Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 2. Clinical considerations and new agents.
暂无分享,去创建一个
[1] L. Short,et al. Photochemical synthesis of N-arylbenzophenanthridine selective estrogen receptor modulators (serms). , 2001, Journal of medicinal chemistry.
[2] D. Thompson,et al. Droloxifene, a new estrogen antagonist/agonist, prevents bone loss in ovariectomized rats. , 1995, Endocrinology.
[3] P. Matthias,et al. Estrogen Receptor (ER)-α, but Not ER-β, Mediates Regulation of the Insulin-like Growth Factor I Gene by Antiestrogens* , 2001, The Journal of Biological Chemistry.
[4] T. Hunter,et al. Protein kinase B/Akt-mediated phosphorylation promotes nuclear exclusion of the winged helix transcription factor FKHR1. , 1999, Proceedings of the National Academy of Sciences of the United States of America.
[5] S. Hilsenbeck,et al. The importance of tamoxifen metabolism in tamoxifen-stimulated breast tumor growth , 2004, Cancer Chemotherapy and Pharmacology.
[6] E. di Salle,et al. Antiestrogenic and antitumor properties of the new triphenylethylene derivative toremifene in the rat. , 1990, Journal of steroid biochemistry.
[7] S. Safe,et al. Differential Interaction of the Methoxychlor Metabolite 2,2-Bis-(p-Hydroxyphenyl)-1,1,1-Trichloroethane with Estrogen Receptors α and β1. , 1999, Endocrinology.
[8] D. Shapiro,et al. Activation of the p38 mitogen-activated protein kinase pathway by estrogen or by 4-hydroxytamoxifen is coupled to estrogen receptor-induced apoptosis. , 2000, The Journal of biological chemistry.
[9] C. Labrie,et al. Effect of Dehydroepiandrosterone on Bone Mass, Serum Lipids, and Dimethylbenz(a)anthracene-Induced Mammary Carcinoma in the Rat. , 1997, Endocrinology.
[10] B. O’Malley,et al. Antiestrogen can establish nonproductive receptor complexes and alter chromatin structure at target enhancers. , 1991, Proceedings of the National Academy of Sciences of the United States of America.
[11] R. Blamey,et al. Combined tamoxifen and luteinizing hormone-releasing hormone (LHRH) agonist versus LHRH agonist alone in premenopausal advanced breast cancer: a meta-analysis of four randomized trials. , 2001, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[12] J. Simard,et al. (S)-(+)-4-[7-(2,2-dimethyl-1-oxopropoxy)-4-methyl-2-[4-[2-(1-piperidinyl)-ethoxy]phenyl]-2H-1-benzopyran-3-yl]-phenyl 2,2-dimethylpropanoate (EM-800): a highly potent, specific, and orally active nonsteroidal antiestrogen. , 1997, Journal of medicinal chemistry.
[13] M. Tattersall,et al. Diethylstilbestrol revisited in advanced breast cancer management. , 1990, Medical and pediatric oncology.
[14] C. Labrie,et al. Synthesis and biological activity of new halo-steroidal antiestrogens. , 1991, Journal of medicinal chemistry.
[15] B. Katzenellenbogen,et al. Coactivator peptides have a differential stabilizing effect on the binding of estrogens and antiestrogens with the estrogen receptor. , 1999, Molecular endocrinology.
[16] D. Thompson,et al. Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene. , 1998, Journal of medicinal chemistry.
[17] V. Jordan,et al. Effect of steroidal and nonsteroidal antiestrogens on the growth of a tamoxifen-stimulated human endometrial carcinoma (EnCa101) in athymic mice. , 1990, Cancer research.
[18] P. Webb,et al. An Antiestrogen-responsive Estrogen Receptor-α Mutant (D351Y) Shows Weak AF-2 Activity in the Presence of Tamoxifen* , 2000, The Journal of Biological Chemistry.
[19] M. Perilä,et al. A new triphenylethylene compound, Fc-1157a , 1986, Cancer Chemotherapy and Pharmacology.
[20] K. Korach,et al. The mechanism of ICI 164,384 antiestrogenicity involves rapid loss of estrogen receptor in uterine tissue. , 1991, Endocrinology.
[21] B. Katzenellenbogen,et al. Novel Ligands that Function as Selective Estrogens or Antiestrogens for Estrogen Receptor-α or Estrogen Receptor-β. , 1999, Endocrinology.
[22] V. Jordan,et al. Structure-function relationships of hydroxylated metabolites of tamoxifen that control the proliferation of estrogen-responsive T47D breast cancer cells in vitro. , 1990, Molecular pharmacology.
[23] G. Leclercq,et al. Derivatives of tamoxifen. Dependence of antiestrogenicity on the 4-substituent. , 1989, Journal of medicinal chemistry.
[24] J. Pento,et al. Nonsteroidal estrogens and antiestrogens: biological activity of cyclopropyl analogs of stilbene and stilbenediol. , 1981, Journal of pharmaceutical sciences.
[25] S. Robinson,et al. Estradiol-stimulated growth of MCF-7 tumors implanted in athymic mice: a model to study the tumoristatic action of tamoxifen. , 1988, Journal of steroid biochemistry.
[26] A. deFazio,et al. Activation of the Ras signalling pathway in human breast cancer cells overexpressing erbB-2. , 1994, Oncogene.
[27] V. Jordan,et al. Molecular classification of estrogens. , 2001, Cancer research.
[28] B. O’Malley,et al. Partial hormone resistance in mice with disruption of the steroid receptor coactivator-1 (SRC-1) gene. , 1998, Science.
[29] L. Moore,et al. 3-[4-(1,2-Diphenylbut-1-enyl)phenyl]acrylic acid: a non-steroidal estrogen with functional selectivity for bone over uterus in rats. , 1994, Journal of medicinal chemistry.
[30] R. Sutherland,et al. Cyclin D1 induction in breast cancer cells shortens G1 and is sufficient for cells arrested in G1 to complete the cell cycle. , 1994, Proceedings of the National Academy of Sciences of the United States of America.
[31] V. Jordan,et al. Structural components necessary for the antiestrogenic activity of tamoxifen. , 1989, Journal of steroid biochemistry.
[32] M. Dowsett,et al. Pyrrolidino-4-iodotamoxifen and 4-iodotamoxifen, new analogues of the antiestrogen tamoxifen for the treatment of breast cancer. , 1991, Cancer research.
[33] Y. Yarden,et al. Cyclin D1 Is Required for Transformation by Activated Neu and Is Induced through an E2F-Dependent Signaling Pathway , 2000, Molecular and Cellular Biology.
[34] Y. K. Hodges,et al. Estrogen Receptors α and β Prevalence of Estrogen Receptor β mRNA in Human Vascular Smooth Muscle and Transcriptional Effects , 2000 .
[35] K. Korach,et al. Tissue Distribution and Quantitative Analysis of Estrogen Receptor-α (ERα) and Estrogen Receptor-β (ERβ) Messenger Ribonucleic Acid in the Wild-Type and ERα-Knockout Mouse. , 1997, Endocrinology.
[36] A. Kauppila,et al. Comparison between the effects of tamoxifen and toremifene on the uterus in postmenopausal breast cancer patients. , 1995, Gynecologic oncology.
[37] J. Simard,et al. Characterization of the effects of the novel non‐steroidal antiestrogen EM‐800 on basal and estrogen‐induced proliferation of T‐47D, ZR‐75‐1 and MCF‐7 human breast cancer cells in vitro , 1997, International journal of cancer.
[38] M. Dowsett,et al. Idoxifene: report of a phase I study in patients with metastatic breast cancer. , 1995, Cancer research.
[39] J Lippman,et al. MCF7/LCC9: an antiestrogen-resistant MCF-7 variant in which acquired resistance to the steroidal antiestrogen ICI 182,780 confers an early cross-resistance to the nonsteroidal antiestrogen tamoxifen. , 1997, Cancer research.
[40] J. Gustafsson,et al. Estrogen receptor β acts as a dominant regulator of estrogen signaling , 2000, Oncogene.
[41] B. Katzenellenbogen,et al. Antagonists Selective for Estrogen Receptor ␣ , 2022 .
[42] R. Erikson,et al. Protein kinase activity associated with the avian sarcoma virus src gene product. , 1978, Proceedings of the National Academy of Sciences of the United States of America.
[43] C. Osborne,et al. Effect of estrogens and antiestrogens on growth of human breast cancer cells in athymic nude mice. , 1985, Cancer research.
[44] F. Labrie,et al. Inhibitory effects of medroxyprogesterone acetate (MPA) and the pure antiestrogen EM-219 on estrone (E1)-stimulated growth of dimethylbenz(a)anthracene (DMBA)-induced mammary carcinoma in the rat , 1995, Breast Cancer Research and Treatment.
[45] R Bucourt,et al. New biospecific adsorbents for the purification of estradiol receptor. , 1978, The Journal of biological chemistry.
[46] Jonathan A. Cooper,et al. Tyr527 is phosphorylated in pp60c-src: implications for regulation. , 1986, Science.
[47] S. Durani,et al. Structure-activity relationship of antiestrogens. Effect of the side chain and its position on the activity of 2,3-diaryl-2H-1-benzopyrans. , 1990, Journal of medicinal chemistry.
[48] V. Jordan,et al. Pharmacology of tamoxifen in laboratory animals. , 1980, Cancer treatment reports.
[49] Virgile Richard,et al. EM-652 (SCH 57068), a third generation SERM acting as pure antiestrogen in the mammary gland and endometrium , 1999, The Journal of Steroid Biochemistry and Molecular Biology.
[50] V. Paralkar,et al. Effects of CP-336,156, a New, Nonsteroidal Estrogen Agonist/Antagonist, on Bone, Serum Cholesterol, Uterus, and Body Composition in Rat Models. , 1998, Endocrinology.
[51] M. Dowsett,et al. Phase I/II study of the anti-oestrogen zindoxifene (D16726) in the treatment of advanced breast cancer. A Cancer Research Campaign Phase I/II Clinical Trials Committee study. , 1990, British Journal of Cancer.
[52] T. Willson,et al. Circumventing tamoxifen resistance in breast cancers using antiestrogens that induce unique conformational changes in the estrogen receptor. , 2001, Cancer research.
[53] S. Robinson,et al. Antitumor actions of toremifene in the 7,12-dimethylbenzanthracene (DMBA)-induced rat mammary tumor model. , 1988, European journal of cancer & clinical oncology.
[54] L. Jin,et al. Evaluation of estrogen receptor, antiestrogen binding sites and calmodulin for antiestrogen resistance of two clones derived from the MCF-7 breast cancer cell line. , 1994, Biochemical pharmacology.
[55] M. Dewhirst,et al. Tamoxifen inhibits angiogenesis in estrogen receptor-negative animal models. , 2000, Clinical cancer research : an official journal of the American Association for Cancer Research.
[56] L. Holmberg,et al. Prognostic and predictive value of c-erbB-2 overexpression in primary breast cancer, alone and in combination with other prognostic markers. , 1998, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[57] P. Satyaswaroop,et al. Human endometrial adenocarcinoma transplanted into nude mice: growth regulation by estradiol. , 1983, Science.
[58] Chris P. Miller,et al. Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. , 2001, Journal of medicinal chemistry.
[59] B. Hennig,et al. Antiestrogens inhibit endothelial cell growth stimulated by angiogenic growth factors. , 1996, Anticancer research.
[60] A. Lykkesfeldt,et al. Effect of estrogen and antiestrogens on cell proliferation and synthesis of secreted proteins in the human breast cancer cell line MCF-7 and a tamoxifen resistant variant subline, AL-1. , 1992, Acta oncologica.
[61] M. Dowsett,et al. Antiproliferative effects of idoxifene in a placebo-controlled trial in primary human breast cancer. , 2000, Clinical cancer research : an official journal of the American Association for Cancer Research.
[62] Y. Ma,et al. Effects of droloxifene on prevention of cancellous bone loss and bone turnover in the axial skeleton of aged, ovariectomized rats. , 1995, Bone.
[63] M Carlquist,et al. Structural insights into the mode of action of a pure antiestrogen. , 2001, Structure.
[64] C. Osborne,et al. Forkhead Homologue in Rhabdomyosarcoma Functions as a Bifunctional Nuclear Receptor-interacting Protein with Both Coactivator and Corepressor Functions* , 2001, The Journal of Biological Chemistry.
[65] I. Ellis,et al. Epidermal growth factor receptor expression in breast cancer: Association with response to endocrine therapy , 2004, Breast Cancer Research and Treatment.
[66] C. Sonnenschein,et al. Identification of human estrogen-inducible transcripts that potentially mediate the apoptotic response in breast cancer , 2000, The Journal of Steroid Biochemistry and Molecular Biology.
[67] B. Rattel,et al. Preclinical data for Droloxifene. , 1994, Cancer letters.
[68] V. Jordan,et al. Determination and pharmacology of a new hydroxylated metabolite of tamoxifen observed in patient sera during therapy for advanced breast cancer. , 1983, Cancer research.
[69] G. Rijksen,et al. c‐Src PROTEIN EXPRESSION IS INCREASED IN HUMAN BREAST CANCER. AN IMMUNOHISTOCHEMICAL AND BIOCHEMICAL ANALYSIS , 1996, The Journal of pathology.
[70] M. Lohuizen,et al. The secrets of selective estrogen receptor modulation: cell-specific coregulation. , 2002, Cancer cell.
[71] B. Katzenellenbogen,et al. Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues. , 2001, Journal of medicinal chemistry.
[72] M. Dowsett,et al. Idoxifene antagonizes estradiol-dependent MCF-7 breast cancer xenograft growth through sustained induction of apoptosis. , 1999, Cancer research.
[73] B. Katzenellenbogen,et al. Transcription Activation by the Human Estrogen Receptor Subtypeβ (ERβ) Studied with ERβ and ERα Receptor Chimeras* *This work was supported by NIH Grants CA-18119 and CA-60514 (to B.S.K.). , 1998, Endocrinology.
[74] V. Müller,et al. A New Interpretation of Antiestrogen Action a , 1995, Annals of the New York Academy of Sciences.
[75] M. Lippman,et al. Isolation and characterization of a tamoxifen-resistant cell line derived from MCF-7 human breast cancer cells. , 1981, The Journal of biological chemistry.
[76] H. Degani,et al. Tamoxifen enhances cell death in implanted MCF7 breast cancer by inhibiting endothelium growth. , 1994, Cancer research.
[77] W. Muller,et al. Mammary tumors expressing the neu proto-oncogene possess elevated c-Src tyrosine kinase activity , 1994, Molecular and cellular biology.
[78] Interaction and dissociation by ligands of estrogen receptor and Hsp90: the antiestrogen RU 58668 induces a protein synthesis-dependent clustering of the receptor in the cytoplasm. , 1998, Molecular endocrinology.
[79] N. Knebel,et al. 1-(aminoalkyl)-2-phenylindoles as novel pure estrogen antagonists. , 1990, Journal of medicinal chemistry.
[80] B. Pittman,et al. LAS, a novel selective estrogen receptor modulator with chemopreventive and therapeutic activity in the N-nitroso-N-methylurea-induced rat mammary tumor model. , 2001, Cancer research.
[81] C. Labrie,et al. Morphological Changes Induced by 6-Month Treatment of Intact and Ovariectomized Mice with Tamoxifen and the Pure Antiestrogen EM-800. , 1997, Endocrinology.
[82] Weiya Ma,et al. p38 Kinase Mediates UV-induced Phosphorylation of p53 Protein at Serine 389* , 1999, The Journal of Biological Chemistry.
[83] S. Nicosia,et al. MEKK1 activation of human estrogen receptor alpha and stimulation of the agonistic activity of 4-hydroxytamoxifen in endometrial and ovarian cancer cells. , 2000, Molecular endocrinology.
[84] A. Wakeling,et al. Novel antioestrogens without partial agonist activity. , 1988, Journal of steroid biochemistry.
[85] B. Haynes,et al. Metabolism of the 4-iodo derivative of tamoxifen by isolated rat hepatocytes. Demonstration that the iodine atom reduces metabolic conversion and identification of four metabolites. , 1990, Biochemical pharmacology.
[86] P. C. Ruenitz,et al. Antiestrogens. 3. Estrogen receptor affinities and antiproliferative effects in MCF-7 cells of phenolic analogues of trioxifene, [3,4-dihydro-2-(4- methoxyphenyl)-1-naphthalenyl][4-[2-(1-pyrrolidinyl)ethoxy]- phenyl]methanone. , 1992, Journal of medicinal chemistry.
[87] J. Carroll,et al. A Pure Estrogen Antagonist Inhibits Cyclin E-Cdk2 Activity in MCF-7 Breast Cancer Cells and Induces Accumulation of p130-E2F4 Complexes Characteristic of Quiescence* , 2000, The Journal of Biological Chemistry.
[88] R. Plevin,et al. Stress-activated protein kinases: activation, regulation and function. , 1997, Cellular signalling.
[89] D. Bentrem,et al. Analysis of cross-resistance of the selective estrogen receptor modulators arzoxifene (LY353381) and LY117018 in tamoxifen-stimulated breast cancer xenografts. , 2001, Clinical cancer research : an official journal of the American Association for Cancer Research.
[90] M. Madsen,et al. Resistance of human breast‐cancer cells to the pure steroidal anti‐estrogen ICI 182,780 is not associated with a general loss of estrogen‐receptor expression or lack of estrogen responsiveness , 1997, International journal of cancer.
[91] P. Sismondi,et al. Cyclophosphamide, methotrexate, and fluorouracil versus tamoxifen plus ovarian suppression as adjuvant treatment of estrogen receptor-positive pre-/perimenopausal breast cancer patients: results of the Italian Breast Cancer Adjuvant Study Group 02 randomized trial. boccardo@hp380.ist.unige.it. , 2000, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[92] B. Katzenellenbogen,et al. Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-alpha-selective agonists. , 2000, Journal of medicinal chemistry.
[93] R. Sutherland,et al. Effects of oestrogens on cell proliferation and cell cycle kinetics. A hypothesis on the cell cycle effects of antioestrogens. , 1983, European journal of cancer & clinical oncology.
[94] C. Benz,et al. Pharmacokinetics of toremifene and its metabolites in patients with advanced breast cancer , 2004, Cancer Chemotherapy and Pharmacology.
[95] V. Jordan,et al. Alteration of endocrine parameters in premenopausal women with breast cancer during long-term adjuvant therapy with tamoxifen as the single agent. , 1991, Journal of the National Cancer Institute.
[96] D. Miles,et al. Overexpression of c-erbB2 is an independent marker of resistance to endocrine therapy in advanced breast cancer , 1999, British Journal of Cancer.
[97] D. McDonnell,et al. The Human Estrogen Receptor-α Is a Ubiquitinated Protein Whose Stability Is Affected Differentially by Agonists, Antagonists, and Selective Estrogen Receptor Modulators* , 2001, The Journal of Biological Chemistry.
[98] R. Sutherland,et al. Inducible overexpression of cyclin D1 in breast cancer cells reverses the growth-inhibitory effects of antiestrogens. , 1997, Clinical cancer research : an official journal of the American Association for Cancer Research.
[99] S. Robinson,et al. Antiestrogenic action of toremifene on hormone-dependent, -independent, and heterogeneous breast tumor growth in the athymic mouse. , 1989, Cancer research.
[100] E. Baulieu,et al. Structural differences between the hormone and antihormone estrogen receptor complexes bound to the hormone response element. , 1991, Proceedings of the National Academy of Sciences of the United States of America.
[101] G. Teutsch,et al. RU 58 668, a new pure antiestrogen inducing a regression of human mammary carcinoma implanted in nude mice , 1994, The Journal of Steroid Biochemistry and Molecular Biology.
[102] G. Leclercq,et al. Synthesis and estrogen receptor binding of 6,7-dihydro-8-phenyl-9-[4-[2-(dimethylamino)ethoxy] phenyl]-5H-benzocycloheptene, a nonisomerizable analogue of tamoxifen. X-ray crystallographic studies. , 1986, Journal of medicinal chemistry.
[103] P. Goss,et al. Aromatase inhibitors in the treatment and prevention of breast cancer. , 2001, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[104] David A. Agard,et al. Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism , 2002, Nature Structural Biology.
[105] D. Thompson,et al. Lasofoxifene (CP-336,156), a selective estrogen receptor modulator, prevents bone loss induced by aging and orchidectomy in the adult rat. , 2000, Endocrinology.
[106] D. Fowlkes,et al. Comparative Analyses of Mechanistic Differences Among Antiestrogens1. , 1999, Endocrinology.
[107] D. Bentrem,et al. Effects of the new selective estrogen receptor modulator LY353381.HCl (Arzoxifene) on human endometrial cancer growth in athymic mice. , 2001, Clinical cancer research : an official journal of the American Association for Cancer Research.
[108] G. Teutsch,et al. RU 58668: Further in vitro and in vivo pharmacological data related to its antitumoral activity , 1996, The Journal of Steroid Biochemistry and Molecular Biology.
[109] D. Wolf,et al. A laboratory model to explain the survival advantage observed in patients taking adjuvant tamoxifen therapy. , 1993, Recent results in cancer research. Fortschritte der Krebsforschung. Progres dans les recherches sur le cancer.
[110] W. Dougall,et al. Intermolecular association and trans-phosphorylation of different neu-kinase forms permit SH2-dependent signaling and oncogenic transformation. , 1995, Oncogene.
[111] S. Venitt,et al. Genotoxic potential of tamoxifen and analogues in female Fischer F344/n rats, DBA/2 and C57BL/6 mice and in human MCL-5 cells. , 1992, Carcinogenesis.
[112] J. Zalcberg,et al. Induction of insulin‐like growth factor binding protein expression by ICI 182,780 in a tamoxifen‐resistant human breast cancer cell line , 1999, Breast Cancer Research and Treatment.
[113] E. Alarid,et al. Proteasome-mediated proteolysis of estrogen receptor: a novel component in autologous down-regulation. , 1999, Molecular endocrinology.
[114] I. Ellis,et al. Expression of ras p21, p53 and c-erbB-2 in advanced breast cancer and response to first line hormonal therapy. , 1995, British Journal of Cancer.
[115] I. Merchenthaler,et al. The Distribution of Estrogen Receptor-β mRNA in Forebrain Regions of the Estrogen Receptor-α Knockout Mouse. , 1997, Endocrinology.
[116] B. Katzenellenbogen,et al. Response-specific antiestrogen resistance in a newly characterized MCF-7 human breast cancer cell line resulting from long-term exposure to trans-hydroxytamoxifen , 1996, The Journal of Steroid Biochemistry and Molecular Biology.
[117] M. Green,et al. Multicenter phase II efficacy trial of toremifene in tamoxifen-refractory patients with advanced breast cancer. , 1993, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[118] V. Jordan,et al. Stable transfection of protein kinase C alpha cDNA in hormone-dependent breast cancer cell lines , 2000, British Journal of Cancer.
[119] B. Katzenellenbogen,et al. The quinone reductase gene: a unique estrogen receptor-regulated gene that is activated by antiestrogens. , 1997, Proceedings of the National Academy of Sciences of the United States of America.
[120] K. Hemminki,et al. Selective Estrogenic Effects of a Novel Triphenylethylene Compound, FC1271a, on Bone, Cholesterol Level, and Reproductive Tissues in Intact and Ovariectomized Rats1. , 2000, Endocrinology.
[121] G. Stancel,et al. Identification of functional estrogen response elements in the gene coding for the potent angiogenic factor vascular endothelial growth factor. , 2000, Cancer research.
[122] V. Jordan,et al. Nonsteroidal antiestrogens: their biological effects and potential mechanisms of action. , 1978, Journal of toxicology and environmental health.
[123] T. Hunter,et al. Transforming gene product of Rous sarcoma virus phosphorylates tyrosine , 1980, Proceedings of the National Academy of Sciences.
[124] A. Howell,et al. Investigation of a new pure antiestrogen (ICI 182780) in women with primary breast cancer. , 1994, Cancer research.
[125] D. Bentrem,et al. Novel antitumor effect of estradiol in athymic mice injected with a T47D breast cancer cell line overexpressing protein kinase Calpha. , 2001, Clinical cancer research : an official journal of the American Association for Cancer Research.
[126] M Carlquist,et al. Structure of the ligand‐binding domain of oestrogen receptor beta in the presence of a partial agonist and a full antagonist , 1999, The EMBO journal.
[127] J. Simard,et al. Blockade of the stimulatory effect of estrogens, OH-tamoxifen, OH-toremifene, droloxifene, and raloxifene on alkaline phosphatase activity by the antiestrogen EM-800 in human endometrial adenocarcinoma Ishikawa cells. , 1997, Cancer research.
[128] C. Labrie,et al. Inhibitory effect of the novel anti‐estrogen EM‐800 and medroxyprogesterone acetate on estrone‐stimulated growth of dimethylbenz[a]anthracene‐induced mammary carcinoma in rats , 1997, International journal of cancer.
[129] H. Rübsamen,et al. Expression of pp60c-src protein kinase in adult and fetal human tissue: high activities in some sarcomas and mammary carcinomas. , 1983, Cancer research.
[130] C. D. Jones,et al. Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effective estrogen antagonist with only minimal in , 1984, Journal of medicinal chemistry.
[131] Virgile Richard,et al. Prevention of bone loss by EM-800 and raloxifene in the ovariectomized rat , 2000, The Journal of Steroid Biochemistry and Molecular Biology.
[132] C. Labrie,et al. Effect of twenty-four-week treatment with the antiestrogen EM-800 on estrogen-sensitive parameters in intact and ovariectomized mice. , 1998, Endocrinology.
[133] M Karin,et al. Potentiation of estrogen receptor activation function 1 (AF-1) by Src/JNK through a serine 118-independent pathway. , 2001, Molecular endocrinology.
[134] C. Arteaga. The epidermal growth factor receptor: from mutant oncogene in nonhuman cancers to therapeutic target in human neoplasia. , 2001, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[135] V. Jordan,et al. EVIDENCE FOR THE METABOLIC ACTIVATION OF NON‐STEROIDAL ANTIOESTROGENS: A STUDY OF STRUCTURE‐ACTIVITY RELATIONSHIPS , 1980, British journal of pharmacology.
[136] D. Bentrem,et al. Molecular mechanism of action at estrogen receptor alpha of a new clinically relevant antiestrogen (GW7604) related to tamoxifen. , 2001, Endocrinology.
[137] V. Jordan,et al. Development of tamoxifen-stimulated growth of MCF-7 tumors in athymic mice after long-term antiestrogen administration. , 1988, Cancer research.
[138] A. Howell,et al. Pharmacokinetics, pharmacological and anti-tumour effects of the specific anti-oestrogen ICI 182780 in women with advanced breast cancer. , 1996, British Journal of Cancer.
[139] Y. Ma,et al. Droloxifene inhibits cortical bone turnover associated with estrogen deficiency in rats. , 1995, Bone.
[140] G. Leclercq,et al. Metabolism of tamoxifen by isolated rat hepatocytes. Identification of the glucuronide of 4-hydroxytamoxifen. , 1990, Biochemical pharmacology.
[141] H. Varmus,et al. Evidence that the transforming gene of avian sarcoma virus encodes a protein kinase associated with a phosphoprotein , 1978, Cell.
[142] C. Hudis,et al. Phase I study of a third-generation selective estrogen receptor modulator, LY353381.HCL, in metastatic breast cancer. , 2001, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[143] B. Katzenellenbogen,et al. Nongenotropic, Sex-Nonspecific Signaling through the Estrogen or Androgen Receptors Dissociation from Transcriptional Activity , 2001, Cell.
[144] C. Labrie,et al. Novel compounds inhibit estrogen formation and action. , 1992, Cancer research.
[145] M. Dowsett,et al. The novel anti-oestrogen idoxifene inhibits the growth of human MCF-7 breast cancer xenografts and reduces the frequency of acquired anti-oestrogen resistance. , 1997, British Journal of Cancer.
[146] P. Hirsimäki,et al. Tamoxifen induces hepatocellular carcinoma in rat liver: A 1-year study with two antiestrogens , 2005, Archives of Toxicology.
[147] I W Taylor,et al. Cell proliferation kinetics of MCF-7 human mammary carcinoma cells in culture and effects of tamoxifen on exponentially growing and plateau-phase cells. , 1983, Cancer research.
[148] S. Hilsenbeck,et al. Oxidative stress and AP-1 activity in tamoxifen-resistant breast tumors in vivo. , 2000, Journal of the National Cancer Institute.
[149] A. Lykkesfeldt,et al. Type I IGF receptor and acquired tamoxifen resistance in oestrogen-responsive human breast cancer cells. , 1993, European journal of cancer.
[150] J. Robertson,et al. Oestrogen receptor: a stable phenotype in breast cancer. , 1996, British Journal of Cancer.
[151] K. Mokbel,et al. Does c-erbB2/HER2 overexpression predict adjuvant tamoxifen failure in patients with early breast cancer? , 2001, European journal of surgical oncology : the journal of the European Society of Surgical Oncology and the British Association of Surgical Oncology.
[152] C Sonnenschein,et al. The two faces of janus: sex steroids as mediators of both cell proliferation and cell death. , 2001, Journal of the National Cancer Institute.
[153] D. Accili,et al. Insulin Inhibits the Activation of Transcription by a C-terminal Fragment of the Forkhead Transcription Factor FKHR , 2000, The Journal of Biological Chemistry.
[154] L. Kangas,et al. Antitumor effects of combination toremifene and medroxyprogesterone acetate (MPA) in vitro and in vivo. , 1990, Journal of steroid biochemistry.
[155] V. Jordan,et al. The interaction of raloxifene and the active metabolite of the antiestrogen EM-800 (SC 5705) with the human estrogen receptor. , 1999, Cancer research.
[156] Valerie Speirs,et al. Coexpression of Estrogen Receptor α and β: Poor Prognostic Factors in Human Breast Cancer? , 1999 .
[157] M. Fernö,et al. ERBB2 amplification is associated with tamoxifen resistance in steroid-receptor positive breast cancer. , 1994, Cancer letters.
[158] B. Katzenellenbogen,et al. Antiestrogen basicity--activity relationships: a comparison of the estrogen receptor binding and antiuterotrophic potencies of several analogues of (Z)-1,2-diphenyl-1-[4-[2-(dimethylamino)ethoxy]phenyl]-1-butene (tamoxifen, Nolvadex) having altered basicity. , 1982, Journal of medicinal chemistry.
[159] P. Lønning,et al. High-dose estrogen treatment in postmenopausal breast cancer patients heavily exposed to endocrine therapy , 2001, Breast Cancer Research and Treatment.
[160] L. Cantley,et al. Evidence that the Rous sarcoma virus transforming gene product phosphorylates phosphatidylinositol and diacylglycerol. , 1984, Proceedings of the National Academy of Sciences of the United States of America.
[161] M. Parker,et al. The antiestrogen ICI 182780 disrupts estrogen receptor nucleocytoplasmic shuttling. , 1993, Journal of cell science.
[162] C. Labrie,et al. Comparison of the effects of the antiestrogens EM-800 and tamoxifen on the growth of human breast ZR-75-1 cancer xenografts in nude mice. , 1998, Cancer research.
[163] Anil K. Jaiswal,et al. Transcriptional Regulation of the Human Quinone Reductase Gene by Antiestrogen-liganded Estrogen Receptor-α and Estrogen Receptor-β* , 1998, The Journal of Biological Chemistry.
[164] V. Jordan,et al. A monohydroxylated metabolite of tamoxifen with potent antioestrogenic activity. , 1977, The Journal of endocrinology.
[165] V. Jordan,et al. Regulation of prolactin synthesis in vitro by estrogenic and antiestrogenic derivatives of estradiol and estrone. , 1989, Endocrinology.
[166] A. deFazio,et al. Antiestrogen inhibition of cell cycle progression in breast cancer cells in associated with inhibition of cyclin-dependent kinase activity and decreased retinoblastoma protein phosphorylation. , 1995, Molecular endocrinology.
[167] Helmut Dotzlaw,et al. Estrogen receptor-beta messenger RNA expression in human breast tumor biopsies: relationship to steroid receptor status and regulation by progestins. , 1999, Cancer research.
[168] J. Pento,et al. A comparison of the efficacy for antitumor activity of the non-steroidal antiestrogens analog II and tamoxifen in 7,12-dimethylbenz[a] anthracene-induced rat mammary tumors. , 1982, Cancer letters.
[169] M. Fernö,et al. ErbB2 status and the benefit from two or five years of adjuvant tamoxifen in postmenopausal early stage breast cancer. , 2000, Annals of oncology : official journal of the European Society for Medical Oncology.
[170] P. Bontempo,et al. Tyrosine kinase/p21ras/MAP‐kinase pathway activation by estradiol‐receptor complex in MCF‐7 cells. , 1996, The EMBO journal.
[171] V. Chinchilli,et al. Elevated serum c-erbB-2 antigen levels and decreased response to hormone therapy of breast cancer. , 1995, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[172] J. Woodburn,et al. Effect of some triphenylethylenes on oestradiol binding in vitro to macromolecules from uterus and anterior pituitary. , 1972, The Journal of endocrinology.
[173] W. Riley,et al. Cardiovascular effects of droloxifene, a new selective estrogen receptor modulator, in healthy postmenopausal women. , 2000, Arteriosclerosis, thrombosis, and vascular biology.
[174] M. Kerin,et al. Increased expression of estrogen receptor beta mRNA in tamoxifen-resistant breast cancer patients. , 1999, Cancer research.
[175] S. Martino,et al. HER-2 expression and response to tamoxifen in estrogen receptor-positive breast cancer: a Southwest Oncology Group Study. , 1998, Clinical cancer research : an official journal of the American Association for Cancer Research.
[176] G. Greene,et al. Cell membrane and nuclear estrogen receptors (ERs) originate from a single transcript: studies of ERalpha and ERbeta expressed in Chinese hamster ovary cells. , 1999, Molecular endocrinology.
[177] G. Greene,et al. Selection and characterization of a breast cancer cell line resistant to the antiestrogen LY 117018. , 1985, Endocrinology.
[178] P. Ravdin,et al. Endocrine status of premenopausal node-positive breast cancer patients following adjuvant chemotherapy and long-term tamoxifen. , 1988, Cancer research.
[179] J. Tobias,et al. The estrogen antagonist ICI 182,780 reduces cancellous bone volume in female rats. , 1993, Endocrinology.
[180] K. Ley,et al. Interaction of oestrogen receptor with the regulatory subunit of phosphatidylinositol-3-OH kinase , 2000, Nature.
[181] C. Labrie,et al. Comparison of the Effects of the New Orally Active Antiestrogen EM-800 with ICI 182 780 and Toremifene on Estrogen-Sensitive Parameters in the Ovariectomized Mouse. , 1998, Endocrinology.
[182] R. Huupponen,et al. Pharmacokinetics of (deaminohydroxy)toremifene in humans: a new, selective estrogen-receptor modulator , 2000, European Journal of Clinical Pharmacology.
[183] B. Rasmussen,et al. Value of epidermal growth factor receptor, HER2, p53, and steroid receptors in predicting the efficacy of tamoxifen in high-risk postmenopausal breast cancer patients. , 2001, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[184] D. Dorsa,et al. The Mitogen-Activated Protein Kinase Pathway Mediates Estrogen Neuroprotection after Glutamate Toxicity in Primary Cortical Neurons , 1999, The Journal of Neuroscience.
[185] C. Osborne,et al. Estrogen-dependent, tamoxifen-resistant tumorigenic growth of MCF-7 cells transfected with HER2/neu , 1992, Breast Cancer Research and Treatment.
[186] A. Wakeling,et al. Novel steroidal pure antiestrogens , 1989, Steroids.
[187] M. Sato,et al. Discovery and synthesis of [6-hydroxy-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]-2-(4-hydroxyphenyl)]b enzo[b]thiophene: a novel, highly potent, selective estrogen receptor modulator. , 1997, Journal of medicinal chemistry.
[188] C. Koch,et al. Tamoxifen induces hypoxia in MCF-7 xenografts. , 1997, Cancer Research.
[189] K. Pollow,et al. Pharmacokinetics of Droloxifene and Its Metabolites in Breast Cancer Patients , 1991, American journal of clinical oncology.
[190] Fernand Labrie,et al. EM-800, a Novel Antiestrogen, Acts as a Pure Antagonist of the Transcriptional Functions of Estrogen Receptors α and β. , 1998, Endocrinology.
[191] V. Jordan,et al. Structural derivatives of tamoxifen and oestradiol 3-methyl ether as potential alkylating antioestrogens. , 1981, European journal of cancer.
[192] D. Collins,et al. Inhibition of angiogenesis by antiestrogens. , 1993, Cancer research.
[193] P. Jain,et al. Synthesis and biological evaluation of a series of 1,1-dichloro-2,2,3-triarylcyclopropanes as pure antiestrogens. , 1991, Journal of medicinal chemistry.
[194] T. Willson,et al. Dissection of the molecular mechanism of action of GW5638, a novel estrogen receptor ligand, provides insights into the role of estrogen receptor in bone. , 1997, Endocrinology.
[195] H W Cole,et al. Synthesis and pharmacology of conformationally restricted raloxifene analogues: highly potent selective estrogen receptor modulators. , 1998, Journal of medicinal chemistry.
[196] Julia A. Taylor,et al. Printed in U.S.A. Copyright © 1998 by The Endocrine Society Transcription and Translation of Estrogen Receptor- � in the Male Reproductive Tract of Estrogen Receptor-� Knock-Out and Wild-Type Mice* , 2022 .
[197] C. Turner,et al. LY353381.HCl: a novel raloxifene analog with improved SERM potency and efficacy in vivo. , 1998, The Journal of pharmacology and experimental therapeutics.
[198] H. Michna,et al. Pharmacological characterization of a novel oestrogen antagonist, ZK 119010, in rats and mice. , 1991, The Journal of endocrinology.
[199] J. Pink,et al. Characterization of a receptor-negative, hormone-nonresponsive clone derived from a T47D human breast cancer cell line kept under estrogen-free conditions. , 1990, Cancer research.
[200] B. Katzenellenbogen,et al. The estrogen receptor enhances AP-1 activity by two distinct mechanisms with different requirements for receptor transactivation functions. , 1999, Molecular endocrinology.
[201] V. Jordan,et al. Short- and long-term estrogen deprivation of T47D human breast cancer cells in culture. , 1989, European journal of cancer & clinical oncology.
[202] J. Foekens,et al. Oncogene amplification and prognosis in breast cancer: relationship with systemic treatment. , 1995, Gene.
[203] A. Wakeling,et al. Steroidal pure antioestrogens. , 1987, The Journal of endocrinology.
[204] S. Newman,et al. Cofactor competition between the ligand-bound oestrogen receptor and an intron 1 enhancer leads to oestrogen repression of ERBB2 expression in breast cancer , 2000, Oncogene.
[205] H W Cole,et al. Structure-activity relationships of selective estrogen receptor modulators: modifications to the 2-arylbenzothiophene core of raloxifene. , 1997, Journal of medicinal chemistry.
[206] J. Skouv,et al. Increased expression of cytochrome p450 1A1 and 1B1 genes in anti‐estrogen–resistant human breast cancer cell lines , 2000, International journal of cancer.
[207] K. Korach,et al. Alteration of reproductive function but not prenatal sexual development after insertional disruption of the mouse estrogen receptor gene. , 1993, Proceedings of the National Academy of Sciences of the United States of America.
[208] Zbigniew Dauter,et al. Molecular basis of agonism and antagonism in the oestrogen receptor , 1997, Nature.
[209] G. Rubanyi,et al. Identification of Selective Estrogen Receptor Modulators by Their Gene Expression Fingerprints* , 2000, The Journal of Biological Chemistry.
[210] F. Sinowatz,et al. Antitumor activity of antiestrogenic phenylindoles on experimental prostate tumors. , 1987, European journal of cancer & clinical oncology.
[211] V. Jordan,et al. Structure-activity relationships of nonisomerizable derivatives of tamoxifen: importance of hydroxyl group and side chain positioning for biological activity. , 1991, Molecular pharmacology.
[212] J. Katzenellenbogen,et al. Novel structural templates for estrogen-receptor ligands and prospects for combinatorial synthesis of estrogens. , 1999, Chemistry & biology.
[213] P. Lønning,et al. Determination of Droloxifene and Two Metabolites in Serum by High‐Pressure Liquid Chromatography , 1995, Therapeutic drug monitoring.
[214] R. Gust,et al. Investigations of new lead structures for the design of selective estrogen receptor modulators. , 2001, Journal of medicinal chemistry.
[215] M. Dowsett,et al. Expression of nuclear receptor interacting proteins TIF-1, SUG-1, receptor interacting protein 140, and corepressor SMRT in tamoxifen-resistant breast cancer. , 1999, Clinical cancer research : an official journal of the American Association for Cancer Research.
[216] Simak Ali,et al. Phosphatidylinositol 3-Kinase/AKT-mediated Activation of Estrogen Receptor α , 2001, The Journal of Biological Chemistry.
[217] R. McPherson,et al. Effect of Long-Term Estrogen Deprivation on Apoptotic Responses of Breast Cancer Cells to 17β-Estradiol , 2001 .
[218] V. Jordan,et al. Silencing and reactivation of the selective estrogen receptor modulator-estrogen receptor alpha complex. , 2001, Cancer research.
[219] K. Cantell,et al. Additive and synergistic antitumor effects with toremifene and interferons. , 1990, Journal of steroid biochemistry.
[220] A. Howell,et al. Fulvestrant, formerly ICI 182,780, is as effective as anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment. , 2002, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[221] M. Parker,et al. Antiestrogen ICI 164,384 reduces cellular estrogen receptor content by increasing its turnover. , 1992, Proceedings of the National Academy of Sciences of the United States of America.
[222] P. Rissanen,et al. Toremifene, a new antiestrogenic compound, for treatment of advanced breast cancer. Phase II study. , 1988, European journal of cancer & clinical oncology.
[223] C. Wade,et al. Printed in U.S.A. Copyright © 2001 by The Endocrine Society Estrogen Receptor (ER) � and ER � Exhibit Unique Pharmacologic Properties When Coupled to Activation of the Mitogen-Activated Protein Kinase Pathway* , 2022 .
[224] A. Wakeling,et al. A potent specific pure antiestrogen with clinical potential. , 1991, Cancer research.
[225] S. Hilsenbeck,et al. Comparison of the effects of a pure steroidal antiestrogen with those of tamoxifen in a model of human breast cancer. , 1995, Journal of the National Cancer Institute.
[226] E. Borden,et al. Differential ability of antiestrogens to stimulate breast cancer cell (MCF-7) growth in vivo and in vitro. , 1989, Cancer research.
[227] C. Labrie,et al. Prevention of development of dimethylbenz(a)anthracene (DMBA)-induced mammary tumors in the rat by the new nonsteroidal antiestrogen EM-800 (SCH57050) , 1998, Breast Cancer Research and Treatment.
[228] C. Osborne,et al. Human breast cancer in the athymic nude mouse: cytostatic effects of long-term antiestrogen therapy. , 1987, European journal of cancer & clinical oncology.
[229] H L Pearce,et al. Arzoxifene, a new selective estrogen receptor modulator for chemoprevention of experimental breast cancer. , 2001, Cancer research.
[230] T. Scanlan,et al. Unique Protein Determinants of the Subtype-selective Ligand Responses of the Estrogen Receptors (ERα and ERβ) at AP-1 Sites* , 2001, The Journal of Biological Chemistry.
[231] D. Hayes,et al. Randomized comparison of tamoxifen and two separate doses of toremifene in postmenopausal patients with metastatic breast cancer. , 1995, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[232] J. Gustafsson,et al. Generation and reproductive phenotypes of mice lacking estrogen receptor beta. , 1998, Proceedings of the National Academy of Sciences of the United States of America.
[233] B. Katzenellenbogen,et al. Synthesis and biological evaluation of a novel series of furans: Ligands selective for estrogen receptor α , 2001 .
[234] S. Fawell,et al. Inhibition of estrogen receptor-DNA binding by the "pure" antiestrogen ICI 164,384 appears to be mediated by impaired receptor dimerization. , 1990, Proceedings of the National Academy of Sciences of the United States of America.
[235] S. Robinson,et al. In vitro estrogenic actions in rat and human cells of hydroxylated derivatives of D16726 (zindoxifene), an agent with known antimammary cancer activity in vivo. , 1988, Cancer research.
[236] L. Kangas,et al. Review of the pharmacological properties of toremifene. , 1990, Journal of steroid biochemistry.
[237] C K Osborne,et al. Double-blind, randomized trial comparing the efficacy and tolerability of fulvestrant versus anastrozole in postmenopausal women with advanced breast cancer progressing on prior endocrine therapy: results of a North American trial. , 2002, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[238] E. von Angerer,et al. 2-Phenylindoles. Effect of N-benzylation on estrogen receptor affinity, estrogenic properties, and mammary tumor inhibiting activity. , 1987, Journal of medicinal chemistry.
[239] Michael E. Greenberg,et al. Opposing Effects of ERK and JNK-p38 MAP Kinases on Apoptosis , 1995, Science.
[240] J. Cairns,et al. Relationship between c-erbB-2 protein product expression and response to endocrine therapy in advanced breast cancer. , 1992, British Journal of Cancer.
[241] K. Pritchard,et al. Droloxifene, a new antiestrogen: Its role in metastatic breast cancer , 2004, Breast Cancer Research and Treatment.