy. Curr Cancer Drug Targets. 2010;10:343-53 pubmed
    ..b>Estrone (ES) was anchored as ligand on to stealth liposome (ES-SL-DOX) for targeting to ERs...
  26. Jasuja G, Travison T, Davda M, Murabito J, Basaria S, Zhang A, et al. Age trends in estradiol and estrone levels measured using liquid chromatography tandem mass spectrometry in community-dwelling men of the Framingham Heart Study. J Gerontol A Biol Sci Med Sci. 2013;68:733-40 pubmed publisher
    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 ..
  27. Shah K, Nakao T, Kubota H, Maeda T. Peripartum changes in plasma estrone sulfate and estradiol-17beta profiles associated with and without the retention of fetal membranes in holstein-friesian cattle. J Reprod Dev. 2007;53:279-88 pubmed
    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 ..
  28. Lee W, Glaeser H, Smith L, Roberts R, Moeckel G, Gervasini G, et al. Polymorphisms in human organic anion-transporting polypeptide 1A2 (OATP1A2): implications for altered drug disposition and central nervous system drug entry. J Biol Chem. 2005;280:9610-7 pubmed
    ..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...
  29. Ferrer Lorente R, Cabot C, Fernández López J, Alemany M. Combined effects of oleoyl-estrone and a beta3-adrenergic agonist (CL316,243) on lipid stores of diet-induced overweight male Wistar rats. Life Sci. 2005;77:2051-8 pubmed
    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...
  30. Soodvilai S, Wright S, Dantzler W, Chatsudthipong V. Involvement of tyrosine kinase and PI3K in the regulation of OAT3-mediated estrone sulfate transport in isolated rabbit renal proximal tubules. Am J Physiol Renal Physiol. 2005;289:F1057-64 pubmed
    ..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...
  31. Cribb A, Knight M, Dryer D, Guernsey J, Hender K, Tesch M, et al. Role of polymorphic human cytochrome P450 enzymes in estrone oxidation. Cancer Epidemiol Biomarkers Prev. 2006;15:551-8 pubmed
    ..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...
  32. Rothnie A, Callaghan R, Deeley R, Cole S. Role of GSH in estrone sulfate binding and translocation by the multidrug resistance protein 1 (MRP1/ABCC1). J Biol Chem. 2006;281:13906-14 pubmed
    ..Unusually, transport of several MRP1 substrates requires glutathione (GSH). For example, estrone sulfate transport by MRP1 is stimulated by GSH, vincristine is co-transported with GSH, or GSH can be transported ..
  33. Vicker N, Lawrence H, Allan G, Bubert C, Smith A, Tutill H, et al. Focused libraries of 16-substituted estrone derivatives and modified e-ring steroids: inhibitors of 17beta-hydroxysteroid dehydrogenase type 1. ChemMedChem. 2006;1:464-81 pubmed
    ..1 (17beta-HSD1), an oxidoreductase which has a preferential reductive activity using NADPH as cofactor, converts estrone to estradiol and is expressed in many steroidogenic tissues including breast and in malignant breast cells...
  34. Adamec J, Beckert R, Weiss D, Klimesova V, Waisser K, Möllmann U, et al. Hybrid molecules of estrone: new compounds with potential antibacterial, antifungal, and antiproliferative activities. Bioorg Med Chem. 2007;15:2898-906 pubmed
    New hybrid molecules of estrone were synthesized as compounds indicating promising biological activity (antibacterial, antimycobacterial, antifungal, and antiproliferative)...
  35. Kruchten P, Werth R, Bey E, Oster A, Marchais Oberwinkler S, Frotscher M, et al. Selective inhibition of 17beta-hydroxysteroid dehydrogenase type 1 (17betaHSD1) reduces estrogen responsive cell growth of T47-D breast cancer cells. J Steroid Biochem Mol Biol. 2009;114:200-6 pubmed publisher
    ..17beta-Hydroxysteroid dehydrogenase type 1 (17betaHSD1) catalyses the NADPH-dependent E2-formation from estrone (E1). It is often overexpressed in breast cancer and endometriosis...
  36. Shareef A, Angove M, Wells J, Johnson B. Sorption of bisphenol A, 17alpha-ethynylestradiol and estrone to mineral surfaces. J Colloid Interface Sci. 2006;297:62-9 pubmed
    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 ..
  37. Muir M, Romalo G, Wolf L, Elger W, Schweikert H. Estrone sulfate is a major source of local estrogen formation in human bone. J Clin Endocrinol Metab. 2004;89:4685-92 pubmed
    b>Estrone sulfate (E1S) is the most abundant estrogen in the circulation of adults...
  38. Binder G, Iliev D, Dufke A, Wabitsch M, Schweizer R, Ranke M, et al. Dominant transmission of prepubertal gynecomastia due to serum estrone excess: hormonal, biochemical, and genetic analysis in a large kindred. J Clin Endocrinol Metab. 2005;90:484-92 pubmed
    ..The mother of the proband had normal age at menarche and no macromastia. Estrone levels of the proband and the other affected boys were elevated, 17beta-estradiol levels were high-normal, and ..
  39. Takenouchi N, Oshima K, Shimada K, Takahashi M. 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. J Vet Med Sci. 2004;66:1315-21 pubmed
    The development of a sensitive enzymeimmunoassay (EIA) for the determination of estrone (E1) and estradiol-17beta (E2 beta) in bovine plasma is described...
  40. Gui C, Hagenbuch B. Role of transmembrane domain 10 for the function of organic anion transporting polypeptide 1B1. Protein Sci. 2009;18:2298-306 pubmed publisher
    ..However, at low concentrations OATP1B1 shows substrate selectivity for estrone-3-sulfate...
  41. Miyagawa M, Maeda K, Aoyama A, Sugiyama Y. 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. J Pharmacol Exp Ther. 2009;329:551-7 pubmed publisher
    ..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 ..
  42. Kakusaka S, Asayama M, Kaihara A, Sasano T, Suzuki T, Kurokawa J, et al. A receptor-independent effect of estrone sulfate on the HERG channel. J Pharmacol Sci. 2009;109:152-6 pubmed
    ..other estrogens have the same effect as that of 17beta-estradiol, we investigated receptor-independent effects of estrone, estrone 3-sulfate, and estriol on hERG currents in patch-clamped estrogen-negative HEK293 cells...
  43. Thibaudeau J, Lepine J, Tojcic J, Duguay Y, Pelletier G, Plante M, et al. Characterization of common UGT1A8, UGT1A9, and UGT2B7 variants with different capacities to inactivate mutagenic 4-hydroxylated metabolites of estradiol and estrone. Cancer Res. 2006;66:125-33 pubmed
    The oxidative metabolism of estrone (E1) and estradiol (E2) to form carcinogenic 4-hydroxy-catecholestrogens (4-OHCE) is associated with uterine and breast carcinogenesis...
  44. Eliassen A, Missmer S, Tworoger S, Hankinson S. Circulating 2-hydroxy- and 16alpha-hydroxy estrone levels and risk of breast cancer among postmenopausal women. Cancer Epidemiol Biomarkers Prev. 2008;17:2029-35 pubmed publisher
    ..Blood samples, collected in 1989 to 1990, were assayed for 2-OH and 16alpha-OH estrone among 340 cases and 677 matched controls not taking postmenopausal hormones...
  45. Gui C, Miao Y, Thompson L, Wahlgren B, Mock M, Stieger B, et al. Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3. Eur J Pharmacol. 2008;584:57-65 pubmed publisher
    ..Transport of estrone-3-sulfate was hardly affected while all other substrates tested were inhibited...
  46. Brozic P, Lanisnik Risner T, Gobec S. Inhibitors of 17beta-hydroxysteroid dehydrogenase type 1. Curr Med Chem. 2008;15:137-50 pubmed
    ..The thoroughly characterized 17beta-hydroxysteroid dehydrogenase type 1 activates the less active estrone to estradiol, a potent ligand for estrogen receptors...
  47. Geisler J, Ekse D, Helle H, Duong N, Lønning P. An optimised, highly sensitive radioimmunoassay for the simultaneous measurement of estrone, estradiol and estrone sulfate in the ultra-low range in human plasma samples. J Steroid Biochem Mol Biol. 2008;109:90-5 pubmed publisher
    ..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...
  48. Salas A, Esteve M, Mar Grasa M, Remesar X. Rats treated with oleoyl-oestrone maintain glucidic homeostasis: comparisons with a pair-fed model. Br J Nutr. 2005;94:738-45 pubmed
  49. Geisler J, Lønning P. Endocrine effects of aromatase inhibitors and inactivators in vivo: review of data and method limitations. J Steroid Biochem Mol Biol. 2005;95:75-81 pubmed
    ..or, alternatively, by measuring their ability to inhibit the conversion of tracer-labelled androstenedione into estrone. While contemporary methods for estrogen measurement (with the exception of estrone sulphate) lack the ..
  50. Motylewska E, Mełeń Mucha G. Estrone and progesterone inhibit the growth of murine MC38 colon cancer line. J Steroid Biochem Mol Biol. 2009;113:75-9 pubmed publisher
    ..The aim of this study was to examine the direct effects of various concentrations of estrone and progesterone (10(-4) to 10(-12)M) applied alone or together with FU on the growth of murine MC38 colon cancer ..
  51. Meyer zu Schwabedissen H, Tirona R, Yip C, Ho R, Kim R. Interplay between the nuclear receptor pregnane X receptor and the uptake transporter organic anion transporter polypeptide 1A2 selectively enhances estrogen effects in breast cancer. Cancer Res. 2008;68:9338-47 pubmed publisher
    ..with its role as a hormone uptake transporter, induction of OATP1A2 was associated with increased uptake of estrone 3-sulfate. The rifampin response was abrogated after small interfering RNA targeting of PXR...
  52. Johnson A, Williams R. A model to estimate influent and effluent concentrations of estradiol, estrone, and ethinylestradiol at sewage treatment works. Environ Sci Technol. 2004;38:3649-58 pubmed
    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...
  53. Noe J, Portmann R, Brun M, Funk C. Substrate-dependent drug-drug interactions between gemfibrozil, fluvastatin and other organic anion-transporting peptide (OATP) substrates on OATP1B1, OATP2B1, and OATP1B3. Drug Metab Dispos. 2007;35:1308-14 pubmed
    ..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...