Abstract
Beginning in the late 1950s into the 1970s the laboratories of El-wood Jensen and Jack Gorski proposed a model by which the inter-action of the receptor and 17ß-estradiol (E2) are involved in transducing the cellular effects of this hormone (Jensen and DeSombre 1973; Toft and Gorski 1966). Their laboratories also performed the isolation and initial characterization of the estrogen receptor (ER; Jensen and DeSombre 1973; Toft and Gorski 1966). Since its initial discovery, significant progress has been made in understanding the mechanisms and manifestations of ER action; however, many new questions have emerged that make this area of research as exciting and interesting as it was 40 years ago.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
Similar content being viewed by others
References
Aronica SM, Kraus WL, Katzenellenbogen BS (1994) Estrogen action via the cAMP signaling pathway: stimulation of adenylate cyclase and cAMP-regulated gene transcription. Proc Natl Acad Sci 91:8517–8521
Bhat RA, Harnish DC, Stevis PE, Lyttle CR, Komm BS (1998) A novel human estrogen receptor beta: identification and functional analysis of additional N-terminal amino acids. J Steroid Biochem Mol Biol 67:233–240
Bourguet W, Ruff M, Chambon P, Gronemeyer H, Moras D (1995) Crystal structure of the ligand-binding domain of the human nuclear receptor RXR-alpha. Nature 375:377–382
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
Cancer CGoHFiB (1997) Breast cancer and hormone replacement therapy: collaborative reanalysis of data from 51 epidemiological studies of 52,705 women with breast cancer and 108,411 women without breast cancer. Lancet 350:1047–1059
Chang L, Karin M (2001) Mammalian MAP kinase signaling cascades. (England — Nature J), pp 37–40
Chen Z, Yuhanna IS, Galcheva-Gargova Z, Karas RH, Mendelsohn ME, Shaul PW (1999) Estrogen receptor alpha mediates the nongenomic activation of endothelial nitric oxide synthase by estrogen. J Clin Invest 103:401–406
Committee NRN (1999) A unified nomenclature of system for the nuclear receptor superfamily. Cell 97:1–3
Couse JF, Korach KS (1999) Estrogen receptor null mice: what have we learned and where will they lead us? [published erratum appears in Endocr Rev 1999 Aug;20(4):459]. Endocr Rev 20:358–417
Danielian PS, White R, Lees JA, Parker MG (1992) Identification of a conserved region required for hormone dependent transcriptional activation by steroid hormone receptors. EMBO J 11:1025–1033
DiDomenico M, Castoria G, Bilancio A, Migliaccio A, Auricchio F (1996) Estradiol activation of human colon carcinoma-derived Caco-2 cell growth. Cancer Res 56:4516–4521
Downward J (1997 a) Cell cycle: routine role for Ras. Curr Biol 7:R258–260
Downward J (1997 b) Role of phosphoinositide-3-OH kinase in Ras signaling. Adv Second Messenger Phosphoprotein Res 31:1–10
Endoh H, Sasaki H, Maruyama K, Takeyama K, Waga I, Shimizu T, Kato S, Kawashima H (1997) Rapid activation of MAP kinase by estrogen in the bone cell line. Biochem Biophys Res Commun 235:99–102
Evans RM (1988) The steroid and thyroid hormone receptor superfamily. Science 240:889–895
Feng W, Webb P, Nguyen P, Liu X, Li J, Karin M, Kushner PJ (2001) Potentiation of estrogen receptor activation function 1 (AF-1) by Src/JNK through a serine 118-independent pathway. Mol Endocrinol 15:32–45
Glass CK, Rose DW, Rosenfeld MG (1997) Nuclear receptor coactivators. Curr Opin Cell Biol 9:222–232
Heery DM, Kalkhoven E, Hoare S, Parker MG (1997) A signature motif in transcriptional co-activators mediates binding to nuclear receptors [see comments]. Nature 387:733–736
Henderson VW (1997) The epidemiology of estrogen replacement therapy and Alzheimer’s disease. Neurology 48: S27–S35
Hollenberg SM, Weinberger C, Ong ES, Cerelli G, Oro A, Lebo R, Thompson EB, Rosenfeld MG, Evans RM (1982) Primary structure and expression of a functional human glucocorticoid receptor cDNA. Nature 318: 635–641
Hubbard SR, Mohammadi M, Schlessinger J (1998) Autoregulatory mechanisms in protein-tyrosine kinases. J Biol Chem 273:11987–11990
Hulley S, Grady D, Bush T, Furberg C, Herrington D, Riggs B, Vittinghoff E (1998) Randomized trial of estrogen plus progestin for secondary prevention of coronary heart disease in postmenopausal women. JAMA 280:605–613
Ing NH, Beekman JM, Tsai SY, Tsai MJ, BW OM (1992) Members of the steroid hormone receptor superfamily interact with TFIIB. J Biol Chem 267:17617–17623
Investigators WGftWsHI (2002) Risks and benefits of estrogen plus progestin in healthy postmenopausal women: principal results from the Women’s Health Initiative randomized controlled trial. JAMA 288:321–333
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
Jensen EV, DeSombre ER (1973) Estrogen-receptor interaction. Science 182:126–134
Johnston SR, Lu B, Scott GK, Kushner PJ, Smith IE, Dowsett M, Benz CC (1999) Increased activator protein-1 DNA binding and c-Jun NH2-terminal kinase activity in human breast tumors with acquired tamoxifen resistance. Clin Cancer Res 5:251–256
Joung I, Strominger JL, Shin J (1996) Molecular cloning of a phosphotyrosine-independent ligand of the p561ck SH2 domain. Proc Natl Acad Sci 93:5991–5995
Kato S, Endoh H, Masuhiro Y, Kitamoto T, Uchiyama S, Sasaki H, Masushige S, Gotoh Y, Nishida E, Kawashima H, et al. (1995 a) Activation of the estrogen receptor through phosphorylation by mitogen-activated protein kinase. Science 270:1491–1494
Kato S, Masuhiro Y, Watanabe M, Kobayashi Y, Takeyama KI, Endoh H, Yanagisawa J (2000) Molecular mechanism of a cross-talk between estrogen and growth factor signaling pathways. Genes Cells 5:593–601
Kato S, Sasaki H, Suzawa M, Masushige S, Tora L, Chambon P, Gronemeyer H (1995 b) Widely spaced, directly repeated PuGGTCA elements act as promiscuous enhancers for different classes of nuclear receptors. Mol Cell Biol 15:5858–5867
Kay BK, Williamson MP, Sudol M (2000) The importance of being proline: the interaction of proline-rich motifs in signaling proteins with their cognate domains. FASEB J 14:231–241
King WJ, Greene GL (1984) Monoclonal antibodies localize estrogen receptor in the nuclei of target cells. Nature 307:745–747
Krege JH, Hodgin JB, Couse JF, Enmark E, Warner M, Mahler JF, Sar M, Korach KS, Gustafsson JA, Smithies O (1998) Generation and reproductive phenotypes of mice lacking estrogen receptor beta. Proc Natl Acad Sci 95:15677–15682
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 93:5925–5930
Kumar V, Chambon P (1988) The estrogen receptor binds tightly to its responsive element as a ligand-induced homodimer. Cell 55:145–156
Kumar V, Green S, Stack G, Berry M, Jin JR, Chambon P (1987) Functional domains of the human estrogen receptor. Cell 51:941–951
Le Mellay V, Grosse B, Lieberherr M (1997) Phospholipase C beta and membrane action of calcitriol and estradiol. J Biol Chem 272:11902 –11907
Lees JA, Fawell SE, Parker MG (1989) Identification of two transactivation domains in the mouse estrogen receptor. Nucleic Acids Res 17:5477–5488
Levin AA (2002) Cellular functions of plasma membrane estrogen receptors. Steroids 67:471–475
Lubahn DB, Moyer JS, Golding TS, Couse JF, Korach KS, Smithies O (1993) Alteration of reproductive function but not prenatal sexual development after insertional disruption of the mouse estrogen receptor gene. Proc Natl Acad Sci 90:11162–11166
Luisi BF, Xu WX, Otwinowski Z, Freedman LP, Yamamoto KR, Sigler PB (1991) Crystallographic analysis of the interaction of the glucocorticoid receptor with DNA [see comments]. Nature 352:497–505
Mangelsdorf DJ, Thummel C, Beato M, Herrlich P, Schutz G, Umesono K, Blumberg B, Kastner P, Mark M, Chambon P, et al. (1995) The nuclear receptor superfamily: the second decade. Cell 83:835–839
Matsuda M, Mayer BJ, Fukui Y, Hanafusa H (1990) Binding of transforming protein, P47gag-crk, to a broad range of phosphotyrosine-containing proteins. Science 248:1537–1539
McKenna NJ, Lanz RB, O’Malley BW (1999) Nuclear receptor coregulators: cellular and molecular biology. Endocr Rev 20:321–344
Metzger D, White JH, Chambon P (1988) The human estrogen receptor functions in yeast. Nature 334:31–36
Meyer ME, Gronemeyer H, Turcotte B, Bocquel MT, Tasset D, Chambon P (1989) Steroid hormone receptors compete for factors that mediate their enhancer function. Cell 57:433–442
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
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
Migliaccio A, Pagano M, Auricchio F (1993) Immediate and transient stimulation of protein tyrosine phosphorylation by estradiol in MCF-7 cells. Oncogene 8:2183–2191
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
Moras DaG H (1998) The nuclear receptor ligand-binding domain: structure and function. Curr Opin Cell Biol 10:384–391
Mosselman S, Polman J, Dijkema R (1996) ER beta: identification and characterization of a novel human estrogen receptor. FEBS Letters 392:49–53
Nasr A, Breckwoldt M (1998) Estrogen replacement therapy and cardiovascular protection: lipid mechanisms are the tip of an iceberg. Gynecol Endocrinology 12:43–59
Ogawa S, Inoue S, Watanabe T, Orimo A, Hosoi T, Ouchi Y, Muramatsu M (1998) Molecular cloning and characterization of human estrogen receptor betacx: a potential inhibitor of estrogen action in human. Nucleic Acids Res 26:3505–3512
Oursler MJ (1998) Estrogen regulation of gene expression in osteoblasts and osteoclasts. Crit Rev Eukaryot Gene Expr 8:125–140
Pietras RJ, Szego CM (1977) Specific binding sites for estrogen at the outer surfaces of isolated endometrial cells. Nature 265:69–72
Pietras RJ, Szego CM (1980) Partial purification and characterization of estrogen receptors in subfractions of hepatocyte plasma membranes. Biochem J 191:743–760
Rastinejad F, Perlmann T, Evans RM, Sigler PB (1995) Structural determinants of nuclear receptor assembly on DNA direct repeats [see comments]. Nature 375:203–211
Renaud JP, Rochel N, Ruff M, Vivat V, Chambon P, Gronermeyer H, Moras D (1995) Crystal structure of the RAR-gamma ligand-binding domain bound to all-trans retinoic acid. Nature 378:681–689
Riggs BL, Khosla S, Melton LJ, III (2002) Sex steroids and the construction and conservation of the adult skeleton. Endocr Rev 23:279–302
Sadovsky Y, Webb P, Lopez G, Baxter JD, Fitzpatrick PM, Gizang-Ginsberg E, Cavailles V, Parker MG, Kushner PJ (1995) Transcriptional activators differ in their responses to overexpression of TATA-box-binding protein. Mol Cell Biol 15:1554–1563
Schule R, Urmesono K, Mangelsdorf DJ, Bolado J, Pike JW, Evans RM (1990) Jun-Fos and receptors for vitamins A and D recognize a common response element in the human osteocalcin gene. Cell 61:497–504
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
Sheppard KA, Rose DW, Haque ZK, Kurokawa R, McInerney E, Westin S, Thanos D, Rosenfeld MG, Glass CK, Collins T (1999) Transcriptional activation by NF-kappaB requires multiple coactivators. Mol Cell Biol 19:6367–6378
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 95:927–937
Shibata H, Spencer TE, Onate SA, Jenster G, Tsai SY, Tsai MJ, O’Malley BW (1997) Role of coactivators and corepressors in the mechanism of steroid/thyroid receptor action. Recent Prog Horm Res 52:141–164
Simoncini T, Hafezl-Moghadam A, Brazil DP, Ley K, Chin WW, Liao JK (2000) Interaction of estrogen receptor with the regulatory subunit of phosphatidylinositol-3-OH kinase. Nature 407:538–541
Singer CA, Figueroa-Masot XA, Batchelor RH, Dorsa DM (1999) The mitogenactivated protein kinase pathway mediates estrogen neuroprotection after glutamate toxicity in primary cortical neurons. J Neurosci 19:2455–2463
Stumpf W, Sar M (1976) Autoradiographic localization of estrogen, androgen, progestin, and glucocorticoid in “target tissues” and “non-target” tissues. In: Pasqualini JR (ed) Receptors and mechanism of action of steroid hormones. Marcel Dekker, New York, pp 41–84
Tesarik J, Mendoza C (1995) Nongenomic effects of 17-estradiol on maturing human oocytes: Relationship to oocyte developmental potential. J Clin Endocrinol Metab 80:1438–1443
Toft D, Gorski J (1966) A receptor molecule for estrogens: isolation from the rat uterus and preliminary characterization. Proc Natl Acad Sci 55:1574–1581
Treisman R (1996) Regulation of transcription by MAP kinase cascades. Curr Opin Cell Biol 8:205–215
Tremblay GB, Tremblay A, Copeland NG, Gilbert DJ, Jenkins NA, Labrie F, Giguere V (1997) Cloning, chromosomal localization, and functional analysis of the murine estrogen receptor beta. Mol Endocrinol 11:353–365
Tsai MJ, O’Malley BW (1994) Molecular mechanisms of action of steroid/ thyroid receptor superfamily members. Annu Rev Biochem 63:451–486
Vadlamudi RK, Wang R-A, Mazumdar A, Kim Y S, 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
Wagner RL, Apriletti JW, McGrath ME, West BL, Baxter JD, Fletterick RJ (1995) A structural role for hormone in the thyroid hormone receptor. Nature 378:690–697
Walter P, Green S, Greene G, Krust A, Bornert JM, Jeltsch JM, Staub A, Jensen E, Scrace G, Waterfield M, et al. (1985) Cloning of the human estrogen receptor cDNA. Proc Natl Acad Sci 82:7889–7893
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
Welshons WV, Lieberman ME, Gorski, J (1984) Nuclear localization of unoccupied estrogen receptor. Nature 307:747–749
Wong C-W, McNally C, Nickbarg E, Komm BS, Cheskis BJ (2002) Estrogen receptor-interacting protein that modulates its nongenomic activitycrosstalk with Src/Erk phosphorylation cascade. Proc Natl Acad Sci 192:569–699
Zhao Q, Chasse SA, Devarakonda S, Sierk ML, Ahvazi B, Rastinejad F (2000) Structural basis of RXR-DNA interactions. J Mol Biol 296:509–520
Zumoff B (1998) Does postmenopausal estrogen administration increase the risk of breast cancer? Contributions of animal, biochemical, and clinical investigative studies to a resolution of the controversy. Proc Soc Exp Biol Med 217:30–37
Editor information
Rights and permissions
Copyright information
© 2004 Springer-Verlag Berlin Heidelberg
About this paper
Cite this paper
Lyttle, C.R., Komm, B.S., Cheskis, B.J. (2004). Estrogens: From Classical Endocrine Action to Tissue Selective Action. In: Korach, K.S., Hillisch, A., Fritzemeier, K.H. (eds) New Molecular Mechanisms of Estrogen Action and Their Impact on Future Perspectives in Estrogen Therapy. Ernst Schering Research Foundation Workshop, vol 46. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-662-05386-7_1
Download citation
DOI: https://doi.org/10.1007/978-3-662-05386-7_1
Publisher Name: Springer, Berlin, Heidelberg
Print ISBN: 978-3-662-05388-1
Online ISBN: 978-3-662-05386-7
eBook Packages: Springer Book Archive