Skip to main content

Estrogen Receptor Pathways and Breast Cancer

  • Chapter
Principles of Molecular Oncology

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 169.00
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Hardcover Book
USD 219.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

References

  1. 1. Lacey JV, Jr., Devesa SS, Brinton LA. 2002 Recent trends in breast cancer incidence and mortality. Environ Mol Mutagen.; 39:82–88

    PubMed  CAS  Google Scholar 

  2. 2. Jemal A, Siegel R, Ward E, Murray T, Xu J, Smigal C, Thun MJ 2006 Cancer Statistics, 2006. CA Cancer J Clin 56:106–130

    PubMed  Google Scholar 

  3. 3. Chlebowski RT 2002 Breast cancer risk reduction: Strategies for women at increased risk. Annu Rev Med 53:519–540

    PubMed  CAS  Google Scholar 

  4. 4. Beatson GT 1896 On the treatment of inoperable cases of carcinoma of the mamma: Suggestions for a new method of treatment with illustrative cases. Lancet 2:104–107

    Google Scholar 

  5. 5. Boyd S 1900 On oophorectomy in cancer of the breast. B M J ii:1161–1167

    Google Scholar 

  6. 6. Jensen EV, Jacobson HI 1962 Basic guides to the mechanism of estrogen action. Recent Prog Horm Res 18:387–414

    CAS  Google Scholar 

  7. 7. Toft D, Gorski J 1966 A receptor molecule for estrogens: isolation from the rat uterus and preliminary characterization. Proc Natl Acad Sci USA 55:1574–1581

    PubMed  CAS  Google Scholar 

  8. 8. Jensen EV, Suzuki T, Kawashima T, Stumpf WE, Jungblut PW, DeSombre ER 1968 A two step mechanism for the interaction of estradiol with rat uterus. Proc Natl Acad Sci USA 95:632–638

    Google Scholar 

  9. 9. Green S, Walter P, Kumar V, Krust A, Bornert JM, Argos P, Chambon P 1986 Human oestrogen receptor cDNA: sequence, expression and homology to v- erb-A. Nature 320:134–139

    PubMed  CAS  Google Scholar 

  10. 10. Greene GL, Gilna P, Waterfield M, Baker A, Hort Y, Shine J 1986 Sequence and expression of human estrogen receptor complementary DNA. Science 231:1150–1154

    PubMed  CAS  Google Scholar 

  11. 11. Kuiper GG, Enmark E, Pelto-Huikko M, Nilsson S, Gustafsson JA 1996 Cloning of a novel receptor expressed in rat prostate and ovary. Proc Natl Acad Sci USA 93:5925–5930

    PubMed  CAS  Google Scholar 

  12. 12. Enmark E, Pelto-Huikko M, Grandien K, Lagercrantz S, Lagercrantz J, Fried G, Nordenskjold M, Gustafsson JA 1997 Human estrogen receptor beta-gene structure, chromosomal localization, and expression pattern. J Clin Endocrinol Metab 82:4258–4265

    PubMed  CAS  Google Scholar 

  13. 13. Enmark E, Gustafsson JA 1999 Oestrogen receptors—an overview. J Intern Med 246:133–138

    PubMed  CAS  Google Scholar 

  14. 14. Saville B, Wormke M, Wang F, Nguyen T, Enmark E, Kuiper G, Gustafsson JA, Safe S 2000 Ligand-, cell-, and estrogen receptor subtype (alpha/beta)-dependent activation at GC-rich (Sp1) promoter elements. J Biol Chem 275:5379–5387

    PubMed  CAS  Google Scholar 

  15. 15. Nilsson S, Gustafsson JA 2002 Estrogen receptor action. Crit Rev Eukaryot Gene Expr 12:237–257

    PubMed  CAS  Google Scholar 

  16. 16. Chang EC, Frasor J, Komm B, Katzenellenbogen BS 2006 Impact of estrogen receptor beta on gene networks regulated by estrogen receptor alpha in breast cancer cells. Endocrinology 147:4831–4842

    PubMed  CAS  Google Scholar 

  17. 17. Barkhem T, Nilsson S, Gustafsson JA 2004 Molecular mechanisms, physiological consequences and pharmacological implications of estrogen receptor action. Am J Pharmacogenomics 4:19–28

    PubMed  CAS  Google Scholar 

  18. 18. Toran-Allerand CD 2004 Estrogen and the brain: beyond ER-alpha and ER-beta. Exp Gerontol 39:1579–1586

    PubMed  CAS  Google Scholar 

  19. 19. Filardo EJ, Quinn JA, Frackelton AR, Jr., Bland KI 2002 Estrogen action via the G protein-coupled receptor, GPR30: Stimulation of adenylyl cyclase and cAMP-mediated attenuation of the epidermal growth factor receptor-to-MAPK signaling axis. Mol Endocrinol 16:70–84

    PubMed  CAS  Google Scholar 

  20. 20. Funakoshi T, Yanai A, Shinoda K, Kawano MM, Mizukami Y 2006 G protein-coupled receptor 30 is an estrogen receptor in the plasma membrane. Biochem Biophys Res Commun 346:904–910

    PubMed  CAS  Google Scholar 

  21. 21. Revankar CM, Cimino DF, Sklar LA, Arterburn JB, Prossnitz ER 2005 A transmembrane intracellular estrogen receptor mediates rapid cell signaling. Science 307:1625–1630

    PubMed  CAS  Google Scholar 

  22. 22. Tsai MJ, O'Malley BW 1994 Molecular mechanisms of action of steroid/thyroid receptor superfamily members. Annu Rev Biochem 63:451–486

    PubMed  CAS  Google Scholar 

  23. 23. Weatherman RV, Fletterick RJ, Scanlan TS 1999 Nuclear-receptor ligands and ligand-binding domains. Annu Rev Biochem 68:559–581

    PubMed  CAS  Google Scholar 

  24. 24. Xie W, Evans RM 2001 Orphan nuclear receptors: the exotics of xenobiotics. J Biol Chem 276:37739–37742

    PubMed  CAS  Google Scholar 

  25. 25. Thornton JW 2001 Evolution of vertebrate steroid receptors from an ancestral estrogen receptor by ligand exploitation and serial genome expansions. Proc Natl Acad Sci USA 98:5671–5676

    PubMed  CAS  Google Scholar 

  26. 26. Kuiper GG, Lemmen JG, Carlsson B, Corton JC, Safe SH, van der Saag PT, van der Burg B, Gustafsson JA 1998 Interaction of estrogenic chemicals and phytoestrogens with estrogen receptor beta. Endocrinology 139:4252–4263.

    PubMed  CAS  Google Scholar 

  27. 27. Mosselman S, Polman J, Dijkema R 1996 ER beta: Identification and characterization of a novel human estrogen receptor. FEBS Lett 392:49–53

    PubMed  CAS  Google Scholar 

  28. 28. Pettersson K, Grandien K, Kuiper GG, Gustafsson JA 1997 Mouse estrogen receptor beta forms estrogen response element-binding heterodimers with estrogen receptor alpha. Mol Endocrinol 11:1486–1496

    PubMed  CAS  Google Scholar 

  29. 29. Berry M, Metzger D, Chambon P 1990 Role of the two activating domains of the oestrogen receptor in the cell-type and promoter-context dependent agonistic activity of the anti-oestrogen 4-hydroxytamoxifen. EMBO J 9:2811–2818

    PubMed  CAS  Google Scholar 

  30. 30. Nilsson S, Makela S, Treuter E, Tujague M, Thomsen J, Andersson G, Enmark E, Pettersson K, Warner M, Gustafsson JA 2001 Mechanisms of estrogen action. Physiol Rev 81:1535–1565

    PubMed  CAS  Google Scholar 

  31. 31. Ariazi EA, Ariazi JL, Cordera F, Jordan VC 2006 Estrogen receptors as therapeutic targets in breast cancer. Curr Top Med Chem 6:181–202

    PubMed  CAS  Google Scholar 

  32. 32. Onate SA, Boonyaratanakornkit V, Spencer TE, Tsai SY, Tsai MJ, Edwards DP, O'Malley BW 1998 The steroid receptor coactivator-1 contains multiple receptor interacting and activation domains that cooperatively enhance the activation function 1 (AF1) and AF2 domains of steroid receptors. J Biol Chem 273:12101–12108

    PubMed  CAS  Google Scholar 

  33. 33. Webb P, Nguyen P, Shinsako J, Anderson C, Feng W, Nguyen MP, Chen D, Huang SM, Subramanian S, McKinerney E, Katzenellenbogen BS, Stallcup MR, Kushner PJ 1998 Estrogen receptor activation function 1 works by binding p160 coactivator proteins. Mol Endocrinol 12:1605–1618

    PubMed  CAS  Google Scholar 

  34. 34. Zhang H, Xie X, Zhu X, Zhu J, Hao C, Lu Q, Ding L, Liu Y, Zhou L, Liu Y, Huang C, Wen C, Ye Q 2005 Stimulatory cross-talk between NFAT3 and estrogen receptor in breast cancer cells. J Biol Chem 280:43188–43197

    PubMed  CAS  Google Scholar 

  35. 35. Montano MM, Katzenellenbogen BS 1997 The quinone reductase gene: a unique estrogen receptor-regulated gene that is activated by antiestrogens. Proc Natl Acad Sci USA 94:2581–2586

    PubMed  CAS  Google Scholar 

  36. 36. Paech K, Webb P, Kuiper GG, Nilsson S, Gustafsson J, Kushner PJ, Scanlan TS 1997 Differential ligand activation of estrogen receptors ERalpha and ERbeta at AP1 sites [see comments]. Science 277:1508–1510

    PubMed  CAS  Google Scholar 

  37. 37. McInerney EM, Weis KE, Sun J, Mosselman S, Katzenellenbogen BS 1998 Transcription activation by the human estrogen receptor subtype beta (ER beta) studied with ER beta and ER alpha receptor chimeras. Endocrinology 139:4513–4522

    PubMed  CAS  Google Scholar 

  38. 38. Montano MM, Jaiswal AK, Katzenellenbogen BS 1998 Transcriptional regulation of the human quinone reductase gene by antiestrogen-liganded estrogen receptor-alpha and estrogen receptor-beta. J Biol Chem 273:25443–25449

    PubMed  CAS  Google Scholar 

  39. 39. Webb P, Nguyen P, Valentine C, Lopez GN, Kwok GR, McInerney E, Katzenellenbogen BS, Enmark E, Gustafsson JA, Nilsson S, Kushner PJ 1999 The estrogen receptor enhances AP-1 activity by two distinct mechanisms with different requirements for receptor transactivation functions. Mol Endocrinol 13:1672–1685

    PubMed  CAS  Google Scholar 

  40. 40. McDonnell DP, Clemm DL, Hermann T, Goldman ME, Pike JW 1995 Analysis of estrogen receptor function in vitro reveals three distinct classes of antiestrogens. Mol Endocrinol 9:659–669

    PubMed  CAS  Google Scholar 

  41. 41. Cowley SM, Parker MG 1999 A comparison of transcriptional activation by ER alpha and ER beta. J Steroid Biochem Mol Biol 69:165–175

    PubMed  CAS  Google Scholar 

  42. 42. Smith CL, O'Malley BW 2004 Coregulator function: a key to understanding tissue specificity of selective receptor modulators. Endocr Rev 25:45–71

    PubMed  CAS  Google Scholar 

  43. 43. Detka D, Kalita K, Kaczmarek L 2006 Activation function 1 domain plays a negative role in dimerization of estrogen receptor beta. J Steroid Biochem Mol Biol 99:157–160

    PubMed  CAS  Google Scholar 

  44. 44. Liu Z, Shi HY, Nawaz Z, Zhang M 2004 Tamoxifen induces the expression of maspin through estrogen receptor-alpha. Cancer Lett 209:55–65

    PubMed  CAS  Google Scholar 

  45. 45. McInerney EM, Katzenellenbogen BS 1996 Different regions in activation function-1 of the human estrogen receptor required for antiestrogen- and estradiol-dependent transcription activation. J Biol Chem 271:24172–24178

    PubMed  CAS  Google Scholar 

  46. 46. Kushner PJ, Agard DA, Greene GL, Scanlan TS, Shiau AK, Uht RM, Webb P 2000 Estrogen receptor pathways to AP-1. J Steroid Biochem Mol Biol 74:311–317

    PubMed  CAS  Google Scholar 

  47. 47. Song RX, McPherson RA, Adam L, Bao Y, Shupnik M, Kumar R, Santen RJ 2002 Linkage of rapid estrogen action to MAPK activation by ERalpha-Shc association and Shc pathway activation. Mol Endocrinol 16:116–127

    PubMed  CAS  Google Scholar 

  48. 48. Lu Q, Pallas DC, Surks HK, Baur WE, Mendelsohn ME, Karas RH 2004 Striatin assembles a membrane signaling complex necessary for rapid, nongenomic activation of endothelial NO synthase by estrogen receptor alpha. Proc Natl Acad Sci USA 101:17126–17131

    PubMed  CAS  Google Scholar 

  49. 49. Le Goff P, Montano MM, Schodin DJ, Katzenellenbogen BS 1994 Phosphorylation of the human estrogen receptor. Identification of hormone-regulated sites and examination of their influence on transcriptional activity. J Biol Chem 269:4458–4466

    PubMed  CAS  Google Scholar 

  50. 50. Ali S, Metzger D, Bornert JM, Chambon P 1993 Modulation of transcriptional activation by ligand-dependent phosphorylation of the human oestrogen receptor A/B region. Embo J 12:1153–1160

    PubMed  CAS  Google Scholar 

  51. 51. Joel PB, Traish AM, Lannigan DA 1995 Estradiol and phorbol ester cause phosphorylation of serine 118 in the human estrogen receptor. Mol Endocrinol 9:1041–1052

    PubMed  CAS  Google Scholar 

  52. 52. Medunjanin S, Hermani A, De Servi B, Grisouard J, Rincke G, Mayer D 2005 Glycogen synthase kinase-3 interacts with and phosphorylates estrogen receptor alpha and is involved in the regulation of receptor activity. J Biol Chem 280:33006–33014

    PubMed  CAS  Google Scholar 

  53. 53. Kato S, Endoh H, Masuhiro Y, Kitamoto T, Uchiyama S, Sasaki H, Masushige S, Gotoh Y, Nishida E, Kawashima H, et al. 1995 Activation of the estrogen receptor through phosphorylation by mitogen- activated protein kinase. Science 270:1491–1494

    PubMed  CAS  Google Scholar 

  54. 54. Bunone G, Briand PA, Miksicek RJ, Picard D 1996 Activation of the unliganded estrogen receptor by EGF involves the MAP kinase pathway and direct phosphorylation. Embo J 15:2174–2183

    PubMed  CAS  Google Scholar 

  55. 55. Migliaccio A, Di Domenico M, Castoria G, de Falco A, Bontempo P, Nola E, Auricchio F 1996 Tyrosine kinase/p21ras/MAP-kinase pathway activation by estradiol-receptor complex in MCF-7 cells. Embo J 15:1292–1300

    PubMed  CAS  Google Scholar 

  56. 56. Migliaccio A, Piccolo D, Castoria G, Di Domenico M, Bilancio A, Lombardi M, Gong W, Beato M, Auricchio F 1998 Activation of the Src/p21ras/Erk pathway by progesterone receptor via cross-talk with estrogen receptor. Embo J 17:2008–2018

    PubMed  CAS  Google Scholar 

  57. 57. Migliaccio A, Castoria G, Di Domenico M, de Falco A, Bilancio A, Lombardi M, Barone MV, Ametrano D, Zannini MS, Abbondanza C, Auricchio F 2000 Steroid-induced androgen receptor-oestradiol receptor beta-Src complex triggers prostate cancer cell proliferation. Embo J 19:5406–5417

    PubMed  CAS  Google Scholar 

  58. 58. Martin MB, Franke TF, Stoica GE, Chambon P, Katzenellenbogen BS, Stoica BA, McLemore MS, Olivo SE, Stoica A 2000 A role for Akt in mediating the estrogenic functions of epidermal growth factor and insulin-like growth factor I. Endocrinology 141:4503–4511

    PubMed  CAS  Google Scholar 

  59. 59. Joel PB, Smith J, Sturgill TW, Fisher TL, Blenis J, Lannigan DA 1998 pp90rsk1 regulates estrogen receptor-mediated transcription through phosphorylation of Ser-167. Mol Cell Biol 18:1978–1984

    PubMed  CAS  Google Scholar 

  60. 60. Arnold SF, Obourn JD, Jaffe H, Notides AC 1995 Phosphorylation of the human estrogen receptor by mitogen-activated protein kinase and casein kinase II: consequence on DNA binding. J Steroid Biochem Mol Biol 55:163–172

    PubMed  CAS  Google Scholar 

  61. 61. Arnold SF, Obourn JD, Jaffe H, Notides AC 1994 Serine 167 is the major estradiol-induced phosphorylation site on the human estrogen receptor. Mol Endocrinol 8:1208–1214

    PubMed  CAS  Google Scholar 

  62. 62. Frodin M, Gammeltoft S 1999 Role and regulation of 90 kDa ribosomal S6 kinase (RSK) in signal transduction. Mol Cell Endocrinol 151:65–77

    PubMed  CAS  Google Scholar 

  63. 63. Davies SP, Reddy H, Caivano M, Cohen P 2000 Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J 351:95–105

    PubMed  CAS  Google Scholar 

  64. 64. Campbell RA, Bhat-Nakshatri P, Patel NM, Constantinidou D, Ali S, Nakshatri H 2001 Phosphatidylinositol 3-kinase/AKT-mediated activation of estrogen receptor alpha: a new model for anti-estrogen resistance. J Biol Chem 276:9817–9824

    PubMed  CAS  Google Scholar 

  65. 65. Sun M, Paciga JE, Feldman RI, Yuan Z, Coppola D, Lu YY, Shelley SA, Nicosia SV, Cheng JQ 2001 Phosphatidylinositol-3-OH Kinase (PI3K)/AKT2, activated in breast cancer, regulates and is induced by estrogen receptor alpha (ERalpha) via interaction between ERalpha and PI3K. Cancer Res 61:5985–5991

    PubMed  CAS  Google Scholar 

  66. 66. Osborne CK, Shou J, Massarweh S, Schiff R 2005 Crosstalk between estrogen receptor and growth factor receptor pathways as a cause for endocrine therapy resistance in breast cancer. Clin Cancer Res 11:865s–870s

    PubMed  CAS  Google Scholar 

  67. 67. Glass CK 1994 Differential recognition of target genes by nuclear receptor monomers, dimers, and heterodimers. Endocr Rev 15:391–407

    PubMed  CAS  Google Scholar 

  68. 68. Schwabe JW, Chapman L, Finch JT, Rhodes D 1993 The crystal structure of the estrogen receptor DNA-binding domain bound to DNA: How receptors discriminate between their response elements. Cell 75:567–578

    PubMed  CAS  Google Scholar 

  69. 69. Vanacker JM, Pettersson K, Gustafsson JA, Laudet V 1999 Transcriptional targets shared by estrogen receptor-related receptors (ERRs) and estrogen receptor (ER) alpha, but not by ERbeta. EMBO J 18:4270–4279

    PubMed  CAS  Google Scholar 

  70. 70. Kuntz MA, Shapiro DJ 1997 Dimerizing the estrogen receptor DNA binding domain enhances binding to estrogen response elements. J Biol Chem 272:27949–27956

    PubMed  CAS  Google Scholar 

  71. 71. Hard T, Kellenbach E, Boelens R, Maler BA, Dahlman K, Freedman LP, Carlstedt-Duke J, Yamamoto KR, Gustafsson JA, Kaptein R 1990 Solution structure of the glucocorticoid receptor DNA-binding domain. Science 249:157–160

    PubMed  CAS  Google Scholar 

  72. 72. Schwabe JW, Neuhaus D, Rhodes D 1990 Solution structure of the DNA-binding domain of the oestrogen receptor. Nature 348:458–461

    PubMed  CAS  Google Scholar 

  73. 73. Green S, Kumar V, Theulaz I, Wahli W, Chambon P 1988 The N-terminal DNA-binding ‘zinc finger’ of the oestrogen and glucocorticoid receptors determines target gene specificity. Embo J 7:3037–3044

    PubMed  CAS  Google Scholar 

  74. 74. Kumar V, Chambon P 1988 The estrogen receptor binds tightly to its responsive element as a ligand-induced homodimer. Cell 55:145–156

    PubMed  CAS  Google Scholar 

  75. 75. Wei X, Xu H, Kufe D 2006 MUC1 oncoprotein stabilizes and activates estrogen receptor alpha. Mol Cell 21:295–305

    PubMed  CAS  Google Scholar 

  76. 76. Bjornstrom L, Sjoberg M 2002 Mutations in the estrogen receptor DNA-binding domain discriminate between the classical mechanism of action and cross-talk with Stat5b and activating protein 1 (AP-1). J Biol Chem 277:48479–48483

    PubMed  CAS  Google Scholar 

  77. 77. Boerner JL, Gibson MA, Fox EM, Posner ED, Parsons SJ, Silva CM, Shupnik MA 2005 Estrogen negatively regulates epidermal growth factor (EGF)-mediated signal transducer and activator of transcription 5 signaling in human EGF family receptor-overexpressing breast cancer cells. Mol Endocrinol 19:2660–2670

    PubMed  CAS  Google Scholar 

  78. 78. Jackson TA, Richer JK, Bain DL, Takimoto GS, Tung L, Horwitz KB 1997 The partial agonist activity of antagonist-occupied steroid receptors is controlled by a novel hinge domain-binding coactivator L7/SPA and the corepressors N-CoR or SMRT. Mol Endocrinol 11:693–705

    PubMed  CAS  Google Scholar 

  79. 79. Bu H, Kashireddy P, Chang J, Zhu YT, Zhang Z, Zheng W, Rao SM, Zhu YJ 2004 ERBP, a novel estrogen receptor binding protein enhancing the activity of estrogen receptor. Biochem Biophys Res Commun 317:54–59

    PubMed  CAS  Google Scholar 

  80. 80. Tcherepanova I, Puigserver P, Norris JD, Spiegelman BM, McDonnell DP 2000 Modulation of estrogen receptor-alpha transcriptional activity by the coactivator PGC-1. J Biol Chem 275:16302–16308

    PubMed  CAS  Google Scholar 

  81. 81. Lee SR, Ramos SM, Ko A, Masiello D, Swanson KD, Lu ML, Balk SP 2002 AR and ER interaction with a p21-activated kinase (PAK6). Mol Endocrinol 16:85–99

    PubMed  CAS  Google Scholar 

  82. 82. Wang C, Fan S, Li Z, Fu M, Rao M, Ma Y, Lisanti MP, Albanese C, Katzenellenbogen BS, Kushner PJ, Weber B, Rosen EM, Pestell RG 2005 Cyclin D1 antagonizes BRCA1 repression of estrogen receptor alpha activity. Cancer Res 65:6557–6567

    PubMed  CAS  Google Scholar 

  83. 83. Muller S, Ledl A, Schmidt D 2004 SUMO: a regulator of gene expression and genome integrity. Oncogene 23:1998–2008

    PubMed  Google Scholar 

  84. 84. Gill G 2005 Something about SUMO inhibits transcription. Curr Opin Genet Dev 15:536–541

    PubMed  CAS  Google Scholar 

  85. 85. Sentis S, Le Romancer M, Bianchin C, Rostan MC, Corbo L 2005 Sumoylation of the estrogen receptor alpha hinge region regulates its transcriptional activity. Mol Endocrinol 19:2671–2684

    PubMed  CAS  Google Scholar 

  86. 86. Kim K, Thu N, Saville B, Safe S 2003 Domains of estrogen receptor alpha (ERalpha) required for ERalpha/Sp1-mediated activation of GC-rich promoters by estrogens and antiestrogens in breast cancer cells. Mol Endocrinol 17:804–817

    PubMed  CAS  Google Scholar 

  87. 87. Evans RM 1988 The steroid and thyroid hormone superfamily. Science 240:889–895

    PubMed  CAS  Google Scholar 

  88. 88. Giguere V, Yang N, Segui P, Evans RM 1988 Identification of a new class of steroid hormone receptors. Nature 331:91–94

    PubMed  CAS  Google Scholar 

  89. 89. Steinmetz AC, Renaud JP, Moras D 2001 Binding of ligands and activation of transcription by nuclear receptors. Annu Rev Biophys Biomol Struct 30:329–359

    PubMed  CAS  Google Scholar 

  90. 90. 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 389:753–758

    PubMed  CAS  Google Scholar 

  91. 91. Shiau AK, Barstad D, Loria PM, Cheng L, Kushner PJ, Agard DA, Greene GL. 1998 The structural basis of estrogen receptor/co-activator recognition and the antagonism of this interaction by tamoxifen. Cell 95:927–937

    PubMed  CAS  Google Scholar 

  92. 92. Tanenbaum DM, Wang Y, Williams SP, Sigler PB 1998 Crystallographic comparison of the estrogen and progesterone receptor's ligand binding domains. Proceedings of the National Academy of Sciences of the United States of America 95:5998–6003

    PubMed  CAS  Google Scholar 

  93. 93. Pettersson K, Gustafsson JA 2001 Role of estrogen receptor beta in estrogen action. Annu Rev Physiol 63:165–192

    PubMed  CAS  Google Scholar 

  94. 94. Bourguet W, Germain P, Gronemeyer H 2000 Nuclear receptor ligand-binding domains: Three-dimensional structures, molecular interactions and pharmacological implications. Trends Pharmacol Sci 21:381–388

    PubMed  CAS  Google Scholar 

  95. 95. Wolf DM, Jordan VC 1994 The estrogen receptor from a tamoxifen stimulated MCF-7 tumor variant contains a point mutation in the ligand binding domain. Breast Cancer Res Treat 31:129–138

    PubMed  CAS  Google Scholar 

  96. 96. Liu H, Lee E.S, De Los Reyes A, Zapf J W, and Jordan, V C 2001 Silencing and reactivation of the selective estrogen receptor modulator-estrogen receptor alpha complex. Cancer Res 61:3632–3639

    PubMed  CAS  Google Scholar 

  97. 97. Liu H, Park, W., Bentrem, D., McKian, K.P., De Los Reyes, A., MacGregor Schafer, J., Zapf, J. and Jordan, V.C. 2002 Structure-function relationships of the raloxifene-estrogen receptor alpha complex for regulating transforming growth factor alpha expression in breast cancer cells. J Biol Chem 277:9189–9198

    PubMed  CAS  Google Scholar 

  98. 98. Wang Y, Chirgadze NY, Briggs SL, Khan S, Jensen EV, Burris TP 2006 A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor {beta}. Proc Natl Acad Sci USA 103:9908–9911

    PubMed  CAS  Google Scholar 

  99. 99. Koehler KF, Helguero LA, Haldosen LA, Warner M, Gustafsson JA 2005 Reflections on the discovery and significance of estrogen receptor beta. Endocr Rev 26:465–478

    PubMed  CAS  Google Scholar 

  100. 100. Harris HA, Katzenellenbogen JA, Katzenellenbogen BS 2002 Characterization of the biological roles of the estrogen receptors, ERalpha and ERbeta, in estrogen target tissues in vivo through the use of an ERalpha-selective ligand. Endocrinology 143:4172–4177

    PubMed  CAS  Google Scholar 

  101. 101. Sun J, Huang YR, Harrington WR, Sheng S, Katzenellenbogen JA, Katzenellenbogen BS 2002 Antagonists selective for estrogen receptor alpha. Endocrinology 143:941–947

    PubMed  CAS  Google Scholar 

  102. 102. Kraichely DM, Sun J, Katzenellenbogen JA, Katzenellenbogen BS 2000 Conformational changes and coactivator recruitment by novel ligands for estrogen receptor-alpha and estrogen receptor-beta: Correlations with biological character and distinct differences among SRC coactivator family members. Endocrinology 141:3534–3545

    PubMed  CAS  Google Scholar 

  103. 103. Shiau AK, Barstad D, Radek JT, Meyers MJ, Nettles KW, Katzenellenbogen BS, Katzenellenbogen JA, Agard DA, Greene GL 2002 Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism. Nat Struct Biol 9:359–364

    PubMed  CAS  Google Scholar 

  104. 104. Pierrat B, Heery DM, Chambon P, Losson R 1994 A highly conserved region in the hormone-binding domain of the human estrogen receptor functions as an efficient transactivation domain in yeast. Gene 143:193–200

    PubMed  CAS  Google Scholar 

  105. 105. Norris JD, Fan D, Kerner SA, and McDonnell D P 1997 Identification of a third autonomous activation domain within the human estrogen receptor. Mol Endocrinol 11:747–754

    PubMed  CAS  Google Scholar 

  106. 106. Jacq X, Brou C, Lutz Y, Davidson I, Chambon P, Tora L 1994 Human TAFII30 is present in a distinct TFIID complex and is required for transcriptional activation by the estrogen receptor. Cell 79:107–117

    PubMed  CAS  Google Scholar 

  107. 107. Nawaz Z, Lonard DM, Dennis AP, Smith CL, O'Malley BW 1999 Proteasome-dependent degradation of the human estrogen receptor. Proc Natl Acad Sci USA 96:1858–1862

    PubMed  CAS  Google Scholar 

  108. 108. Lonard DM, Nawaz Z, Smith CL, O'Malley BW 2000 The 26S proteasome is required for estrogen receptor-alpha and coactivator turnover and for efficient estrogen receptor-alpha transactivation. Mol Cell 5:939–948

    PubMed  CAS  Google Scholar 

  109. 109. Reid G, Hubner MR, Metivier R, Brand H, Denger S, Manu D, Beaudouin J, Ellenberg J, Gannon F 2003 Cyclic, proteasome-mediated turnover of unliganded and liganded ERalpha on responsive promoters is an integral feature of estrogen signaling. Mol Cell 11:695–707

    PubMed  CAS  Google Scholar 

  110. 110. Valley CC, Metivier R, Solodin NM, Fowler AM, Mashek MT, Hill L, Alarid ET 2005 Differential regulation of estrogen-inducible proteolysis and transcription by the estrogen receptor alpha N terminus. Mol Cell Biol 25:5417–5428

    PubMed  CAS  Google Scholar 

  111. 111. Herynk MH, Fuqua SA 2004 Estrogen receptor mutations in human disease. Endocr Rev 25:869–898

    PubMed  CAS  Google Scholar 

  112. 112. Penot G, Le Peron C, Merot Y, Grimaud-Fanouillere E, Ferriere F, Boujrad N, Kah O, Saligaut C, Ducouret B, Metivier R, Flouriot G 2005 The human estrogen receptor-alpha isoform hERalpha46 antagonizes the proliferative influence of hERalpha66 in MCF7 breast cancer cells. Endocrinology 146:5474–5484

    PubMed  CAS  Google Scholar 

  113. 113. Wang Z, Zhang X, Shen P, Loggie BW, Chang Y, Deuel TF 2005 Identification, cloning, and expression of human estrogen receptor-alpha36, a novel variant of human estrogen receptor-alpha66. Biochem Biophys Res Commun 336:1023–1027

    PubMed  CAS  Google Scholar 

  114. 114. Wang Z, Zhang X, Shen P, Loggie BW, Chang Y, Deuel TF 2006 A variant of estrogen receptor-{alpha}, hER-{alpha}36: Transduction of estrogen- and antiestrogen-dependent membrane-initiated mitogenic signaling. Proc Natl Acad Sci USA 103:9063–9068

    PubMed  CAS  Google Scholar 

  115. 115. Saji S, Hirose M, Toi M 2005 Clinical significance of estrogen receptor beta in breast cancer. Cancer Chemother Pharmacol 56 Suppl 1:21–26

    Google Scholar 

  116. 116. Hall JM, Couse JF, Korach KS 2001 The multifaceted mechanisms of estradiol and estrogen receptor signaling. J Biol Chem 276:36869–36872

    PubMed  CAS  Google Scholar 

  117. 117. Lonard DM, O'Malley BW 2005 Expanding functional diversity of the coactivators. Trends Biochem Sci 30:126–132

    PubMed  CAS  Google Scholar 

  118. 118. Lonard DM, O'Malley BW 2006 The expanding cosmos of nuclear receptor coactivators. Cell 125:411–414

    PubMed  CAS  Google Scholar 

  119. 119. Wu RC, Smith CL, O'Malley BW 2005 Transcriptional regulation by steroid receptor coactivator phosphorylation. Endocr Rev 26:393–399

    PubMed  CAS  Google Scholar 

  120. 120. Chen D, Ma H, Hong H, Koh SS, Huang SM, Schurter BT, Aswad DW, Stallcup MR 1999 Regulation of transcription by a protein methyltransferase. Science 284:2174–2177

    PubMed  CAS  Google Scholar 

  121. 121. Koh SS, Chen D, Lee YH, Stallcup MR 2001 Synergistic enhancement of nuclear receptor function by p160 coactivators and two coactivators with protein methyltransferase activities. J Biol Chem 276:1089–1098

    PubMed  CAS  Google Scholar 

  122. 122. Metivier R, Penot G, Hubner MR, Reid G, Brand H, Kos M, Gannon F 2003 Estrogen receptor-alpha directs ordered, cyclical, and combinatorial recruitment of cofactors on a natural target promoter. Cell 115:751–763

    PubMed  CAS  Google Scholar 

  123. 123. Jaber BM, Gao T, Huang L, Karmakar S, Smith CL 2006 The pure estrogen receptor antagonist ICI 182,780 promotes a novel interaction of estrogen receptor-{alpha} with the CBP/p300 coactivators. Mol Endocrinol 20:2695–2710

    PubMed  CAS  Google Scholar 

  124. 124. Jepsen K, Rosenfeld MG 2002 Biological roles and mechanistic actions of co-repressor complexes. J Cell Sci 115:689–698

    PubMed  CAS  Google Scholar 

  125. 125. Dobrzycka KM, Townson SM, Jiang S, Oesterreich S 2003 Estrogen receptor corepressors—a role in human breast cancer? Endocr Relat Cancer 10:517–536

    PubMed  CAS  Google Scholar 

  126. 126. Chen JD, Evans RM 1995 A transcriptional co-repressor that interacts with nuclear hormone receptors [see comments]. Nature 377:454–457

    PubMed  CAS  Google Scholar 

  127. 127. Horlein AJ, Naar AM, Heinzel T, Torchia J, Gloss B, Kurokawa R, Ryan A, Kamei Y, Soderstrom M, Glass CK, et al. 1995 Ligand-independent repression by the thyroid hormone receptor mediated by a nuclear receptor co-repressor. Nature 377:397–404

    PubMed  CAS  Google Scholar 

  128. 128. Smith CL, Nawaz Z, O'Malley BW 1997 Coactivator and Corepressor regulation of the agonist/antagonist activity of the mixed antiestrogen, 4-hydroxytamoxifen. Mol Endocrinol 11:657–666

    PubMed  CAS  Google Scholar 

  129. 129. Wagner BL, Norris JD, Knotts TA, Weigel NL, McDonnell DP 1998 The nuclear corepressors NCoR and SMRT are key regulators of both ligand- and 8-bromo-cyclic AMP-dependent transcriptional activity of the human progesterone receptor. Mol Cell Biol 18:1369–1378

    PubMed  CAS  Google Scholar 

  130. 130. DeNardo DG, Kim HT, Hilsenbeck S, Cuba V, Tsimelzon A, Brown PH 2005 Global gene expression analysis of estrogen receptor transcription factor cross talk in breast cancer: Identification of estrogen-induced/activator protein-1-dependent genes. Mol Endocrinol 19:362–378

    PubMed  CAS  Google Scholar 

  131. 131. Barkhem T, Haldosen LA, Gustafsson JA, Nilsson S 2002 Transcriptional synergism on the pS2 gene promoter between a p160 coactivator and estrogen receptor-alpha depends on the coactivator subtype, the type of estrogen response element, and the promoter context. Mol Endocrinol 16:2571–2581

    PubMed  CAS  Google Scholar 

  132. 132. Laganiere J, Deblois G, Giguere V 2005 Functional genomics identifies a mechanism for estrogen activation of the retinoic acid receptor alpha1 gene in breast cancer cells. Mol Endocrinol 19:1584–1592

    PubMed  CAS  Google Scholar 

  133. 133. Bjornstrom L, Sjoberg M 2005 Mechanisms of estrogen receptor signaling: convergence of genomic and nongenomic actions on target genes. Mol Endocrinol 19:833–842

    PubMed  Google Scholar 

  134. 134. Matthews J, Wihlen B, Tujague M, Wan J, Strom A, Gustafsson JA 2006 Estrogen receptor (ER) beta modulates ERalpha-mediated transcriptional activation by altering the recruitment of c-Fos and c-Jun to estrogen-responsive promoters. Mol Endocrinol 20:534–543

    PubMed  CAS  Google Scholar 

  135. 135. Stoner M, Wormke M, Saville B, Samudio I, Qin C, Abdelrahim M, Safe S 2004 Estrogen regulation of vascular endothelial growth factor gene expression in ZR-75 breast cancer cells through interaction of estrogen receptor alpha and SP proteins. Oncogene 23:1052–1063

    PubMed  CAS  Google Scholar 

  136. 136. Higgins KJ, Liu S, Abdelrahim M, Yoon K, Vanderlaag K, Porter W, Metz RP, Safe S 2006 Vascular endothelial growth factor receptor-2 expression is induced by 17beta-estradiol in ZR-75 breast cancer cells by estrogen receptor alpha/Sp proteins. Endocrinology 147:3285–3295

    PubMed  CAS  Google Scholar 

  137. 137. Fujita N, Kajita M, Taysavang P, Wade PA 2004 Hormonal regulation of metastasis-associated protein 3 transcription in breast cancer cells. Mol Endocrinol 18:2937–2949

    PubMed  CAS  Google Scholar 

  138. 138. Wietzke JA, Ward EC, Schneider J, Welsh J 2005 Regulation of the human vitamin D3 receptor promoter in breast cancer cells is mediated through Sp1 sites. Mol Cell Endocrinol 230:59–68

    PubMed  CAS  Google Scholar 

  139. 139. Varshochi R, Halim F, Sunters A, Alao JP, Madureira PA, Hart SM, Ali S, Vigushin DM, Coombes RC, Lam EW 2005 ICI182,780 induces p21Waf1 gene transcription through releasing histone deacetylase 1 and estrogen receptor alpha from Sp1 sites to induce cell cycle arrest in MCF-7 breast cancer cell line. J Biol Chem 280:3185–3196

    PubMed  CAS  Google Scholar 

  140. 140. Stossi F, Likhite VS, Katzenellenbogen JA, Katzenellenbogen BS 2006 Estrogen-occupied estrogen receptor represses cyclin G2 gene expression and recruits a repressor complex at the cyclin G2 promoter. J Biol Chem 281:16272–16278

    PubMed  CAS  Google Scholar 

  141. 141. Galien R, Garcia T 1997 Estrogen receptor impairs interleukin-6 expression by preventing protein binding on the NF-kappaB site. Nucleic Acids Res 25:2424–2429

    PubMed  CAS  Google Scholar 

  142. 142. Biswas DK, Dai SC, Cruz A, Weiser B, Graner E, Pardee AB 2001 The nuclear factor kappa B (NF-kappa B): A potential therapeutic target for estrogen receptor negative breast cancers. Proc Natl Acad Sci USA 98:10386–10391

    PubMed  CAS  Google Scholar 

  143. 143. Biswas DK, Singh S, Shi Q, Pardee AB, Iglehart JD 2005 Crossroads of estrogen receptor and NF-kappaB signaling. Sci STKE 2005(288):pe27

    PubMed  Google Scholar 

  144. 144. Zhou Y, Eppenberger-Castori S, Eppenberger U, Benz CC 2005 The NFkappaB pathway and endocrine-resistant breast cancer. Endocr Relat Cancer 12 Suppl 1:S37–46

    Google Scholar 

  145. 145. Lannigan DA 2003 Estrogen receptor phosphorylation. Steroids 68:1–9

    PubMed  CAS  Google Scholar 

  146. 146. Levin ER 2003 Bidirectional signaling between the estrogen receptor and the epidermal growth factor receptor. Mol Endocrinol 17:309–317

    PubMed  CAS  Google Scholar 

  147. 147. Lopez GN, Turck CW, Schaufele F, Stallcup MR, Kushner PJ 2001 Growth factors signal to steroid receptors through mitogen-activated protein kinase regulation of p160 coactivator activity. J Biol Chem 276:22177–22182

    PubMed  CAS  Google Scholar 

  148. 148. Shupnik MA 2004 Crosstalk between steroid receptors and the c-Src-receptor tyrosine kinase pathways: Implications for cell proliferation. Oncogene 23:7979–7989

    PubMed  CAS  Google Scholar 

  149. 149. Glaros S, Atanaskova N, Zhao C, Skafar DF, Reddy KB 2006 Activation function-1 domain of estrogen receptor regulates the agonistic and antagonistic actions of tamoxifen. Mol Endocrinol 20:996–1008

    PubMed  CAS  Google Scholar 

  150. 150. Rayala SK, Talukder AH, Balasenthil S, Tharakan R, Barnes CJ, Wang RA, Aldaz M, Khan S, Kumar R 2006 P21-activated kinase 1 regulation of estrogen receptor-alpha activation involves serine 305 activation linked with serine 118 phosphorylation. Cancer Res 66:1694–1701

    PubMed  CAS  Google Scholar 

  151. 151. Shou J, Massarweh S, Osborne CK, Wakeling AE, Ali S, Weiss H, Schiff R 2004 Mechanisms of tamoxifen resistance: increased estrogen receptor-HER2/neu cross-talk in ER/HER2-positive breast cancer. J Natl Cancer Inst 96:926–935

    PubMed  CAS  Google Scholar 

  152. 152. Trowbridge JM, Rogatsky I, Garabedian MJ 1997 Regulation of estrogen receptor transcriptional enhancement by the cyclin A/Cdk2 complex. Proc Natl Acad Sci USA 94:10132–10137

    PubMed  CAS  Google Scholar 

  153. 153. Zwijsen RM, Buckle RS, Hijmans EM, Loomans CJ, Bernards R 1998 Ligand-independent recruitment of steroid receptor coactivators to estrogen receptor by cyclin D1. Genes Dev 12:3488–3498

    PubMed  CAS  Google Scholar 

  154. 154. Liu MM, Albanese C, Anderson CM, Hilty K, Webb P, Uht RM, Price RH, Jr., Pestell RG, Kushner PJ 2002 Opposing action of estrogen receptors alpha and beta on cyclin D1 gene expression. J Biol Chem 277:24353–24360

    PubMed  CAS  Google Scholar 

  155. 155. Levin ER 2005 Integration of the extranuclear and nuclear actions of estrogen. Mol Endocrinol 19:1951–1959

    PubMed  CAS  Google Scholar 

  156. 156. Manavathi B, Kumar R 2006 Steering estrogen signals from the plasma membrane to the nucleus: Two sides of the coin. J Cell Physiol 207:594–604

    PubMed  CAS  Google Scholar 

  157. 157. Pietras R, Szego CM 1977 Specific binding sites for oestrogen at the outer surfaces of isolated endometrial cells. Nature 265:69–72

    PubMed  CAS  Google Scholar 

  158. 158. Pappas TC, Gametchu B, Watson CS 1995 Membrane estrogen receptors identified by multiple antibody labeling and impeded-ligand binding. Faseb J 9:404–410

    PubMed  CAS  Google Scholar 

  159. 159. Norfleet AM, Thomas ML, Gametchu B, Watson CS 1999 Estrogen receptor-alpha detected on the plasma membrane of aldehyde-fixed GH3/B6/F10 rat pituitary tumor cells by enzyme-linked immunocytochemistry. Endocrinology 140:3805–3814

    PubMed  CAS  Google Scholar 

  160. 160. Razandi M, Pedram A, Green GL, Levin ER 1999 Cell membrane and nuclear estrogen receptors (ERs) originate from a single transcript: Studies of ER alpha and ER beta expressed in Chinese hamster ovary cells. Endocrinology 13:307–319

    CAS  Google Scholar 

  161. 161. Ropero AB, Soria B, Nadal A 2002 A nonclassical estrogen membrane receptor triggers rapid differential actions in the endocrine pancreas. Mol Endocrinol 16:497–505

    PubMed  CAS  Google Scholar 

  162. 162. Watson CS, Campbell CH, Gametchu B 2002 The dynamic and elusive membrane estrogen receptor-alpha. Steroids 67:429–437

    PubMed  CAS  Google Scholar 

  163. 163. Acconcia F, Ascenzi P, Bocedi A, Spisni E, Tomasi V, Trentalance A, Visca P, Marino M 2005 Palmitoylation-dependent estrogen receptor alpha membrane localization: Regulation by 17beta-estradiol. Mol Biol Cell 16:231–237

    PubMed  CAS  Google Scholar 

  164. 164. Song RX, Barnes CJ, Zhang Z, Bao Y, Kumar R, Santen RJ 2004 The role of Shc and insulin-like growth factor 1 receptor in mediating the translocation of estrogen receptor alpha to the plasma membrane. Proc Natl Acad Sci USA 101:2076–2081

    PubMed  CAS  Google Scholar 

  165. 165. Vadlamudi RK, Wang RA, Mazumdar A, Kim Y, Shin J, Sahin A, Kumar R 2001 Molecular cloning and characterization of PELP1, a novel human coregulator of estrogen receptor alpha. J Biol Chem 276:38272–38279

    PubMed  CAS  Google Scholar 

  166. 166. Wong CW, McNally C, Nickbarg E, Komm BS, Cheskis BJ 2002 Estrogen receptor-interacting protein that modulates its nongenomic activity-crosstalk with Src/Erk phosphorylation cascade. Proc Natl Acad Sci USA 99:14783–14788

    PubMed  CAS  Google Scholar 

  167. 167. Vadlamudi RK, Manavathi B, Balasenthil S, Nair SS, Yang Z, Sahin AA, Kumar R 2005 Functional implications of altered subcellular localization of PELP1 in breast cancer cells. Cancer Res 65:7724–7732

    PubMed  CAS  Google Scholar 

  168. 168. Cabodi S, Moro L, Baj G, Smeriglio M, Di Stefano P, Gippone S, Surico N, Silengo L, Turco E, Tarone G, Defilippi P 2004 p130Cas interacts with estrogen receptor alpha and modulates non-genomic estrogen signaling in breast cancer cells. J Cell Sci 117:1603–1611

    PubMed  CAS  Google Scholar 

  169. 169. Fernando RI, Wimalasena J 2004 Estradiol abrogates apoptosis in breast cancer cells through inactivation of BAD: Ras-dependent nongenomic pathways requiring signaling through ERK and Akt. Mol Biol Cell 15:3266–3284

    PubMed  CAS  Google Scholar 

  170. 170. Zhang GJ, Kimijima I, Onda M, Kanno M, Sato H, Watanabe T, Tsuchiya A, Abe R, Takenoshita S 1999 Tamoxifen-induced apoptosis in breast cancer cells relates to down-regulation of bcl-2, but not bax and bcl-X(L), without alteration of p53 protein levels. Clin Cancer Res 5:2971–2977

    PubMed  CAS  Google Scholar 

  171. 171. Schlegel A, Wang C, Katzenellenbogen BS, Pestell RG, Lisanti MP 1999 Caveolin-1 potentiates estrogen receptor alpha (ERalpha) signaling. caveolin-1 drives ligand-independent nuclear translocation and activation of ERalpha. J Biol Chem 274:33551–33556

    PubMed  CAS  Google Scholar 

  172. 172. Kumar R, Wang RA, Mazumdar A, Talukder AH, Mandal M, Yang Z, Bagheri-Yarmand R, Sahin A, Hortobagyi G, Adam L, Barnes CJ, Vadlamudi RK 2002 A naturally occurring MTA1 variant sequesters oestrogen receptor-alpha in the cytoplasm. Nature 418:654–657

    PubMed  CAS  Google Scholar 

  173. 173. Thomas P, Pang Y, Filardo EJ, Dong J 2005 Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. Endocrinology 146:624–632

    PubMed  CAS  Google Scholar 

  174. 174. Maggiolini M, Vivacqua A, Fasanella G, Recchia AG, Sisci D, Pezzi V, Montanaro D, Musti AM, Picard D, Ando S 2004 The G protein-coupled receptor GPR30 mediates c-fos up-regulation by 17beta-estradiol and phytoestrogens in breast cancer cells. J Biol Chem 279:27008–27016

    PubMed  CAS  Google Scholar 

  175. 175. Pedram A, Razandi M, Levin ER 2006 Nature of functional estrogen receptors at the plasma membrane. Mol Endocrinol 20:1996–2009

    PubMed  CAS  Google Scholar 

  176. 176. Ahola TM, Manninen T, Alkio N, Ylikomi T 2002 G protein-coupled receptor 30 is critical for a progestin-induced growth inhibition in MCF-7 breast cancer cells. Endocrinology 143:3376–3384

    PubMed  CAS  Google Scholar 

  177. 177. Jensen EV, Jordan VC 2003 The estrogen receptor: a model for molecular medicine. The Dorothy P. Landon AACR Prize for Translational Research. Clin Cancer Res 9:1980–1989

    CAS  Google Scholar 

  178. 178. Jordan VC 2003 Tamoxifen: A most unlikely pioneering medicine. Nature Reviews Drug Discovery 2:205–213

    PubMed  CAS  Google Scholar 

  179. EBCTCG 2005 Effects of chemotherapy and hormonal therapy for early breast cancer on recurrence and 15-year survival: an overview of the randomised trials. Lancet 365:1687–1717

    Google Scholar 

  180. 180. Goss PE, Ingle J N, Martino S et al. 2003 A randomized trial of letrozole in postmenopausal women after five years of tamoxifen therapy for early-stage breast cancer. New Engl J Med 349:1793–1802.

    PubMed  CAS  Google Scholar 

  181. 181. Howell A, Cuzick J, Baum M, Buzdar A, Dowsett M, Forbes JF, Hoctin-Boes G, Houghton J, Locker GY, Tobias JS, Group AT 2005 Results of the ATAC (Arimidex, Tamoxifen, Alone or in Combination) trial after completion of 5 years' adjuvant treatment for breast cancer. Lancet 365:60–62

    PubMed  CAS  Google Scholar 

  182. Thurlimann B, Keshaviah A, Coates AS, Mouridsen H, Mauriac L, Forbes JF, Paridaens R, Castiglione-Gertsch M, Gelber RD, Rabaglio M, Smith I, Wardly A, Price KN, Goldhirsch A, BIG (Breast International Group), Group I-C 2005 A comparison of letrozole and tamoxifen in postmenopausal women with early breast cancer. N Engl J Med 353:2747–2757

    Google Scholar 

  183. 183. Coombes RC, Hall E, Gibson LJ, Paridaens R, Jassem J, Delozier T, Jones SE, Alvarez I, Bertelli G, Ortmann O, Coates AS, Bajetta E, Dodwell D, Coleman RE, Fallowfield LJ, Mickiewicz E, Andersen J, Lonning PE, Cocconi G, Stewart A, Stuart N, Snowdon CF, Carpentieri M, Massimini G, Bliss JM 2004 A randomized trial of exemestane after two to three years of tamoxifen therapy in postmenopausal women with primary breast cancer. N Engl J Med 350:1081–1092

    PubMed  CAS  Google Scholar 

  184. EBCTCG 1998 Tamoxifen for early breast cancer: An overview of the randomised trials. Lancet 354:1451–1467

    Google Scholar 

  185. 185. Jordan VC 1976 Effect of tamoxifen (ICI 46,474) on initiation and growth of DMBA- induced rat mammary carcinoma. Eur J Cancer 12:419–424

    PubMed  CAS  Google Scholar 

  186. 186. Cuzick J, Baum M 1985 Tamoxifen and contralateral breast cancer [letter]. Lancet 2:282

    PubMed  CAS  Google Scholar 

  187. 187. Fornander T, Rutqvist L E, Cedermark B, Glas, U, Mattsson A, Silfversward C, Skoog L, Somell, A, Theve T, Wilking, N, and Hjalmar M-L. 1989 Adjuvant tamoxifen in early breast cancer: Occurrence of new primary cancers. Lancet 1:117–120

    PubMed  CAS  Google Scholar 

  188. 188. Fisher B, Costantino J, Redmond C, Poisson R, Bowman D, Couture J, Dimitrov NV, Wolmark N, Wickerham DL, Fisher ER, et al. 1989 A randomized clinical trial evaluating tamoxifen in the treatment of patients with node-negative breast cancer who have estrogen-receptor- positive tumors. N Engl J Med 320:479–484.

    PubMed  CAS  Google Scholar 

  189. 189. Fisher B, Costantino, JP, Wickerham, DL, Redmond, CK, Kavanah M, Cronin WM, Vogel V, Robidoux A, Dimitrov, N Atkins J, Daly M, Wieand S, Tan-Chiu E, Ford L, and 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 90:1371–1388

    PubMed  CAS  Google Scholar 

  190. 190. Fisher B, Costantino JP, Wickerham DL, Cecchini RS, Cronin WM, Robidoux A, Bevers, TB, Kavanah MT, Atkins JN, Margolese RG, Runowicz CD, James, JM, Ford LG, and Wolmark N. 2005 Tamoxifen for the prevention of breast cancer: current status of the National Surgical Adjuvant Breast and Bowel Project P-1 study. J Natl Cancer Inst 97:1652–1662

    PubMed  CAS  Google Scholar 

  191. 191. Jordan VC, Phelps E, and Lindgren JU, 1987 Effects of anti-estrogens on bone in castrated and intact female rats. Breast Cancer Res Treat 10:31–35

    PubMed  CAS  Google Scholar 

  192. 192. Love RR, Mazess RB, Barden HS, Epstein S, Newcomb PA, Jordan VC, Carbone PP, and DeMets DL, 1992 Effects of tamoxifen on bone mineral density in postmenopausal women with breast cancer. N Engl J Med 326:852–856

    PubMed  CAS  Google Scholar 

  193. 193. Jordan VC 1988 Chemosuppression of breast cancer with tamoxifen: Laboratory evidence and future clinical investigations. Cancer Invest 6:589–595

    PubMed  CAS  Google Scholar 

  194. 194. Lerner L, Jordan VC. 1990 The development of antiestrogens for the treatment of breast cancer: Eighth Cain Memorial Award Lecture. Cancer Res 50:4177–4189

    PubMed  CAS  Google Scholar 

  195. 195. Buzdar A, Marcus C, Holmes F, Hug V, Hortobagyi G 1988 Phase II evaluation of Ly156758 in metastatic breast cancer. Oncology 45:344–345

    PubMed  CAS  Google Scholar 

  196. 196. Ettinger B, Black DM, Mitlak BH, Knickerbocker RK Nickelsen T, Genant HK, Christiansen C, Delmas, PD, Zanchetta JR, Stakkestad J, Gluer CC, Krueger K., Cohen, FJ, Eckert S, Ensrud KE, Avioli LV, Lips P, and Cummings SR. 1999 Reduction of vertebral fracture risk in postmenopausal women with osteoporosis treated with raloxifene: Results from a 3-year randomized clinical trial Multiple Outcomes of Raloxifene Evaluation (MORE) Investigators [see comments] JAMA 282:637–645

    PubMed  CAS  Google Scholar 

  197. 197. 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, and 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: 2189–2197

    PubMed  CAS  Google Scholar 

  198. 198. Martino S, Cauley JA, Barrett-Connor E, Powles TJ, Mershon J, Disch D, Secrest RJ, Cummings SR 2004 For the CORE Investigators Continuing Outcomes Relevant to Evista: Breast Cancer Incidence in Postmenopausal Osteoporotic Women in a Randomized Trial of Raloxifene. J Natl Cancer Inst 96:1751–1761

    PubMed  CAS  Google Scholar 

  199. 199. Glass CK, Rosenfeld MG 2000 The coregulator exchange in transcriptional functions of nuclear receptors. Genes Dev 14:121–141

    PubMed  CAS  Google Scholar 

  200. 200. Aranda A, Pascual A 2001 Nuclear hormone receptors and gene expression. Physiol Rev 81:1269–1304

    PubMed  CAS  Google Scholar 

  201. 201. Mak HY, Hoare S, Henttu PM, Parker MG 1999 Molecular determinants of the estrogen receptor-coactivator interface. Mol Cell Biol 19:3895–3903

    PubMed  CAS  Google Scholar 

  202. 202. Lavinsky RM, Jepsen K, Heinzel T, Torchia J, Mullen TM, Schiff R, Del-Rio AL, Ricote M, Ngo S, Gemsch J, Hilsenbeck SG, Osborne CK, Glass CK, Rosenfeld MG, Rose DW 1998 Diverse signaling pathways modulate nuclear receptor recruitment of N-CoR and SMRT complexes. Proc Natl Acad Sci USA 95:2920–2925

    PubMed  CAS  Google Scholar 

  203. 203. Jepsen K, Hermanson O, Onami TM, Gleiberman AS, Lunyak V, McEvilly RJ, Kurokawa R, Kumar V, Liu F, Seto E, Hedrick SM, Mandel G, Glass CK, Rose DW, Rosenfeld MG 2000 Combinatorial roles of the nuclear receptor corepressor in transcription and development. Cell 102:753–763

    PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 2008 Humana Press Inc.

About this chapter

Cite this chapter

Peng, J., Jordan, V.C. (2008). Estrogen Receptor Pathways and Breast Cancer. In: Bronchud, M.H., Foote, M.A., Giaccone, G., Olopade, O., Workman, P. (eds) Principles of Molecular Oncology. Humana Press. https://doi.org/10.1007/978-1-59745-470-4_9

Download citation

  • DOI: https://doi.org/10.1007/978-1-59745-470-4_9

  • Publisher Name: Humana Press

  • Print ISBN: 978-1-934115-25-1

  • Online ISBN: 978-1-59745-470-4

  • eBook Packages: MedicineMedicine (R0)

Publish with us

Policies and ethics