EM-652 (SCH57068), a pure SERM having complete antiestrogenic activity in the mammary gland and endometrium

Journal of Steroid Biochemistry and Molecular Biology

Volumn 79, Issue 1-5, 2001, Pages 213-225

  Labrie, Fernand ^a   Labrie, Claude ^a   Bélanger, Alain ^a   Simard, Jacques ^a   Giguère, Vincent ^b   Tremblay, André ^b   Tremblay, Gilles ^b  

^a LAVAL UNIVERSITY   (Canada)

^b MCGILL UNIVERSITY   (Canada)

Author keywords

Antiestrogen; Breast cancer; Chemoprevention; EM 652; Estrogen receptor; Osteoporosis; SCH57068; Uterine cancer

Indexed keywords

4 [4 METHYL 2 [4 [2 (1 PIPERIDINYL)ETHOXY]PHENYL] 7 PIVALOYLOXY 2H 1 BENZOPYRAN 3 YLPHENYL] PIVALATE; ACOLBIFENE; ADJUVANT; ANTIESTROGEN; ARZOXIFENE; CHOLESTEROL; DIMETHYLBENZ[A]ANTHRACENE; DROLOXIFENE; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; FULVESTRANT; IDOXIFENE; N BUTYL 11 (16ALPHA CHLORO 3,17BETA DIHYDROXYESTRA 1,3,5(10) TRIEN 7ALPHA YL) N METHYLUNDECANAMIDE; N BUTYL 11 (3,17BETA DIHYDROXYESTRA 1,3,5(10) TRIEN 7ALPHA YL) N METHYLUNDECANAMIDE; RALOXIFENE; SCH 57068; SELECTIVE ESTROGEN RECEPTOR MODULATOR; TAMOXIFEN; TOREMIFENE; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

BONE ATROPHY; BREAST CARCINOMA; CANCER CELL CULTURE; CANCER GROWTH; CANCER PREVENTION; CANCER RISK; CELL STRAIN MCF 7; CHOLESTEROL BLOOD LEVEL; CLINICAL TRIAL; CONFERENCE PAPER; DRUG INHIBITION; DRUG MECHANISM; ENDOMETRIUM; ENDOMETRIUM CARCINOMA; ENZYME ACTIVITY; ESTROGEN ACTIVITY; HUMAN; IN VITRO STUDY; INCUBATION TIME; MAMMARY GLAND; NONHUMAN; OVARIECTOMY; RISK FACTOR; STIMULATION; TRANSCRIPTION INITIATION; TRIACYLGLYCEROL BLOOD LEVEL; UTERUS CARCINOMA;

ANIMALS; BENZOPYRANS; BREAST; BREAST NEOPLASMS; CHOLESTEROL; ENDOMETRIAL NEOPLASMS; ENDOMETRIUM; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; ESTROGEN RECEPTOR MODULATORS; FEMALE; HUMANS; MAMMARY NEOPLASMS, EXPERIMENTAL; MICE; NEOPLASMS, HORMONE-DEPENDENT; OSTEOPOROSIS; PIPERIDINES; PROPIONATES; RATS; RECEPTORS, ESTROGEN; SELECTIVE ESTROGEN RECEPTOR MODULATORS; TAMOXIFEN; TRANSCRIPTION, GENETIC; TRIGLYCERIDES; TUMOR CELLS, CULTURED;

ANIMALIA; MINK CELL FOCUS-FORMING VIRUS;

EID: 0035714539     PISSN: 09600760     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-0760(01)00139-X     Document Type: Conference Paper

References (112)

1. Cancer statistics 2000
2. Effects of estradiol and prolactin on steroid receptor levels in 7,12-dimethylbenz(a)anthracene-induced mammary tumors and uterus in the rat
3. Estrogen receptors in human breast cancer: An overview
4. The role of estrogens in growth regulation of breast cancer
5. Control of aromatase in breast cancer cells and its importance for tumor growth
6. Fundamental research leading to improved endocrine therapy for breast cancer
7. Intracrinology
8. DHEA and peripheral androgen and estrogen formation: Intracrinology
9. The 3β-hydroxysteroid dehydrogenase/isomerase gene family: Lessons from type II 3β-HSD congenital deficiency
10. Inhibition of cell cycle kinetics and proliferation by the androgen 5α-dihydrotestosterone and antiestrogen N, n-butyl-N-methyl-11-(16′α-chloro-3′,17β-dihydroxy- estra-1′,3′,5′-(10′)triene-7′α-yl) undecanamide in human breast cancer ZR-75-1 cells
11. Additive inhibitory effects of an androgen and the antiestrogen EM-170 on estradiol-stimulated growth of human ZR-75-1 breast tumors in athymic mice
12. Synthesis and biological activity of new halo-steroidal antiestrogens
13. Inhibitory effect of a steroidal antiestrogen (EM-170) on estrone-stimulated growth of 7,12 dimethylbenz(a)anthracene (DMBA)-induced mammary carcinoma in the rat
14. Biology and mode of action of pure antiestrogens
15. Novel compounds inhibit estrogen formation and action
16. Mechanisms of antihormone action
17. Human oestrogen receptor cDNA: Sequence, expression and homology to v-erb-A
18. The estrogen receptor binds tightly to its responsive element as a ligand-induced homodimer
19. Long-term Tamoxifen adjuvant therapy in node-positive breast cancer: A metabolic and pilot clinical study
20. Scottish Study, The Scottish trial
21. Tamoxifen for prevention of breast cancer: Report of the national surgical adjuvant breast and bowel project P-1 study
22. Risk and prognosis of endometrial cancer after Tamoxifen for breast cancer. Comprehensive cancer centres' ALERT Group. Assessment of liver and endometrial cancer risk following Tamoxifen
23. The future of new pure antiestrogens in clinical breast cancer
24. A potent specific pure antiestrogen with clinical potential
25. ICI 182,780, a new antioestrogen with clinical potential
26. Sequence and characterization of a coactivator for the steroid hormone receptor superfamily
27. A CBP integrator complex mediates transcriptional activation and AP-1 inhibition by nuclear receptors
28. TIF2, a 160 kDa transcriptional mediator for the ligand-dependent activation function AF-2 of nuclear receptors
29. GRIP1, a novel mouse protein that serves as a transcriptional coactivator in yeast for the hormone binding domains of steroid receptors
30. AIB1, a steroid receptor coactivator amplified in breast and ovarian cancer
31. The transcriptional co-activator p/CIP binds CBP and mediates nuclear-receptor function
32. Nuclear receptor coactivator ACTR is a novel histone acetyltransferase and form a multimeric activation complex with P/CAF and CBP/p300
33. RAC3, a steroid/nuclear receptor-associated coactivator that is related to SRC-1 and TIF2
34. Role of the two activating domains of the oestrogen receptor in cell-type and promoter-context dependent agonistic activity of the anti-oestrogen 4-hydroxytamoxifen
35. Functional domains of the human estrogen receptor
36. Characterization of the amino-terminal transcriptional activation function of the human estrogen receptor in animal and yeast cells
37. Peptide growth factors elicit estrogen receptor-dependent transcriptional activation of an estrogen-responsive element
38. Stimulation of estrogen receptor-mediated transcription and alteration in the phosphorylation state of the rat uterine estrogen receptor by estrogen, cyclic adenosine monophosphate, and insulin-like growth factor-I
39. Activation of the unliganded estrogen receptor by EGF involves the MAP kinase pathway and direct phosphoryltion
40. Dopaminergic and ligand-independent activation of steroid hormone receptors
41. Modulation of the ligand-independent activation of the human estrogen receptor by hormone and antihormone
42. Cloning, chromosomal localization and functional analysis of the murine estrogen receptor β
43. Modulation of transcriptional activation by ligand-dependent phosphorylation of the human oestrogen receptor A/B region
44. Activation of the estrogen receptor through phosphorylation by mitogen-activated protein kinase
45. Estrogen-responsive element of the human pS2 gene is an imperfectly palindromic sequence
46. Mammary cancer induced by a single feeding of polynuclear hydrocarbons, and its suppression
47. Host factors affecting the growth of carcinogen-induced rat mammary carcinomas: A review and tribute to Charles Brenton Huggins
48. Estrogen-prolactin dependency in 7,12-dimethylbenz(a)anthacene-induced tumors
49. Control of hormone receptor levels and growth of 7,12-dimethylbenz(a)anthracene-induced mammary tumors by estrogens, progesterone and prolactin
50. 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
51. Controlled release low dose medroxyprogesterone acetate (MPA) inhibits the development of mammary tumors induced by dimethylbenz(a)anthracene in the rat
52. Endocrine regulation of growth and hormone receptor levels in DMBA-induced mammary tumors
53. High inhibitory activity of a new antiestrogen, RU16117 (11α-methoxy-ethinyl estradiol) on the development of dimethylbenz(a)anthracene-induced mammary tumors
54. Effect of adrenal estrogens on the growth of dimethylbenz(a)antracene-induced mammary carcinoma in the rat
55. Additive inhibitory effects of bromocriptine (CB-154) and medroxyprogesterone acetate (MPA) on dimethylbenz(a)anthracene (DMBA)-induced mammary tumors in the rat
56. Potent inhibitory activity of a new antiestrogen, RU16117, on the development and growth of DMBA-induced rat mammary adenocarcinoma
57. Evaluation of the antitumour activity of the non-steroidal antioestrogen monohydroxytamoxifen in the DMBA-induced rat mammary carcinoma model
58. Prevention by dehydroepiandrosterone of the development of mammary carcinoma induced by 7,12-dimethylbenz(a)anthracene (DMBA) in the rat
59. Comparative effects of 28-day treatment with the new antiestrogen EM-800 and Tamoxifen on estrogen-sensitive parameters in the intact mouse
60. Combined effects of dehydroepiandrosterone and EM-800 on bone mass, serum lipids, and the development of dimethylbenz(a)anthracene (DMBA)-induced mammary carcinoma in the rat
61. Inhibitory effect of the novel antiestrogen EM-800 and medroxyprogesterone acetate (MPA) on estrone-stimulated growth of dimethylbenz(a)anthracene (DMBA)-induced mammary carcinoma in the rat
62. (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
63. 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
64. Prevention of development of dimenthylbenz(a)anthracene (DMBA)-induced mammary carcinoma in the rat by the new nonsteroidal antiestrogen EM-800 (SCH 57050)
65. Use of the DMBA-induced rat mammary carcinoma system for the evaluation of Tamoxifen as a potential adjuvant therapy
66. Effect of Tamoxifen (ICI 46,474) on initiation and growth of DMBA-induced rat mammary carcinoma
67. Antitumor effects of Droloxifene, a new antiestrogen drug, against 7,12-dimethylbenz(a)anthracene-induced mammary tumors in rats
68. Tamoxifen in advanced breast cancer
69. Estrogenic regulation of growth and polypeptide growth factor secretion in human breast carcinoma
70. Response to a specific antiestrogen (ICI 182780) in Tamoxifen-resistant breast cancer
71. Proliferation, hormonal responsiveness, and estrogen receptor content of MCF-7 human breast cancer cells grown in the short-term and long-term absence of estrogens
72. Antiestrogenic properties of keoxifene, trans-4-hydroxytamoxifen and ICI164384, a new steroidal antiestrogen, in ZR-75-1 human breast cancer cells
73. Effects of antioestrogens on the proliferation of MCF-7 human breast cancer cells
74. Contrasting actions of Tamoxifen on endometrial and breast tumor growth in the athymic mouse
75. Comparison of the effects of a pure steroidal antiestrogen with those of Tamoxifen in a model of human breast cancer
76. Effect of estrogens and antiestrogens on cell proliferation and synthesis of secreted proteins in the human breast cancer cell line MCF-7 and Tamoxifen-resistant variant subline
77. Response after withdrawal of Tamoxifen and progestogens in advanced breast cancer
78. Clinical significance of Tamoxifen withdrawal response
79. Tamoxifen therapy in premenopausal patients with metastatic breast cancer
80. Combined modality therapy for first recurrence of breast cancer. A southwest oncology group study
81. Tamoxifen resistance in breast cancer
82. MCF7/LCC2: A 4-hydroxytamoxifen resistant human breast cancer variant that retains sensitivity to the steroidal antiestrogen ICI 182,780
83. Altered expression of estrogen-regulated genes in a Tamoxifen-resistant and ICI 164,384 and ICI 182,780 sensitive human breast cancer cell line, MCF-7/TAMR-1
84. Anti-proliferative and anti-estrogenic effects of ICI 164,384 and ICI 182,780 in 4-OH-Tamoxifen-resistant human breast-cancer cells
85. Inhibition of Tamoxifen-stimulated growth of an MCF-7 tumor variant in athymic mice by novel steroidal antiestrogens
86. Acquired Tamoxifen resistance: Correlation with reduced breast tumor levels of Tamoxifen and isomerization of trans-4-hydroxytamoxifen
87. Endocrine therapy testing of human breast cancers in the soft agar clonogenic assay
88. Regulation of pS2 gene expression by affinity labeling and reversibly binding estrogens and antiestrogens: Comparison of effects on the native gene and on pS2-chloramphenicol acetyltransferase fusion genes transfected into MCF-7 human breast cancer cells
89. Differential effects of estrogen and antiestrogen on in vitro clonogenic growth of human breast cancers in soft agar
90. Effects of 4-hydroxytamoxifen and a novel pure antioestrogen (ICI 182780) on the clonogenic growth of human breast cancer cells in vitro
91. Comparative studies on the effects of steroidal and nonsteroidal oestrogen antagonists on the proliferation of human breast cancer cells
92. Effects of estradiol and Tamoxifen on human breast cancer cells in serum-free culture
93. Tamoxifen stimulation of human breast cancer cell proliferation in vitro: A possible model for Tamoxifen tumour flare
94. Hormone dependency and the action of Tamoxifen in human mammary carcinoma cells
95. Phenol red in tissue culture media is a weak estrogen: Implications concerning the study of estrogen-responsive cells in culture
96. Contrasting ability of antiestrogens to inhibit MCF-7 growth stimulated by estradiol or epidermal growth factor
97. The pharmacology and clinical uses of Tamoxifen
98. Efficacy of Tamoxifen as treatment of breast cancer
99. Potential role of Tamoxifen in prevention of breast cancer
100. A simple and sensitive microtiter plate estrogen bioassay based on stimulation of alkaline phosphatase in Ishikawa cells: Estrogenic action of D5 adrenal steroids
101. 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
102. Characterization of the ovariectomized rat model for the evaluation of estrogen effects on plasma cholesterol levels
103. Raloxifene (LY139481 HCl) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats
104. Benzopyran selective estrogen receptor modulators (SERMs): Pharmacological effects and structural correlation with raloxifen
105. Estradiol and Tamoxifen interactions with thyroid hormone in the ovariectomized-thyroidectomized rat
106. Effects of Tamoxifen therapy on lipid and lipoprotein levels in postmenopausal patients with node-negative breast cancer
107. Effects of Tamoxifen on cardiovascular risk factors in postmenopausal women
108. Droloxifene, a new estrogen antagonist/agonist, prevents bone loss in ovariectomized rats
109. Binding characteristics of novel nonsteroidal antiestrogens to the rat uterine estrogen receptors
110. EM-800, a novel antiestrogen, acts as a pure antagonist of the transcriptional functions of estrogen receptors α and β
111. EM-652 (SCH 57068), a third generation SERM acting as pure antiestrogen in the mammary gland and endometrium