Skip to main content
Key Specialties
Cardiology Diabetology Endocrinology Gastroenterology Geriatrics and Gerontology Gynecology and Obstetrics Hematology Infectious Disease Internal Medicine Nephrology Neurology Oncology Pediatrics Respiratory Medicine Rheumatology Surgery
Congress Coverage
2024 ACC Congress 2023 ESMO Congress 2023 EASD Congress 2023 ERS Congress 2023 ESC Congress
Clinical Collections
Advances in Alzheimer’s

At a glance: The STEP trials

A round-up of the STEP phase 3 clinical trials evaluating semaglutide for weight loss in people with overweight or obesity.
ADVANCED SEARCH
Log in
Top
Breast Cancer Research and Treatment
Published in: Breast Cancer Research and Treatment 2/2012

01-07-2012 | Preclinical Study

Specific transcriptional response of four blockers of estrogen receptors on estradiol-modulated genes in the mouse mammary gland

Authors: Ezequiel Calvo, Van Luu-The, Pascal Belleau, Céline Martel, Fernand Labrie

Published in: Breast Cancer Research and Treatment | Issue 2/2012

Login to get access

Abstract

Novel agents for the endocrine therapy of breast cancer are needed, especially in order to take advantage of the multiple consecutive responses observed in metastatic progressing breast cancer following previous hormone therapy, thus delaying the use of cytotoxic chemotherapy with its frequent poor tolerance and serious side effects. Acolbifene (ACOL) is a novel and unique antiestrogen which represents a unique opportunity to achieve the most potent and specific blockade of estrogen action in the mammary gland and uterus while exerting estrogen-like beneficial effects in other tissues, especially the bones. To better understand the specificity of action of ACOL, we have used Affymetrix GeneChips containing 45,000 probe sets to analyze 34,000 genes to determine the specificity of this compound compared to the pure antiestrogen fulvestrant, as well as to the mixed antagonists/agonists tamoxifen and raloxifene to block the effect of estradiol (E2) and to induce effects of their own on the genomic profile in the mouse mammary gland. The genes modulated by E2 were those identified in two separate experiments and validated by quantitative real-time PCR (qPCR). Three hours after the single subcutaneous injection of E2 (0.05 μg), the simultaneous administration of ACOL, fulvestrant, tamoxifen, and raloxifene blocked by 98, 61, 43, and 92 % the number of E2-upregulated genes, respectively. On the other hand, 70, 10, 25, and 55 % of the genes down-regulated by E2 were blocked by the same compounds. Of the 128 genes modulated by E2, 49 are associated with tumorigenesis while 22 are known to be associated with breast cancer. When used alone, ACOL modulated the smallest number of genes also influenced by E2, namely 4 %, thus possibly explaining potential utilities of this compound in breast cancer prevention and therapy.
Literature
1.
Ai L, Kim WJ, Demircan B, Dyer LM, Bray KJ, Skehan RR, Massoll NA, Brown KD (2008) The transglutaminase 2 gene (TGM2), a potential molecular marker for chemotherapeutic drug sensitivity, is epigenetically silenced in breast cancer. Carcinogenesis 29:510–518PubMedCrossRef
2.
Antonyak MA, Li B, Regan AD, Feng Q, Dusaban SS, Cerione RA (2009) Tissue transglutaminase is an essential participant in the epidermal growth factor-stimulated signaling pathway leading to cancer cell migration and invasion. J Biol Chem 284:17914–17925PubMedCrossRef
3.
Asselin-Labat ML, Sutherland KD, Barker H, Thomas R, Shackleton M, Forrest NC, Hartley L, Robb L, Grosveld FG, van der Wees J, Lindeman GJ, Visvader JE (2007) Gata-3 is an essential regulator of mammary-gland morphogenesis and luminal-cell differentiation. Nat Cell Biol 9:201–209. doi:10.​1038/​ncb1530 PubMedCrossRef
4.
Asselin-Labat ML, Sutherland KD, Vaillant F, Gyorki DE, Wu D, Holroyd S, Breslin K, Ward T, Shi W, Bath ML, Deb S, Fox SB, Smyth GK, Lindeman GJ, Visvader JE (2011) Gata-3 negatively regulates the tumor-initiating capacity of mammary luminal progenitor cells and targets the putative tumor suppressor caspase-14. Mol Cell Biol 31:4609–4622. doi:10.​1128/​MCB.​05766-11 PubMedCrossRef
5.
Benjamini Y, Drai D, Elmer G, Kafkafi N, Golani I (2001) Controlling the false discovery rate in behavior genetics research. Behav Brain Res 125:279–284PubMedCrossRef
6.
Bieche I, Lerebours F, Tozlu S, Espie M, Marty M, Lidereau R (2004) Molecular profiling of inflammatory breast cancer: identification of a poor-prognosis gene expression signature. Clin Cancer Res 10:6789–6795PubMedCrossRef
7.
Bitton-Worms K, Pikarsky E, Aronheim A (2010) The AP-1 repressor protein, JDP2, potentiates hepatocellular carcinoma in mice. Mol Cancer 9:54PubMedCrossRef
8.
Bohn OL, Nasir I, Brufsky A, Tseng GC, Bhargava R, MacManus K, Chivukula M (2009) Biomarker profile in breast carcinomas presenting with bone metastasis. Int J Clin Exp Pathol 3:139–146PubMed
9.
Bottner M, Suter-Crazzolara C, Schober A, Unsicker K (1999) Expression of a novel member of the TGF-beta superfamily, growth/differentiation factor-15/macrophage-inhibiting cytokine-1 (GDF-15/MIC-1) in adult rat tissues. Cell Tissue Res 297:103–110PubMedCrossRef
10.
Brzozowski AM, Pike AC, Dauter Z, Hubbard RE, Bonn T, Engstrom O, Ohman L, Greene GL, Gustafsson JA, Carlquist M (1997) Molecular basis of agonism and antagonism in the oestrogen receptor. Nature 389:753–758PubMedCrossRef
11.
Canney PA, Griffiths T, Latief TN, Priestman TJ (1987) Clinical significance of Tamoxifen withdrawal response. Lancet 1:36PubMedCrossRef
12.
Carroll JS, Liu XS, Brodsky AS, Li W, Meyer CA, Szary AJ, Eeckhoute J, Shao W, Hestermann EV, Geistlinger TR, Fox EA, Silver PA, Brown M (2005) Chromosome-wide mapping of estrogen receptor binding reveals long-range regulation requiring the forkhead protein FoxA1. Cell 122:33–43. doi:10.​1016/​j.​cell.​2005.​05.​008 PubMedCrossRef
13.
Cerliani JP, Guillardoy T, Giulianelli S, Vaque JP, Gutkind JS, Vanzulli SI, Martins R, Zeitlin E, Lamb CA, Lanari C (2011) Interaction between FGFR-2, STAT5, and progesterone receptors in breast cancer. Cancer Res 71:3720–3731PubMedCrossRef
14.
Chekhun VF, Lukyanova NY, Kovalchuk O, Tryndyak VP, Pogribny IP (2007) Epigenetic profiling of multidrug-resistant human MCF-7 breast adenocarcinoma cells reveals novel hyper- and hypomethylated targets. Mol Cancer Ther 6:1089–1098PubMedCrossRef
15.
16.
Cicatiello L, Mutarelli M, Grober OM, Paris O, Ferraro L, Ravo M, Tarallo R, Luo S, Schroth GP, Seifert M, Zinser C, Chiusano ML, Traini A, De Bortoli M, Weisz A (2010) Estrogen receptor alpha controls a gene network in luminal-like breast cancer cells comprising multiple transcription factors and microRNAs. Am J Pathol 176:2113–2130. doi:10.​2353/​ajpath.​2010.​090837 PubMedCrossRef
17.
Cummings SR, Eckert S, Krueger KA, Grady D, Powles TJ, Cauley JA, Norton L, Nickelsen T, Bjarnason NH, Morrow M, Lippman ME, Black D, Glusman JE, Costa A, Jordan VC (1999) The effect of raloxifene on risk of breast cancer in postmenopausal women: results from the MORE randomized trial. Multiple Outcomes of Raloxifene Evaluation. JAMA 281:2189–2197PubMedCrossRef
18.
Dalby KN, Tekedereli I, Lopez-Berestein G, Ozpolat B (2010) Targeting the prodeath and prosurvival functions of autophagy as novel therapeutic strategies in cancer. Autophagy 6:322–329PubMedCrossRef
19.
DeFriend DJ, Anderson E, Bell J, Wilks DP, West CM, Mansel RE, Howell A (1994) Effects of 4-hydroxytamoxifen and a novel pure antioestrogen (ICI 182780) on the clonogenic growth of human breast cancer cells in vitro. Br J Cancer 70:204–211PubMedCrossRef
20.
21.
Ettinger B, Black DM, Mitlak BH, Knickerbocker RK, Nickelsen T, Genant HK, Christiansen C, Delmas P, Zanchetta J, Stakkestad J, Glüer CC, Krueger K, Cohen FJ, Eckert S, Ensrud KE, Avioli LV, Lips P, Cummings SR, Investigators ftMOoREM (1999) Reduction of vertebral fracture risk in postmenopausal women with osteoporosis treated with Raloxifene (Results from a 3-year randomized clinical trial). JAMA 282:637–645PubMedCrossRef
22.
Fabian CJ, Kimler BF (2005) Selective estrogen-receptor modulators for primary prevention of breast cancer. J Clin Oncol 23:1644–1655PubMedCrossRef
23.
Fisher B, Costantino JP, Lawrence Wickerham D, Redmond CK, Kavanah M, Cronin WM, Vogel V, Robidoux A, Dimitrov N, Atkins J, Daly M, Wieand S, Tan-Chiu E, Ford L, Wolmark N (1998) Tamoxifen for prevention of breast cancer: report of the national surgical adjuvant breast and bowel project P-1 study. J Natl Cancer Inst 90:1371–1388PubMedCrossRef
24.
Gauthier S, Caron B, Cloutier J, Dory YL, Favre A, Larouche D, Mailhot J, Ouellet C, Schwerdtfeger A, Leblanc G, Martel C, Simard J, Mérand Y, Bélanger A, Labrie C, Labrie F (1997) (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. J Med Chem 40:2117–2122PubMedCrossRef
25.
Gautier L, Cope L, Bolstad BM, Irizarry RA (2004) affy—analysis of Affymetrix GeneChip data at the probe level. Bioinformatics 20:307–315PubMedCrossRef
26.
Gottardis MM, Jordan VC (1988) Development of tamoxifen-stimulated growth of MCF-7 tumors in athymic mice after long-term antiestrogen administration. Cancer Res 48:5183–5187PubMed
27.
Gutman M, Couillard S, Roy J, Labrie F, Candas B, Labrie C (2002) Comparison of the effects of EM-652 (SCH 57068), Tamoxifen, toremifene, droloxifene, idoxifene, GW-5638 and Raloxifene on the growth of human ZR-75-1 breast tumors in nude mice. Int J Cancer 99:273–278PubMedCrossRef
28.
Herman JF, Mangala LS, Mehta K (2006) Implications of increased tissue transglutaminase (TG2) expression in drug-resistant breast cancer (MCF-7) cells. Oncogene 25:3049–3058PubMedCrossRef
29.
Hermenegildo C, Garcia-Martinez MC, Tarin JJ, Cano A (2002) Inhibition of low-density lipoprotein oxidation by the pure antiestrogens ICI 182780 and EM-652 (SCH 57068). Menopause 9:430–435PubMedCrossRef
30.
Hoogstraten B, Gad el Mawla N, Maloney TR, Fletcher WS, Vaughn CB, Tranum BL, Athens JW, Costanzi JJ, Foulkes M (1984) Combined modality therapy for first recurrence of breast cancer. A Southwest Oncology Group study. Cancer 54:2248–2256PubMedCrossRef
31.
Howell A, Dodwell DJ, Anderson H, Redford J (1992) Response after withdrawal of tamoxifen and progestogens in advanced breast cancer. Ann Oncol 3:611–617PubMed
32.
Ingle JN, Ahmann DL, Green SJ, Edmonson JH, Bisel HF, Kvols LK et al (1981) Randomized clinical trial of diethylstilbestrol versus tamoxifen in postmenopausal women with advanced breast cancer. N Engl J Med 304:16–21PubMedCrossRef
33.
Irizarry RA, Hobbs B, Collin F, Beazer-Barclay YD, Antonellis KJ, Scherf U, Speed TP (2003) Exploration, normalization, and summaries of high density oligonucleotide array probe level data. Biostatistics 4:249–264PubMedCrossRef
34.
Jagannathan V, Robinson-Rechavi M (2011) Meta-analysis of estrogen response in MCF-7 distinguishes early target genes involved in signaling and cell proliferation from later target genes involved in cell cycle and DNA repair. BMC Syst Biol 5:138. doi:10.​1186/​1752-0509-5-138 PubMedCrossRef
35.
36.
Jensen J, Kitlen JW, Briand P, Labrie F, Lykkesfeldt AE (2003) Effect of antiestrogens and aromatase inhibitor on basal growth of the human breast cancer cell line MCF-7 in serum-free medium. J Steroid Biochem Mol Biol 84:469–478PubMedCrossRef
37.
38.
Kiguchi K, Giometti C, Chubb CH, Fujiki H, Huberman E (1992) Differentiation induction in human breast tumor cells by okadaic acid and related inhibitors of protein phosphatases 1 and 2A. Biochem Biophys Res Commun 189:1261–1267PubMedCrossRef
39.
Kim CH, Park JY, Lee KU, Kim JH, Kim HK (2009) Association of serum gamma-glutamyltransferase and alanine aminotransferase activities with risk of type 2 diabetes mellitus independent of fatty liver. Diabetes Metab Res Rev 25:64–69PubMedCrossRef
40.
Kim KK, Lee JJ, Yang Y, You KH, Lee JH (2008) Macrophage inhibitory cytokine-1 activates AKT and ERK-1/2 via the transactivation of ErbB2 in human breast and gastric cancer cells. Carcinogenesis 29:704–712PubMedCrossRef
41.
Komine O, Hayashi K, Natsume W, Watanabe T, Seki Y, Seki N, Yagi R, Sukzuki W, Tamauchi H, Hozumi K, Habu S, Kubo M, Satake M (2003) The Runx1 transcription factor inhibits the differentiation of naive CD4+ T cells into the Th2 lineage by repressing GATA3 expression. J Exp Med 198:51–61. doi:10.​1084/​jem.​20021200 PubMedCrossRef
42.
Koptyra M, Gupta S, Talati P, Nevalainen MT (2011) Signal transducer and activator of transcription 5a/b: biomarker and therapeutic target in prostate and breast cancer. Int J Biochem Cell Biol 43:1417–1421PubMedCrossRef
43.
Kumar A, Gao H, Xu J, Reuben J, Yu D, Mehta K (2011) Evidence that aberrant expression of tissue transglutaminase promotes stem cell characteristics in mammary epithelial cells. PLoS ONE 6:e20701PubMedCrossRef
44.
Kuroso K, Imai Y, Kobayashi M, Yanagimoto K, Suzuki T, Kojima M, Ueda Y (2010) Immunohistochemical detection of fibroblast growth factor receptor 3 in human breast cancer: correlation with clinicopathological/molecular parameters and prognosis. Pathobiology 77:231–240PubMedCrossRef
45.
Labrie F (2008) Combination of breast cancer prevention with tissue-targeted hormone replacement therapy. In: Pasqualini JR (ed) Breast cancer: prognosis, treatment, and prevention, 2nd edn. Taylor & Francis, New York, pp 201–252
46.
Labrie F (2007) Drug Insight: breast cancer prevention and tissue-targeted hormone replacement therapy. Nat Clin Pract Endocrinol Metab 3:584–593PubMedCrossRef
47.
Labrie F (2002) Endocrine-sensitive cancers of the prostate and breast. In: Baxter J, Melmed S, New MI (eds) Genetics in Endocrinology. Lippincott-William and Wilkins, Philadelphia, pp 607–661
48.
Labrie F (1995) Endocrine therapy of prostate cancer: optimal form and timing. J Clin Endocrinol Metab 80:1066–1071PubMedCrossRef
49.
Labrie F, Champagne P, Labrie C, Bélanger A, Roy J, Laverdière J, Deschênes L, Provencher L, Potvin M, Drolet Y, Pollak M, Panasci L, L’Espérance B, Dufresne J, Latreille J, Robert J, Samson B, Jolivet J, Yelle L, Cusan L, Diamond P, Candas B (2004) Activity and safety of the orally active pure antiestrogen EM-800 (SCH 57050) in Tamoxifen-resistant breast cancer. J Clin Oncol 22:864–871PubMedCrossRef
50.
Labrie F, El-Alfy M, Berger L, Labrie C, Martel C, Bélanger A, Candas B, Pelletier G (2003) The combination of a novel SERM with an estrogen protects the mammary gland and uterus in a rodent model: the future of postmenopausal women’s health? Endocrinology 144:4700–4706PubMedCrossRef
51.
Labrie F, Labrie C, Bélanger A, Giguère V, Simard J, Mérand Y, Gauthier S, Luu-The V, Candas B, Martel C, Luo S (2001) Pure selective estrogen receptor modulators, new molecules having absolute cell specificity ranging from pure antiestrogenic to complete estrogen-like activities. In: Scolnick EM (ed) Advances in protein chemistry: drug discovery and design. Academic Press, San Diego, pp 293–368CrossRef
52.
Labrie F, Labrie C, Bélanger A, Simard J (2002) Third and fourth generation SERMs. In: Manni A, Verderame M (eds) Selective estrogen receptor modulators: research and clinical applications. Humana Press Inc., Totowa, pp 167–187CrossRef
53.
Labrie F, Labrie C, Bélanger A, Simard J, Gauthier S, Luu-The V, Mérand Y, Giguère V, Candas B, Luo S, Martel C, Singh SM, Fournier M, Coquet A, Richard V, Charbonneau R, Charpenet G, Tremblay A, Tremblay G, Cusan L, Veilleux R (1999) EM-652 (SCH 57068), a third generation SERM acting as pure antiestrogen in the mammary gland and endometrium. J Steroid Biochem Mol Biol 69:51–84PubMedCrossRef
54.
Labrie F, Labrie C, Bélanger A, Simard J, Giguère V, Tremblay A, Tremblay G (2001) EM-652 (SCH 57068), a pure SERM having complete antiestrogenic activity in the mammary gland and endometrium. J Steroid Biochem Mol Biol 79:213–225PubMedCrossRef
55.
Lacerda L, Pusztai L, Woodward WA (2010) The role of tumor initiating cells in drug resistance of breast cancer: implications for future therapeutic approaches. Drug Resist Updat 13:99–108PubMedCrossRef
56.
Laganiere J, Deblois G, Lefebvre C, Bataille AR, Robert F, Giguere V (2005) From the Cover: location analysis of estrogen receptor alpha target promoters reveals that FOXA1 defines a domain of the estrogen response. Proc Natl Acad Sci USA 102:11651–11656PubMedCrossRef
57.
Langer S, Singer CF, Hudelist G, Dampier B, Kaserer K, Vinatzer U, Pehamberger H, Zielinski C, Kubista E, Schreibner M (2006) Jun and Fos family protein expression in human breast cancer: correlation of protein expression and clinicopathological parameters. Eur J Gynaecol Oncol 27:345–352PubMed
58.
Lemieux C, Gelinas Y, Lalonde J, Labrie F, Cianflone K, Deshaies Y (2005) Hypolipidemic action of the SERM acolbifene is associated with decreased liver MTP and increased SR-BI and LDL receptors. J Lipid Res 46:1285–1294PubMedCrossRef
59.
Lemieux C, Gelinas Y, Lalonde J, Labrie F, Richard D, Deshaies Y (2006) Hypocholesterolemic action of the selective estrogen receptor modulator acolbifene in intact and ovariectomized rats with diet-induced hypercholesterolemia. Metabolism 55:605–613PubMedCrossRef
60.
Lemieux C, Gelinas Y, Lalonde J, Labrie F, Richard D, Deshaies Y (2005) The selective estrogen receptor modulator acolbifene reduces cholesterolemia independently of its anorectic action in control and cholesterol-fed rats. J Nutr 135:2225–2229PubMed
61.
Lemieux C, Phaneuf D, Labrie F, Giguere V, Richard D, Deshaies Y (2005) Estrogen receptor alpha-mediated adiposity-lowering and hypocholesterolemic actions of the selective estrogen receptor modulator acolbifene. Int J Obes Relat Metab Disord 29:1236–1244CrossRef
62.
Lemieux C, Picard F, Labrie F, Richard D, Deshaies Y (2003) The estrogen antagonist EM-652 and dehydroepiandrosterone prevent diet- and ovariectomy-induced obesity. Obes Res 11:477–490PubMedCrossRef
63.
Li B, Antonyak MA, Druso JE, Cheng L, Nikitin AY, Cerione RA (2010) EGF potentiated oncogenesis requires a tissue transglutaminase-dependent signaling pathway leading to Src activation. Proc Natl Acad Sci USA 107:1408–1413PubMedCrossRef
64.
Luo S, Labrie C, Labrie F (1998) Prevention of development of dimenthylbenz(a)anthracene (DMBA)-induced mammary carcinoma in the rat by the new nonsteroidal antiestrogen EM-800 (SCH 57050). Breast Cancer Res Treat 49:1–11PubMedCrossRef
65.
Luo S, Sourla A, Labrie C, Bélanger A, Labrie F (1997) 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. Endocrinology 138:4435–4444PubMedCrossRef
66.
Luo S, Stojanovic M, Labrie C, Labrie F (1997) 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. Int J Cancer 73:580–586PubMedCrossRef
67.
Luu-The V, Paquet N, Calvo E, Cumps J (2005) Improved real-time RT-PCR method for high-throughput measurements using second derivative calculation and double correction. Biotechniques 38:287–293PubMedCrossRef
68.
Lykkesfeldt AE, Sorensen EK (1992) 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. AL 1. Acta Oncol 31:131–138PubMedCrossRef
69.
Man CH, Fung TK, Ho C, Han HH, Chow HC, Ma AC, Choi WW, Lok S, Cheung AM, Eaves C, Kwong YL, Leung AY (2012) Sorafenib treatment of FLT3-ITD+ acute myeloid leukemia: favorable initial outcome and mechanisms of subsequent non-responsiveness associated with a D835 mutation. Blood. doi:10.​1182/​blood-2011-06-363960 PubMed
70.
Mangala LS, Fok JY, Zorrilla-Calancha IR, Verma A, Mehta K (2007) Tissue transglutaminase expression promotes cell attachment, invasion and survival in breast cancer cells. Oncogene 26:2459–2470PubMedCrossRef
71.
Martel C, Picard S, Richard V, Bélanger A, Labrie C, Labrie F (2000) Prevention of bone loss by EM-800 and raloxifene in the ovariectomized rat. J Steroid Biochem Mol Biol 74:45–56PubMedCrossRef
72.
Martino S, Cauley JA, Barrett-Connor E, Powles TJ, Mershon J, Disch D, Secrest RJ, Cummings SR (2004) Continuing outcomes relevant to Evista: breast cancer incidence in postmenopausal osteoporotic women in a randomized trial of raloxifene. J Natl Cancer Inst 96:1751–1761PubMedCrossRef
73.
Mehta RJ, Jain RK, Leung S, Choo J, Nielsen T, Huntsman D, Nakshatri H, Badve S (2012) FOXA1 is an independent prognostic marker for ER-positive breast cancer. Breast Cancer Res Treat 131:881–890PubMedCrossRef
74.
Milde-Langosch K, Janke S, Wagner I, Schroder C, Streichert T, Bamberger AM, Janicke F, Loning T (2008) Role of Fra-2 in breast cancer: influence on tumor cell invasion and motility. Breast Cancer Res Treat 107(3):337–347PubMedCrossRef
75.
Mimeault M, Batra SK (2010) Divergent molecular mechanisms underlying the pleiotropic functions of macrophage inhibitory cytokine-1 in cancer. J Cell Physiol 224:626–635PubMedCrossRef
76.
Osborne CK, Coronado Heinsohn EB, Hilsenbeck SG, McCue BL, Wakeling AE, McClelland RA, Manning DL, Nicholson RI (1995) Comparison of the effects of a pure steroidal antiestrogen with those of tamoxifen in a model of human breast cancer. J Natl Cancer Inst 87:746–750PubMedCrossRef
77.
Park YJ, Lee H, Lee JH (2010) Macrophage inhibitory cytokine-1 transactivates ErbB family receptors via the activation of Src in SK-BR-3 human breast cancer cells. BMB Rep 43:91–96PubMedCrossRef
78.
Peck AR, Witkiewicz AK, Liu C, Stringer GA, Klimowicz AC, Pequignot E, Freydin B, Tran TH, Yang N, Rosenberg AL, Hooke JA, Kovatich AJ, Nevalainen MT, Shriver CD, Hyslop T, Sauter G, Rimm DL, Magliocco AM, Rui H (2011) Loss of nuclear localized and tyrosine phosphorylated Stat5 in breast cancer predicts poor clinical outcome and increased risk of antiestrogen therapy failure. J Clin Oncol 29:2448–2458PubMedCrossRef
79.
Picard F, Deshaies Y, Lalonde J, Samson P, Labrie C, Bélanger A, Labrie F, Richard D (2000) Effects of the estrogen antagonist EM-652.HCl on energy balance and lipid metabolism in ovariectomized rats. Int J Obes Relat Metab Disord 24:830–840PubMedCrossRef
80.
Poulin R, Merand Y, Poirier D, Levesque C, Dufour JM, Labrie F (1989) Antiestrogenic properties of Keoxifene trans-4-hydroxytamoxifen, and ICI 164384, a new steroidal antiestrogen, in ZR-75-1 human breast cancer cells. Breast Cancer Res Treat 14:65–76PubMedCrossRef
81.
Pritchard KI, Thomson DB, Myers RE, Sutherland DJ, Mobbs BG, Meakin JW (1980) Tamoxifen therapy in premenopausal patients with metastatic breast cancer. Cancer Treat Rep 64:787–796PubMed
82.
Punyadeera C, Kamps R, Defrere S, Dijcks F, de Goeij A, Ederveen A, Dunselman G, Groothuis P (2008) Effects of selective oestrogen receptor modulators on proliferation in tissue cultures of pre- and postmenopausal human endometrium. J Steroid Biochem Mol Biol 112:102–109. doi:10.​1016/​j.​jsbmb.​2008.​09.​002 S0960-0760(08)00224-0[pii]PubMedCrossRef
83.
Reichenstein M, Rauner G, Barash I (2011) Conditional repression of STAT5 expression during lactation reveals its exclusive roles in mammary gland morphology, milk-protein gene expression, and neonate growth. Mol Reprod Dev 78:585–596PubMedCrossRef
84.
Roy J, Couillard S, Gutman M, Labrie F (2003) A novel pure SERM achieves complete regression of the majority of human breast cancer tumors in nude mice. Breast Cancer Res Treat 81:223–229PubMedCrossRef
85.
Sanges R, Cordero F, Calogero RA (2007) oneChannelGUI: a graphical interface to Bioconductor tools, designed for life scientists who are not familiar with R language. Bioinformatics 23:3406–3408PubMedCrossRef
86.
Shiau AK, Barstad D, Loria PM, Cheng L, Kushner PJ, Agard DA, Greene GL (1998) The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen. Cell 95:927–937PubMedCrossRef
87.
Simard J, Labrie C, Bélanger A, Gauthier S, Singh SM, Mérand Y, Labrie F (1997) 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. Int J Cancer 73:104–112PubMedCrossRef
88.
Simard J, Sanchez R, Poirier D, Gauthier S, Singh SM, Mérand Y, Bélanger A, Labrie C, Labrie F (1997) 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. Cancer Res 57:3494–3497PubMed
89.
Simoncini T, Varone G, Fornari L, Mannella P, Luisi M, Labrie F, Genazzani AR (2002) Genomic and nongenomic mechanisms of nitric oxide synthesis induction in human endothelial cells by a fourth-generation selective estrogen receptor modulator. Endocrinology 143:2052–2061PubMedCrossRef
90.
Strauss BL, Bratthauer GL, Tavassoli FA (2006) STAT 5a expression in the breast is maintained in secretory carcinoma, in contrast to other histologic types. Hum Pathol 37:586–592PubMedCrossRef
91.
Tatchum-Talom R, Martel C, Labrie F, Marette A (2003) Acute vascular effects of the selective estrogen receptor modulator EM-652 (SCH 57068) in the rat mesenteric vascular bed. Cardiovasc Res 57:535–543PubMedCrossRef
92.
Thompson PA, Hsu CH, Green S, Stopeck AT, Johnson K, Alberts DS, Chow HH (2010) Sulindac and sulindac metabolites in nipple aspirate fluid and effect on drug targets in a phase I trial. Cancer Prev Res (Phila) 3:101–107CrossRef
93.
94.
Tomlinson D, Knowles M, Speirs V (2012) Mechanisms of FGFR3 actions in endocrine resistant breast cancer. Int J Cancer 130(12):2857–2866PubMedCrossRef
95.
Vogel VG, Costantino JP, Wickerham DL, Cronin WM, Cecchini RS, Atkins JN, Bevers TB, Fehrenbacher L, Pajon ER Jr, Wade JL 3rd, Robidoux A, Margolese RG, James J, Lippman SM, Runowicz CD, Ganz PA, Reis SE, McCaskill-Stevens W, Ford LG, Jordan VC, Wolmark N (2006) Effects of tamoxifen vs raloxifene on the risk of developing invasive breast cancer and other disease outcomes: the NSABP Study of Tamoxifen and Raloxifene (STAR) P-2 trial. JAMA 295:2727–2741PubMedCrossRef
96.
Warrington JA, Nair A, Mahadevappa M, Tsyganskaya M (2000) Comparison of human adult and fetal expression and identification of 535 housekeeping/maintenance genes. Physiol Genomics 2:143–147PubMed
97.
Wiebe VJ, Osborne CK, Fuqua SA, DeGregorio MW (1993) Tamoxifen resistance in breast cancer. Crit Rev Oncol Hematol 14:173–188PubMedCrossRef
98.
Williamson EA, Wolf I, O’Kelly J, Bose S, Tanosaki S, Koeffler HP (2006) BRCA1 and FOXA1 proteins coregulate the expression of the cell cycle-dependent kinase inhibitor p27(Kip1). Oncogene 25:1391–1399PubMedCrossRef
99.
Yamashita H, Takahashi S, Ito Y, Yamashita T, Ando Y, Toyama T, Sugiura H, Yoshimoto N, Kobayashi S, Fujii Y, Iwase H (2009) Predictors of response to exemestane as primary endocrine therapy in estrogen receptor-positive breast cancer. Cancer Sci 100:2028–2033PubMedCrossRef
100.
Yoon NK, Maresh EL, Shen D, Elshimali Y, Apple S, Horvath S, Mah V, Bose S, Chia D, Chang HR, Goodglick L (2010) Higher levels of GATA3 predict better survival in women with breast cancer. Hum Pathol 41:1794–1801PubMedCrossRef
101.
Yuanhong X, Feng X, Qingchang L, Jianpeng F, Zhe L, Kejian G (2010) Downregulation of AP-1 repressor JDP2 is associated with tumor metastasis and poor prognosis in patients with pancreatic carcinoma. Int J Biol Markers 25:136–140PubMed
Metadata
Title
Specific transcriptional response of four blockers of estrogen receptors on estradiol-modulated genes in the mouse mammary gland
Authors
Ezequiel Calvo
Van Luu-The
Pascal Belleau
Céline Martel
Fernand Labrie
Publication date
01-07-2012
Publisher
Springer US
Published in
Breast Cancer Research and Treatment / Issue 2/2012
Print ISSN: 0167-6806
Electronic ISSN: 1573-7217
DOI
https://doi.org/10.1007/s10549-012-2104-7

Other articles of this Issue 2/2012

Breast Cancer Research and Treatment 2/2012 Go to the issue

Clinical trial

HER-2 gene amplification by fluorescence in situ hybridization (FISH) compared with immunohistochemistry (IHC) in breast cancer: a study of 528 equivocal cases

Letter to the Editor

A bias in genotyping the miR-27a rs895819 and rs11671784 variants

Epidemiology

Body size and breast cancer prognosis in relation to hormone receptor and menopausal status: a meta-analysis

Preclinical Study

Low expression of ULK1 is associated with operable breast cancer progression and is an adverse prognostic marker of survival for patients

Clinical trial

TOP2A RNA expression and recurrence in estrogen receptor-positive breast cancer

Clinical Trial

Expression of activated type I receptor tyrosine kinases in early breast cancer
Webinar | 19-02-2024 | 17:30 (CET)

Keynote webinar | Spotlight on antibody–drug conjugates in cancer

Watch now

Antibody–drug conjugates (ADCs) are novel agents that have shown promise across multiple tumor types. Explore the current landscape of ADCs in breast and lung cancer with our experts, and gain insights into the mechanism of action, key clinical trials data, existing challenges, and future directions.

Dr. Véronique Diéras
Prof. Fabrice Barlesi
Developed by: Springer Medicine
Image Credits