Page last updated: 2024-09-03

estrone-3-o-sulfamate and estrone

estrone-3-o-sulfamate has been researched along with estrone in 51 studies

Compound Research Comparison

Studies
(estrone-3-o-sulfamate)
Trials
(estrone-3-o-sulfamate)
Recent Studies (post-2010)
(estrone-3-o-sulfamate)
Studies
(estrone)
Trials
(estrone)
Recent Studies (post-2010) (estrone)
8901510,2664321,372

Protein Interaction Comparison

ProteinTaxonomyestrone-3-o-sulfamate (IC50)estrone (IC50)
Estrogen receptorHomo sapiens (human)0.1261
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)6.589
17-beta-hydroxysteroid dehydrogenase type 1Homo sapiens (human)0.4134
Sodium-dependent serotonin transporterHomo sapiens (human)5.301
Estrogen receptor betaHomo sapiens (human)0.3743
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)3

Research

Studies (51)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's13 (25.49)18.2507
2000's30 (58.82)29.6817
2010's8 (15.69)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Billich, A; Nussbaumer, P; Winiski, AP1
Kim, BM; Liu, Y; Mostafa, Y; Phan, CM; Taylor, SD1
Cortés-Benítez, F; Dutour, R; Poirier, D; Roy, J1
Howarth, NM; Potter, BV; Purohit, A; Reed, MJ; Williams, GJ1
Potter, BV; Purohit, A; Reed, MJ; Roberts, CJ; Williams, GJ1
Duncan, LJ; Potter, BV; Purohit, A; Reed, MJ; Roberts, CJ; Singh, A; Williams, GJ1
Dauvois, S; Parker, MG; Potter, BV; Purohit, A; Reed, MJ; Williams, GJ1
Jagannathan, S; Johnson, DA; Li, PK; Rhodes, ME1
Lightowler, M; Potter, BV; Purohit, A; Reed, MJ; Woo, LW1
Hidalgo Aragones, MI; Parish, D; Potter, BV; Pouton, CW; Purohit, A; Reed, MJ; Sahm, UG1
Howarth, NM; Potter, BV; Purohit, A; Reed, MJ1
Bodmer, M; Brand, H; Foulkes, R; Leonard, J; Porter, JP; Shaw, S; Suitters, AJ; Wales, MR; Woodger, R1
Froome, VA; Potter, BV; Purohit, A; Reed, MJ; Wang, DY1
Parker, MG; Potter, BV; Purohit, A; Reed, MJ1
Hejaz, HA; Hummelinck, AE; Potter, BV; Purohit, A; Reed, MJ; Vernon, KA; Woo, LW1
Farr, SA; Flood, JF; Johnson, DA; Li, PK; Morley, JE1
Dunphy, G; Ely, DL; Lib, PK; Turner, M; Valigora, SD1
Malini, B; Potter, BV; Purohit, A; Reed, MJ; Woo, LL1
MacCarthy-Morrogh, L; Packham, G; Purohit, A; Reed, MJ; Townsend, PA1
Barth, A; Oettel, M; Römer, W1
Bonser, J; Franks, S; Mason, HD; Potter, BV; Purohit, A; Reed, MJ; Walker, J; Willis, DS1
Ahmed, S; James, K; Owen, CP; Patel, CK; Patel, M3
de Gooyer, ME; Ederveen, AG; Kleyn, GT; Kloosterboer, HJ; Smits, KC; Verheul, HA1
Ahmed, S; James, K; Owen, CP; Patel, CK; Patel, MB1
Billich, A; Hoffmann, R; Niiyama, S; Rot, A1
Ahmed, S; James, K; Owen, CP; Patel, CK1
Ahmed, S; James, K; Owen, CP2
Kabler, H; Li, PK; Sarap, J; Selcer, KW; Xiao, Z1
Fischer, DS; Mahon, MF; Potter, BV; Purohit, A; Reed, MJ; Woo, LW1
Chander, SK; Fenton, JC; Fischer, DS; Potter, BV; Purohit, A; Reed, MJ; Woo, LW1
Casini, A; Montero, JL; Scozzafava, A; Supuran, CT; Vullo, D; Winum, JY1
Ganeshapillai, D; Ho, YT; Leese, MP; Newman, SP; Potter, BV; Purohit, A; Reed, MJ; Robinson, JJ; Vicker, N; Woo, LW1
Fujii, T; Iwashita, S; Koizumi, N; Nakagawa, T; Okada, M; Takegawa, S1
Abbate, F; Casini, A; Montero, JL; Potter, BV; Scozzafava, A; Supuran, CT; Winum, JY1
Chander, SK; Potter, BV; Purohit, A; Reed, MJ; Woo, LW1
Newman, SP; Potter, BV; Purohit, A; Reed, MJ; Woo, LW1
Day, JM; Potter, BV; Purohit, A; Raobaikady, B; Reed, MJ1
Leblond, B; Leese, MP; Newman, SP; Potter, BV; Purohit, A; Reed, MJ1
Acharya, KR; Ho, YT; Lloyd, MD; Potter, BV; Purohit, A; Reed, MJ; Sutcliffe, OB; Thiyagarajan, N; Woo, LW1
Akaike, A; Kaneko, S; Katsuki, H; Kume, T; Shirakawa, H1
Numazawa, M; Tada, Y; Tominaga, T; Watari, Y1
Parsons, MF; Purohit, A; Raobaikady, B; Reed, MJ1
Acharya, KR; Baker, MD; Cozier, GE; Leese, MP; Lloyd, MD; Potter, BV; Thiyagarajan, N1
Ishida, H; Nakata, T; Shiotsu, Y1
Lawrence Woo, LW; Leblond, B; Potter, BV; Purohit, A1
Edwards, DR; Wolfenden, R1
Potter, BV; Thomas, MP2

Reviews

4 review(s) available for estrone-3-o-sulfamate and estrone

ArticleYear
The role of cytokines and sulphatase inhibitors in regulating oestrogen synthesis in breast tumours.
    The Journal of steroid biochemistry and molecular biology, 1995, Volume: 53, Issue:1-6

    Topics: Breast Neoplasms; Cytokines; Dehydroepiandrosterone; Dehydroepiandrosterone Sulfate; Estradiol Dehydrogenases; Estrogens; Estrone; Fibroblast Growth Factor 2; Growth Substances; Humans; In Vitro Techniques; Insulin-Like Growth Factor I; Interleukin-2; Lymphocytes; Macrophages; Sulfatases; Transforming Growth Factor alpha; Tumor Cells, Cultured

1995
Steroid sulfatase: molecular biology, regulation, and inhibition.
    Endocrine reviews, 2005, Volume: 26, Issue:2

    Topics: Animals; Breast Neoplasms; Clinical Trials, Phase I as Topic; Coumarins; Enzyme Inhibitors; Estrone; Female; Humans; Models, Molecular; Neoplasms, Hormone-Dependent; Steryl-Sulfatase; Sulfonamides; Sulfonic Acids

2005
[Steroid sulfatase inhibitor].
    Nihon rinsho. Japanese journal of clinical medicine, 2010, Volume: 68, Issue:6

    Topics: Animals; Breast Neoplasms; Clinical Trials as Topic; Coumarins; Drug Design; Enzyme Inhibitors; Estradiol; Estrogens; Estrone; Female; Humans; Steryl-Sulfatase; Sulfonamides

2010
Estrogen O-sulfamates and their analogues: Clinical steroid sulfatase inhibitors with broad potential.
    The Journal of steroid biochemistry and molecular biology, 2015, Volume: 153

    Topics: Animals; Coumarins; Enzyme Inhibitors; Estradiol; Estrogens; Estrone; Humans; Models, Molecular; Steryl-Sulfatase; Sulfonamides

2015

Other Studies

47 other study(ies) available for estrone-3-o-sulfamate and estrone

ArticleYear
Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase.
    Journal of medicinal chemistry, 2003, Nov-06, Volume: 46, Issue:23

    Topics: Benzopyrans; Binding, Competitive; Breast Neoplasms; Cell Division; Cell Line, Tumor; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Estrogen Receptor alpha; Estrogen Receptor beta; Estrogens; Female; Fluorescence Polarization; Humans; Ligands; Receptors, Estrogen; Steryl-Sulfatase; Structure-Activity Relationship; Sulfonic Acids

2003
Inhibition of steroid sulfatase with 4-substituted estrone and estradiol derivatives.
    Bioorganic & medicinal chemistry, 2011, Oct-15, Volume: 19, Issue:20

    Topics: Breast Neoplasms; Enzyme Inhibitors; Estradiol; Estrone; Female; Humans; Kinetics; Placenta; Pregnancy; Steryl-Sulfatase

2011
Targeting cytochrome P450 (CYP) 1B1 with steroid derivatives.
    Bioorganic & medicinal chemistry letters, 2016, 11-01, Volume: 26, Issue:21

    Topics: Cytochrome P-450 CYP1B1; Cytochrome P-450 Enzyme Inhibitors; Estrogens; Humans; Inhibitory Concentration 50; Molecular Docking Simulation; Structure-Activity Relationship

2016
Inactivation of steroid sulfatase by an active site-directed inhibitor, estrone-3-O-sulfamate.
    Biochemistry, 1995, Sep-12, Volume: 34, Issue:36

    Topics: Arylsulfatases; Binding Sites; Breast Neoplasms; Enzyme Inhibitors; Estrone; Female; Humans; Hydrogen-Ion Concentration; Hydrolysis; Kinetics; Microsomes; Placenta; Steryl-Sulfatase; Substrate Specificity; Tumor Cells, Cultured

1995
In vivo inhibition of oestrone sulphatase and dehydroepiandrosterone sulphatase by oestrone-3-O-sulphamate.
    International journal of cancer, 1995, Sep-27, Volume: 63, Issue:1

    Topics: Animals; Arylsulfatases; Dose-Response Relationship, Drug; Enzyme Inhibitors; Estradiol; Estrone; Female; Fulvestrant; Liver; Mammary Neoplasms, Experimental; Rats; Rats, Wistar; Steryl-Sulfatase; Sulfatases; Tamoxifen; Time Factors

1995
The hydrolysis of oestrone sulphate and dehydroepiandrosterone sulphate by human steroid sulphatase expressed in transfected COS-1 cells.
    The Journal of steroid biochemistry and molecular biology, 1994, Volume: 50, Issue:1-2

    Topics: Animals; Arylsulfatases; Catalysis; Cell Line; Chlorocebus aethiops; Dehydroepiandrosterone; Dehydroepiandrosterone Sulfate; Estrogens, Conjugated (USP); Estrone; Female; Humans; Hydrolysis; Placenta; Steryl-Sulfatase; Transfection

1994
Reversal of scopolamine induced amnesia in rats by the steroid sulfatase inhibitor estrone-3-O-sulfamate.
    Brain research. Cognitive brain research, 1995, Volume: 2, Issue:4

    Topics: Amnesia; Animals; Arylsulfatases; Dehydroepiandrosterone; Dehydroepiandrosterone Sulfate; Enzyme Inhibitors; Estrone; Male; Rats; Reaction Time; Scopolamine; Steryl-Sulfatase

1995
Heteroatom-substituted analogues of the active-site directed inhibitor estra-1,3,5(10)-trien-17-one-3-sulphamate inhibit estrone sulphatase by a different mechanism.
    The Journal of steroid biochemistry and molecular biology, 1996, Volume: 57, Issue:1-2

    Topics: Chromatography, High Pressure Liquid; Dose-Response Relationship, Drug; Enzyme Inhibitors; Estrone; Female; Humans; Models, Biological; Models, Chemical; Placenta; Structure-Activity Relationship; Sulfatases

1996
Pharmacokinetics of oestrone-3-O-sulphamate.
    The Journal of steroid biochemistry and molecular biology, 1996, Volume: 58, Issue:5-6

    Topics: Animals; Enzyme Inhibitors; Estrone; Female; Rats; Rats, Wistar; Sulfatases

1996
Estrone sulfonates as inhibitors of estrone sulfatase.
    Steroids, 1997, Volume: 62, Issue:4

    Topics: Chromatography, Thin Layer; Enzyme Inhibitors; Estrone; Magnetic Resonance Spectroscopy; Naphthols; Structure-Activity Relationship; Sulfatases; Sulfonic Acids

1997
Immune enhancing effects of dehydroepiandrosterone and dehydroepiandrosterone sulphate and the role of steroid sulphatase.
    Immunology, 1997, Volume: 91, Issue:2

    Topics: Adjuvants, Immunologic; Animals; Arylsulfatases; Dehydroepiandrosterone; Dehydroepiandrosterone Sulfate; Dermatitis, Contact; Dexamethasone; Enzyme Inhibitors; Estrone; Male; Mice; Mice, Inbred BALB C; Oxazolone; Steryl-Sulfatase

1997
Measurement of oestrone sulphatase activity in white blood cells to monitor in vivo inhibition of steroid sulphatase activity by oestrone-3-O-sulphamate.
    The Journal of steroid biochemistry and molecular biology, 1997, Volume: 62, Issue:1

    Topics: Animals; Carbon Radioisotopes; Enzyme Inhibitors; Estrone; Female; Humans; Kinetics; Leukocytes; Liver; Male; Metabolic Clearance Rate; Rats; Reproducibility of Results; Scintillation Counting; Spleen; Sulfatases; Tissue Distribution; Tritium

1997
Steroid sulphatase: expression, isolation and inhibition for active-site identification studies.
    Chemico-biological interactions, 1998, Feb-20, Volume: 109, Issue:1-3

    Topics: Animals; Arylsulfatases; Binding Sites; CHO Cells; Cricetinae; Enzyme Inhibitors; Estrone; Humans; Steryl-Sulfatase

1998
The development of A-ring modified analogues of oestrone-3-O-sulphamate as potent steroid sulphatase inhibitors with reduced oestrogenicity.
    The Journal of steroid biochemistry and molecular biology, 1998, Volume: 64, Issue:5-6

    Topics: Animals; Arylsulfatases; Breast Neoplasms; Enzyme Inhibitors; Estrone; Female; Microsomes; Molecular Structure; Organ Size; Ovariectomy; Placenta; Rats; Rats, Inbred Strains; Steryl-Sulfatase; Uterus

1998
Peripheral steroid sulfatase inhibition potentiates improvement of memory retention for hippocampally administered dehydroepiandrosterone sulfate but not pregnenolone sulfate.
    Psychoneuroendocrinology, 1999, Volume: 24, Issue:8

    Topics: Animals; Arylsulfatases; Avoidance Learning; Brain Mapping; Dehydroepiandrosterone Sulfate; Dose-Response Relationship, Drug; Drug Synergism; Enzyme Inhibitors; Estrone; Hippocampus; Injections; Male; Maze Learning; Mice; Pregnenolone; Retention, Psychology; Steryl-Sulfatase

1999
Steroid sulfatase inhibitor alters blood pressure and steroid profiles in hypertensive rats.
    The Journal of steroid biochemistry and molecular biology, 2000, Volume: 73, Issue:3-4

    Topics: Animals; Arylsulfatases; Corticosterone; Enzyme Inhibitors; Estrogens; Estrone; Female; Male; Rats; Rats, Inbred SHR; Rats, Inbred WKY; Steryl-Sulfatase; Testosterone

2000
Potent active site-directed inhibition of steroid sulphatase by tricyclic coumarin-based sulphamates.
    Chemistry & biology, 2000, Volume: 7, Issue:10

    Topics: Alanine; Antineoplastic Agents; Arylsulfatases; Binding Sites; Breast Neoplasms; Coumarins; Dehydroepiandrosterone Sulfate; Dose-Response Relationship, Drug; Estrone; Female; Glycine; Heterocyclic Compounds, 3-Ring; Humans; Hydrogen Bonding; Kinetics; Microsomes; Models, Molecular; Placenta; Postmenopause; Steryl-Sulfatase; Structure-Activity Relationship; Sulfatases; Sulfonamides; Sulfonic Acids

2000
Differential effects of estrone and estrone-3-O-sulfamate derivatives on mitotic. Arrest, apoptosis, and microtubule assembly in human breast cancer cells.
    Cancer research, 2000, Oct-01, Volume: 60, Issue:19

    Topics: Antineoplastic Agents; Apoptosis; Breast Neoplasms; Cell Cycle; Cell Division; Estrone; Humans; Hydroxyestrones; Microtubules; Mitosis; Tubulin; Tumor Cells, Cultured

2000
Influence of subchronic administration of oestrone-3-O-sulphamate on oestrone sulphatase activity in liver, spleen and white blood cells of ovariectomized rats.
    Archives of toxicology, 2000, Volume: 74, Issue:7

    Topics: Administration, Oral; Animals; Animals, Outbred Strains; Body Weight; Enzyme Inhibitors; Estrone; Female; Injections, Subcutaneous; Leukocytes; Microsomes, Liver; Organ Size; Ovariectomy; Rats; Rats, Wistar; Spleen; Sulfatases; Toxicity Tests; Uterus

2000
Human granulosa cells are a site of sulphatase activity and are able to utilize dehydroepiandrosterone sulphate as a precursor for oestradiol production.
    The Journal of endocrinology, 2000, Volume: 167, Issue:3

    Topics: Androstenedione; Cells, Cultured; Dehydroepiandrosterone; Dehydroepiandrosterone Sulfate; Enzyme Inhibitors; Estradiol; Estrone; Female; Granulosa Cells; Humans; Insulin; Luteinizing Hormone; Progesterone; Sulfatases

2000
Novel inhibitors of the enzyme estrone sulfatase (ES).
    Bioorganic & medicinal chemistry letters, 2001, Mar-26, Volume: 11, Issue:6

    Topics: Alkanes; Coumarins; Enzyme Inhibitors; Estrone; Inhibitory Concentration 50; Ketones; Mesylates; Sulfatases; Sulfonamides; Sulfonic Acids

2001
Acid dissociation constant, a potential physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES).
    Bioorganic & medicinal chemistry letters, 2001, Apr-09, Volume: 11, Issue:7

    Topics: Estrogens; Estrone; Inhibitory Concentration 50; Kinetics; Phenols; Structure-Activity Relationship; Sulfatases; Sulfonic Acids

2001
Hydrophobicity, a physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES).
    Bioorganic & medicinal chemistry letters, 2001, Sep-17, Volume: 11, Issue:18

    Topics: Chemistry, Physical; Coumarins; Enzyme Inhibitors; Estrone; Inhibitory Concentration 50; Models, Biological; Models, Chemical; Structure-Activity Relationship; Sulfatases; Sulfonamides

2001
Tibolone: a compound with tissue specific inhibitory effects on sulfatase.
    Molecular and cellular endocrinology, 2001, Oct-25, Volume: 183, Issue:1-2

    Topics: Animals; Antineoplastic Agents, Hormonal; Breast; Cell Line; Endometrium; Enzyme Inhibitors; Estrone; Female; Humans; Norpregnenes; Organ Specificity; Osteoblasts; Sulfatases; Tumor Cells, Cultured

2001
Determination and use of a transition state for the enzyme estrone sulfatase (ES) from a proposed reaction mechanism.
    Bioorganic & medicinal chemistry letters, 2001, Dec-03, Volume: 11, Issue:23

    Topics: Catalytic Domain; Coumarins; Enzyme Inhibitors; Estrone; Inhibitory Concentration 50; Models, Molecular; Protein Conformation; Structure-Activity Relationship; Sulfatases; Sulfonamides; Sulfonic Acids

2001
Steroid sulfatase in the human hair follicle concentrates in the dermal papilla.
    The Journal of investigative dermatology, 2001, Volume: 117, Issue:6

    Topics: Adult; Alopecia; Androgens; Arylsulfatases; Dehydroepiandrosterone Sulfate; Dihydrotestosterone; Enzyme Inhibitors; Estrone; Female; Hair Follicle; Humans; Immunohistochemistry; In Vitro Techniques; Male; Steryl-Sulfatase; Tritium

2001
Synthesis and biochemical evaluation of novel and potent inhibitors of the enzyme oestrone sulphatase (ES).
    The Journal of steroid biochemistry and molecular biology, 2002, Volume: 80, Issue:4-5

    Topics: Coumarins; Dose-Response Relationship, Drug; Enzyme Inhibitors; Estrone; Humans; Hydrolysis; Inhibitory Concentration 50; Kinetics; Microsomes; Models, Chemical; Placenta; Spectrophotometry, Infrared; Sulfatases; Sulfonamides; Time Factors

2002
The design, synthesis, and biochemical evaluation of derivatives of biphenyl sulfamate-based compounds as novel inhibitors of estrone sulfatase.
    Biochemical and biophysical research communications, 2002, May-31, Volume: 294, Issue:1

    Topics: Catalysis; Coumarins; Enzyme Inhibitors; Estrone; Models, Chemical; Models, Molecular; Sulfatases; Sulfonamides

2002
Inhibition of steryl sulfatase activity in LNCaP human prostate cancer cells.
    Steroids, 2002, Volume: 67, Issue:10

    Topics: Arylsulfatases; Breast Neoplasms; Danazol; Dehydroepiandrosterone Sulfate; Enzyme Inhibitors; Estrone; Female; Humans; Kinetics; Male; Microsomes; Prostatic Neoplasms; Steryl-Sulfatase; Sulfonamides; Tumor Cells, Cultured; Tyramine

2002
Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES).
    The Journal of steroid biochemistry and molecular biology, 2002, Volume: 82, Issue:4-5

    Topics: Coumarins; Drug Design; Enzyme Inhibitors; Estrone; Inhibitory Concentration 50; Kinetics; Models, Chemical; Models, Molecular; Molecular Conformation; Molecular Mimicry; Structure-Activity Relationship; Sulfatases; Sulfonamides; Sulfonic Acids

2002
D-ring modified estrone derivatives as novel potent inhibitors of steroid sulfatase.
    Bioorganic & medicinal chemistry, 2003, Apr-17, Volume: 11, Issue:8

    Topics: Crystallography, X-Ray; Enzyme Inhibitors; Estrone; Humans; Inhibitory Concentration 50; Microsomes; Molecular Structure; Placenta; Reference Standards; Steryl-Sulfatase; Structure-Activity Relationship

2003
Novel D-ring modified steroid derivatives as potent, non-estrogenic, steroid sulfatase inhibitors with in vivo activity.
    The Journal of steroid biochemistry and molecular biology, 2003, Volume: 84, Issue:2-3

    Topics: Animals; Arylsulfatases; Breast Neoplasms; Chromatography, Thin Layer; Enzyme Inhibitors; Estrogens; Estrone; Female; Inhibitory Concentration 50; Liver; Models, Chemical; Ovary; Rats; Rats, Wistar; Steryl-Sulfatase; Time Factors

2003
Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes I and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors.
    Journal of medicinal chemistry, 2003, May-22, Volume: 46, Issue:11

    Topics: Antigens, Neoplasm; Arylsulfatases; Biomarkers, Tumor; Carbonic Anhydrase I; Carbonic Anhydrase II; Carbonic Anhydrase IX; Carbonic Anhydrases; Cytosol; Enzyme Inhibitors; Estrone; Humans; Membrane Proteins; Neoplasm Proteins; Steryl-Sulfatase; Structure-Activity Relationship; Sulfonic Acids

2003
Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamates.
    Biochemical and biophysical research communications, 2003, Jun-13, Volume: 305, Issue:4

    Topics: Antineoplastic Agents; Binding Sites; Carbonic Anhydrase II; Carbonic Anhydrase Inhibitors; Estrone; Humans; Inhibitory Concentration 50; Models, Molecular; Steroids; Sulfonamides

2003
Development of novel steroid sulfatase inhibitors. I. Synthesis and biological evaluation of biphenyl-4-O-sulfamates.
    The Journal of steroid biochemistry and molecular biology, 2003, Volume: 87, Issue:2-3

    Topics: Animals; Biphenyl Compounds; Breast Neoplasms; Cell Line, Tumor; Enzyme Inhibitors; Estradiol; Estrogen Receptor alpha; Estrone; Female; Humans; Liver; Organ Size; Rats; Rats, Sprague-Dawley; Receptors, Estrogen; Steryl-Sulfatase; Structure-Activity Relationship; Sulfonic Acids; Uterus

2003
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase.
    Bioorganic & medicinal chemistry letters, 2004, Jan-05, Volume: 14, Issue:1

    Topics: Carbonic Anhydrase II; Carbonic Anhydrase Inhibitors; Crystallography, X-Ray; Estrone; Humans; Isoenzymes; Steryl-Sulfatase

2004
The role of steroid sulphatase in regulating the oestrogenicity of oestrogen sulphamates.
    Biochemical and biophysical research communications, 2004, Sep-10, Volume: 322, Issue:1

    Topics: Animals; Coumarins; Drug Combinations; Estrogens; Estrone; Female; Homeostasis; Organ Size; Ovariectomy; Rats; Rats, Wistar; Steryl-Sulfatase; Sulfonamides; Sulfonic Acids; Uterus

2004
The nature of inhibition of steroid sulphatase activity by tibolone and its metabolites.
    The Journal of steroid biochemistry and molecular biology, 2005, Volume: 94, Issue:1-3

    Topics: Enzyme Inhibitors; Estrogen Replacement Therapy; Estrone; Female; Humans; Kinetics; Microsomes; Norpregnenes; Placenta; Pregnancy; Steryl-Sulfatase

2005
Anti-cancer activities of novel D-ring modified 2-substituted estrogen-3-O-sulfamates.
    The Journal of steroid biochemistry and molecular biology, 2005, Volume: 94, Issue:1-3

    Topics: Antineoplastic Agents; Breast Neoplasms; Cell Division; Cell Line, Tumor; Estrone; Female; Humans; Kinetics; Structure-Activity Relationship

2005
First crystal structures of human carbonic anhydrase II in complex with dual aromatase-steroid sulfatase inhibitors.
    Biochemistry, 2005, May-10, Volume: 44, Issue:18

    Topics: Aromatase Inhibitors; Binding Sites; Carbonic Anhydrase II; Crystallization; Crystallography, X-Ray; Dimethyl Sulfoxide; Drug Stability; Enzyme Stability; Estrone; Humans; Ligands; Recombinant Proteins; Solvents; Steryl-Sulfatase

2005
Pregnenolone sulphate attenuates AMPA cytotoxicity on rat cortical neurons.
    The European journal of neuroscience, 2005, Volume: 21, Issue:9

    Topics: alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid; Animals; Cerebral Cortex; Drug Interactions; Drug Synergism; Enzyme Inhibitors; Estrone; Excitatory Amino Acid Agonists; Membrane Potentials; Neurons; Neuroprotective Agents; Organ Culture Techniques; Pregnenolone; Rats; Rats, Wistar; Receptors, AMPA; Steryl-Sulfatase

2005
Inhibition of estrone sulfatase by aromatase inhibitor-based estrogen 3-sulfamates.
    Steroids, 2006, Volume: 71, Issue:5

    Topics: Aromatase Inhibitors; Estrone; Humans; Microsomes; Molecular Conformation; Placenta; Stereoisomerism; Structure-Activity Relationship; Sulfatases; Time Factors

2006
Tibolone and its delta-4, 7alpha-methyl norethisterone metabolite are reversible inhibitors of human aromatase.
    The Journal of steroid biochemistry and molecular biology, 2007, Volume: 104, Issue:3-5

    Topics: Aromatase; Aromatase Inhibitors; Dose-Response Relationship, Drug; Estrone; Humans; Models, Biological; Norethindrone; Norpregnenes; Time Factors; Tumor Cells, Cultured

2007
Structures of human carbonic anhydrase II/inhibitor complexes reveal a second binding site for steroidal and nonsteroidal inhibitors.
    Biochemistry, 2010, Apr-27, Volume: 49, Issue:16

    Topics: Bicarbonates; Binding Sites; Carbon Dioxide; Carbonic Anhydrase II; Colorimetry; Enzyme Inhibitors; Estrone; Humans; Kinetics; Models, Molecular; Protein Conformation

2010
Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors.
    Bioorganic & medicinal chemistry, 2012, Apr-15, Volume: 20, Issue:8

    Topics: Enzyme Inhibitors; Estrone; Humans; Molecular Structure; Stereoisomerism; Steryl-Sulfatase; Structure-Activity Relationship

2012
Proton-in-flight mechanism for the spontaneous hydrolysis of N-methyl O-phenyl sulfamate: implications for the design of steroid sulfatase inhibitors.
    The Journal of organic chemistry, 2012, May-04, Volume: 77, Issue:9

    Topics: Arylsulfatases; Catalysis; Coumarins; Esters; Estrone; Hydrogen-Ion Concentration; Hydrolysis; Kinetics; Molecular Structure; Steryl-Sulfatase; Sulfonamides; Sulfonic Acids

2012
Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health.
    Journal of medicinal chemistry, 2015, Oct-08, Volume: 58, Issue:19

    Topics: Animals; Antineoplastic Agents; Aromatase Inhibitors; Breast Neoplasms; Drug Discovery; Endometriosis; Estrone; Female; Humans; Male; Molecular Targeted Therapy; Prostatic Neoplasms; Steryl-Sulfatase; Sulfonic Acids; Tubulin Modulators

2015