Nonnuclear actions of estrogen

Arteriosclerosis, Thrombosis, and Vascular Biology

Volumn 22, Issue 12, 2002, Pages 1952-1961

  Ho, Karen J ^a   Liao, James K ^a  

^a BRIGHAM AND WOMEN S HOSPITAL   (United States)

Author keywords

Estrogen; Estrogen receptors; Signaling; Transcription; Vasculature

Indexed keywords

2 (2 AMINO 3 METHOXYPHENYL)CHROMONE; 4 (1,2 DIPHENYL 1 BUTENYL)CINNAMIC ACID; 4 [4 METHYL 2 [4 [2 (1 PIPERIDINYL)ETHOXY]PHENYL] 7 PIVALOYLOXY 2H 1 BENZOPYRAN 3 YLPHENYL] PIVALATE; 6 HYDROXY 2 (4 HYDROXYPHENYL) 3 [4 [2 (1 PYRROLIDINYL)ETHOXY]BENZOYL]BENZO[B]THIOPHENE; ESTRADIOL; ESTROGEN; ESTROGEN RECEPTOR; LIGAND; RALOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATOR; TAMOXIFEN; TRANSCRIPTION FACTOR;

BLOOD VESSEL INJURY; CARDIOVASCULAR DISEASE; CARDIOVASCULAR EFFECT; DRUG EFFECT; DRUG RECEPTOR BINDING; ESTROGEN ACTIVITY; FEMALE; HEART INFARCTION; HEART MUSCLE INJURY; HEART PROTECTION; HEART VENTRICLE HYPERTROPHY; HUMAN; MALE; NONHUMAN; PRIMARY PREVENTION; PRIORITY JOURNAL; RECEPTOR INTRINSIC ACTIVITY; SECONDARY PREVENTION; SHORT SURVEY; SIGNAL TRANSDUCTION; TRANSCRIPTION REGULATION; VASODILATATION;

ANIMALS; CARDIOVASCULAR PHYSIOLOGY; CELL NUCLEUS; CYTOPLASM; ESTROGENS; HUMANS; RECEPTORS, ESTROGEN; SECOND MESSENGER SYSTEMS; SIGNAL TRANSDUCTION;

EID: 0036929353     PISSN: 10795642     EISSN: None     Source Type: Journal    
DOI: 10.1161/01.ATV.0000041200.85946.4A     Document Type: Short Survey

References (153)

1. Mendelsohn ME, Karas RH. The protective effects of estrogen on the cardiovascular system. N Engl J Med. 1999;340:1801-1811.
2. Babiker FA, De Windt LJ, van Eickels M, Grohe C, Meyer R, Doevendans PA. Estrogenic hormone action in the heart: Regulatory network and function. Cardiovasc Res. 2002;53:709-719.
3. Stevenson JC. Cardiovascular effects of oestrogens. J Steroid Biochem Mol Biol. 2000;74:387-393.
4. White RE, Darkow DJ, Lang JL. Estrogen relaxes coronary arteries by opening BKCa channels through a cGMP-dependent mechanism. Circ Res. 1995;77:936-942.
5. Bourassa PA, Milos PM, Gaynor BJ, Breslow JL. Aiello RJ. Estrogen reduces atherosclerotic lesion development in apolipoprotein E-deficient mice. Proc Natl Acad Sci USA. 1996;93:10022-10027.
6. Akishita M, Ouchi Y, Miyoshi H, Kozaki K, Inoue S, Ishikawa M, Eto M, Toba K, Orimo H. Estrogen inhibits cuff-induced intimal thickening of rat femoral artery: Effects on migration and proliferation of vascular smooth muscle cells. Atherosclerosis. 1997;130:1-10.
7. White CR, Shelton J, Chen SJ, Darley-Usmar V, Allen L, Nabors C, Sanders PW, Chen YF, Oparil S. Estrogen restores endothelial cell function in an experimental model of vascular injury. Circulation. 1997;96:1624-1630.
8. Chen SJ. Li H, Durand J, Oparil S, Chen YF. Estrogen reduces myointimal proliferation after balloon injury of rat carotid artery. Circulation. 1996;93:577-584.
9. Sullivan TR Jr, Karas RH, Aronovitz M, Faller GT, Ziar JP. Smith JJ, O'Donnell TF Jr, Mendelsohn ME. Estrogen inhibits the response-to-injury in a mouse carotid artery model. J Clin Invest. 1995;96:2482-2488.
10. Oparil S, Levine RL, Chen SJ, Durand J, Chen YF. Sexually dimorphic response of the balloon-injured rat carotid artery to hormone treatment. Circulation. 1997;95:1301-1307.
11. McHugh NA, Cook SM, Schairer JL, Bidgoli MM, Merrill GF. Ischemia- and reperfusion-induced ventricular arrhythmias in dogs: Effects of estrogen. Am J Physiol. 1995;268:H2569-H2573.
12. Node K, Kitakaze M, Kosaka H, Minamino T, Funaya H, Hori M. Amelioration of ischemia- and reperfusion-induced myocardial injury by 17β-estradiol: Role of nitric oxide and calcium-activated potassium channels. Circulation. 1997;96:1953-1963.
13. Farhat MY, Chen MF, Bhatti T, Iqbal A, Cathapermal S, Ramwell PW. Protection by oestradiol against the development of cardiovascular changes associated with monocrotaline pulmonary hypertension in rats. Br J Pharmacol. 1993;110:719-723.
14. Douglas PS, Katz SE, Weinberg EO, Chen MH, Bishop SP, Lorell BH . Hypertrophic remodeling: Gender differences in the early response to left ventricular pressure overload. J Am Coll Cardiol. 1998;32:1118-1125.
15. Mangelsdorf DJ, Thummel C, Beato M, Herrlich P, Schutz G, Umesono K, Blumberg B, Kastner P. Mark M. Chambon P. et al. The nuclear receptor superfamily: The second decade. Cell. 1995;83:835-839.
16. Beato M, Herrlich P. Schutz G. Steroid hormone receptors: Many actors in search of a plot. Cell. 1995;83:851-857.
17. Hall JM, Couse JF, Korach KS. The multifaceted mechanisms of estradiol and estrogen receptor signaling. J Biol Chem. 2001;276:36869-36872.
18. Rosenfeld MG, Glass CK. Coregulator codes of transcriptional regulation by nuclear receptors. J Biol Chem. 2001;276:36865-36868.
19. McDonnell DP, Norris JD. Connections and regulation of the human estrogen receptor. Science. 2002;296:1642-1644.
20. Couse JF, Korach KS. Estrogen receptor null mice: What have we learned and where will they lead us? Endocr Rev. 1999;20:358-417.
21. Sudhir K, Chou TM, Chatterjee K, Smith EP, Williams TC, Kane JP, Malloy MJ, Korach KS, Rubanyi GM, Premature coronary artery disease associated with a disruptive mutation in the estrogen receptor gene in a man. Circulation. 1997;96:3774-3777.
22. Sudhir K, Chou TM, Messina LM, Hutchison SJ, Korach KS, Chatterjee K, Rubanyi GM. Endothelial dysfunction in a man with disruptive mutation in oestrogen-receptor gene. Lancet. 1997;349:1146-1147.
23. Iafrati MD, Karas RH, Aronovitz M, Kim S, Sullivan TR Jr, Lubahn DB, O'Donnell TF Jr, Korach KS, Mendelsohn ME. Estrogen inhibits the vascular injury response in estrogen receptor α-deficient mice. Nat Med. 1997;3:545-548.
24. Karas RH, Schulten H, Pare G, Aronovitz MJ, Ohlsson C, Gustafsson JA, Mendelsohn ME. Effects of estrogen on the vascular injury response in estrogen receptor α, α (double) knockout mice. Circ Res. 2001:89:534-539.
25. Pendaries C, Darblade B, Rochaix P, Krust A, Chambon P. Korach KS, Bayard F, Amal JF. The AF-1 activation-function of ERα may be dispensable to mediate the effect of estradiol on endothelial NO production in mice. Proc Natl Acad Sci U S A . 2002;99:2205-2210.
26. Dupont S, Krust A, Gansmuller A, Dierich A, Chambon P, Mark M. Effect of single and compound knockouts of estrogen receptors α (ERα) and (ERβ) on mouse reproductive phenotypes. Development. 2000;127:4277-4291.
27. Pare G, Krust A, Karas RH, Dupont S. Aronovitz M, Chambon P, Mendelsohn ME. Estrogen receptor-α mediates the protective effects of estrogen against vascular injury. Circ Res. 2002;90:1087-1092.
28. Zhai P, Eurell TE, Cooke PS, Lubahn DB, Gross DR. Myocardial ischemia-reperfusion injury in estrogen receptor-α knockout and wild-type mice. Am J Physiol. 2000;278: H1640-H1647.
29. Dubal DB, Zhu H, Yu J, Rau SW, Shughrue PJ, Merchenthaler I, Kindy MS, Wise PM. Estrogen receptor α, not β, is a critical link in estradiol-mediated protection against brain injury. Proc Natl Acad Sci USA. 2001;98:1952-1957.
30. Pettersson K, Gustafsson JA. Role of estrogen receptor β in estrogen action. Annu Rev Physiol. 2001;63:165-192.
31. Lindner V, Kim SK, Karas RH, Kuiper GG, Gustafsson JA, Mendelsohn ME. Increased expression of estrogen receptor-β mRNA in male blood vessels after vascular injury. Circ Res. 1998;83:224-229.
32. Zhu Y, Bian Z, Lu P, Karas RH, Bao L, Cox D, Hodgin J, Shaul PW, Thoren P, Smithies O, Gustafsson JA, Mendelsohn ME. Abnormal vascular function and hypertension in mice deficient in estrogen receptor β. Science. 2002;295:505-508.
33. Collins P, Webb C. Estrogen hits the surface. Nat Med. 1999;5:1130-1131.
34. Kelly MJ, Levin ER. Rapid actions of plasma membrane estrogen receptors. Trends Endocrinol Metab. 2001;12:152-156.
35. Pietras RJ, Nemere I, Szego CM. Steroid hormone receptors in target cell membranes. Endocrine. 2001;14:417-427.
36. Luconi M, Forti G, Baldi E. Genomic and nongenomic effects of estrogens: Molecular mechanisms of action and clinical implications for male reproduction. J Steroid Biochem Mol Biol. 2002;80:369-381.
37. Levin ER. Cell localization, physiology, and nongenomic actions of estrogen receptors. J Appl Physiol. 2001;91:1860-1867.
38. Falkenstein E, Tillmann HC, Christ M, Feuring M, Wehling M. Multiple actions of steroid hormones: A focus on rapid, nongenomic effects. Pharmacol Rev. 2000;52:513-556.
39. Falkenstein E, Norman AW, Wehling M. Mannheim classification of nongenomically initiated (rapid) steroid action(s). J Clin Endocrinol Metab. 2000;85:2072-2075.
40. Falkenstein E, Wehling M. Nongenomically initiated steroid actions. Eur J Clin Invest. 2000;30(suppl 3):51-54.
41. Levin ER. Cellular functions of plasma membrane estrogen receptors. Steroids. 2002;67:471-475.
42. Moggs JG, Orphanides G. Estrogen receptors: Orchestrators of pleiotropic cellular responses. EMBO Rep. 2001;2:775-781.
43. Pietras RJ, Szego CM. Specific binding sites for oestrogen at the outer surfaces of isolated endometrial cells. Nature. 1977;265:69-72.
44. Pappas TC, Gametchu B, Watson CS. Membrane estrogen receptors identified by multiple antibody labeling and impeded-ligand binding. FASEB J. 1995;9:404-410.
45. Norfleet AM, Thomas ML, Gametchu B, Watson CS. Estrogen receptor-α detected on the plasma membrane of aldehyde-fixed GH3/B6/F10 rat pituitary tumor cells by enzyme-linked immunocytochemistry. Endocrinology. 1999;140:3805-3814.
46. Norfleet AM, Clarke CH, Gametchu B, Watson CS. Antibodies to the estrogen receptor-α modulate rapid prolactin release from rat pituitary tumor cells through plasma membrane estrogen receptors. FASEB J. 2000;14:157-165.
47. Watson CS, Norfleet AM, Pappas TC, Gametchu B. Rapid actions of estrogens in GH3/B6 pituitary tumor cells via a plasma membrane version of estrogen receptor-α. Steroids. 1999;64:5-13.
48. Watson CS, Campbell CH, Gametchu B. The dynamic and elusive membrane estrogen receptor-α. Steroids. 2002;67:429-437.
49. Ropero AB, Sofia B, Nadal A. A nonclassical estrogen membrane receptor triggers rapid differential actions in the endocrine pancreas. Mol Endocrinol. 2002;16:497-505.
50. Razandi M, Pedram A, Greene GL, Levin ER. Cell membrane and nuclear estrogen receptors (ERs) originate from a single transcript: Studies of ERα and ERβ expressed in Chinese hamster ovary cells. Mol Endocrinol. 1999;13:307-319.
51. Kuroki Y, Fukushima K, Kanda Y, Mizuno K, Watanabe Y. Putative membrane-bound estrogen receptors possibly stimulate mitogen-activated protein kinase in the rat hippocampus. Eur J Pharmacol. 2000;400:205-209.
52. Watters JJ, Campbell JS, Cunningham MJ, Krebs EG, Dorsa DM. Rapid membrane effects of steroids in neuroblastoma cells: Effects of estrogen on mitogen activated protein kinase signalling cascade and c-fos immediate early gene transcription. Endocrinology. 1997;138:4030-4033.
53. Razandi M, Pedram A, Levin ER. Plasma membrane estrogen receptors signal to antiapoptosis in breast cancer. Mol Endocrinol. 2000;14:1434-1447.
54. Berthois Y, Pourreau-Schneider N, Gandilhon P, Mittre H, Tubiana N, Martin PM. Estradiol membrane binding sites on human breast cancer cell lines: Use of a fluorescent estradiol conjugate to demonstrate plasma membrane binding systems. J Steroid Biochem. 1986;25:963-972.
55. Morey AK, Razandi M, Pedram A, Hu RM, Prins BA, Levin ER. Oestrogen and progesterone inhibit the stimulated production of endothelin-1. Biochem J. 1998;330(pt 3):1097-1105.
56. Razandi M, Pedram A, Levin ER. Estrogen signals to the preservation of endothelial cell form and function. J Biol Chem. 2000;275:38540-38546.
57. Gratton JP, Morales-Ruiz M, Kureishi Y, Fulton D, Walsh K, Sessa WC. Akt down-regulation of p38 signaling provides a novel mechanism of vascular endothelial growth factor-mediated cytoprotection in endothelial cells. J Biol Chem. 2001;276:30359-30365.
58. Honda K, Sawada H, Kihara T, Urushitani M, Nakamizo T, Akaike A, Shimohama S. Phosphatidylinositol 3-kinase mediates neuroprotection by estrogen in cultured cortical neurons. J Neurosci Res. 2000;60:321-327.
59. Hisamoto K, Ohmichi M, Kurachi H, Hayakawa J, Kanda Y, Nishio Y, Adachi K, Tasaka K, Miyoshi E, Fujiwara N, Taniguchi N, Murata Y. Estrogen induces the Akt-dependent activation of endothelial nitric-oxide synthase in vascular endothelial cells. J Biol Chem. 2001;276:3459-3467.
60. Simoncini T, Hafezi-Moghadam A, Brazil DP, Ley K, Chin WW, Liao JK. Interaction of oestrogen receptor with the regulatory subunit of phosphatidylinositol-3-OH kinase. Nature. 2000;407:538-541.
61. Denninger JW, Marietta MA. Guanylate cyclase and the .NO/cGMP signaling pathway. Biochim Biophys Acta., 1999;1411:334-350.
62. Lantin-Hermoso RL, Rosenfeld CR, Yuhanna IS, German Z, Chen Z, Shaul PW. Estrogen acutely stimulates nitric oxide synthase activity in fetal pulmonary artery endothelium. Am J Physiol. 1997;273: L119-L126.
63. Chen Z, Yuhanna IS, Galcheva-Gargova Z, Karas RH, Mendelsohn ME, Shaul PW. Estrogen receptor α mediates the nongenomic activation of endothelial nitric oxide synthase by estrogen. J Clin Invest. 1999;103:401-406.
64. Hafezi-Moghadam A, Simoncini T, Yang E, Limbourg FP, Plumier JC, Rebsamen MC, Hsieh CM, Chui DS, Thomas KL, Prorock AJ, Laubach VE, Moskowitz MA, French BA, Ley K, Liao JK. Acute cardiovascular protective effects of corticosteroids are mediated by non-transcriptional activation of endothelial nitric oxide synthase. Nat Med. 2002;8:473-479.
65. Salom JB, Burguete MC, Perez-Asensio FJ, Centeno JM, Torregrosa G, Alborch E. Acute relaxant effects of 17-β-estradiol through nongenomic mechanisms in rabbit carotid artery. Steroids. 2002;67:339-346.
66. Garcia-Cardena G, Fan R, Shah V, Sorrentino R, Cirino G, Papapetropoulos A, Sessa WC. Dynamic activation of endothelial nitric oxide synthase by Hsp90. Nature. 1998;392:821-824.
67. Russell KS, Haynes MP, Caulin-Glaser T, Rosneck J, Sessa WC, Bender JR. Estrogen stimulates heat shock protein 90 binding to endothelial nitric oxide synthase in human vascular endothelial cells: Effects on calcium sensitivity and NO release. J Biol Chem. 2000;275:5026-5030.
68. Bucci M, Roviezzo F, Cicala C, Pinto A, Cirino G. 17-β-oestradiol induced vasorelaxation in vitro is mediated by eNOS through hsp90 and akt/pkb dependent mechanism. Br J Pharmacol. 2002;135:1695-1700.
69. Fontana J, Fulton D, Chen Y, Fairchild TA, McCabe TJ, Fujita N, Tsuruo T, Sessa WC. Domain mapping studies reveal that the M domain of hsp90 serves as a molecular scaffold to regulate Akt-dependent phosphorylation of endothelial nitric oxide synthase and NO release. Circ Res. 2002;90:866-873.
70. Nuedling S, Kahlert S, Loebbert K, Meyer R, Vetter H, Grohe C. Differential effects of 17β-estradiol on mitogen-activated protein kinase pathways in rat cardiomyocytes. FEBS Lett. 1999;454:271-276.
71. Di Domenico M, Castoria G, Bilancio A, Migliaccio A, Auricchio F. Estradiol activation of human colon carcinoma-derived Caco-2 cell growth. Cancer Res. 1996;56:4516-4521.
72. Castoria G, Barone MV, Di Domenico M, Bilancio A, Ametrano D, Migliaccio A, Auricchio. F. Non-transcriptional action of oestradiol and progestin triggers DNA synthesis. EMBO J. 1999;18:2500-2510.
73. Endoh H, Sasaki H, Maruyama K, Takeyama K, Waga I, Shimizu T, Kato S, Kawashima H. Rapid activation of MAP kinase by estrogen in the bone cell line. Biochem Biophys Res Commun. 1997;235:99-102.
74. Jessop HL, Sjoberg M, Cheng MZ, Zaman G, Wheeler-Jones CP, Lanyon LE. Mechanical strain and estrogen activate estrogen receptor α in bone cells, J Bone Miner Res. 2001;16:1045-1055.
75. Hwang KC, Lee KH, Jang Y. Inhibition of MEK1,2/ERK mitogenic pathway by estrogen with antiproliferative properties in rat aortic smooth muscle cells. J Steroid Biochem Mol Biol. 2002;80:85-90.
76. Flores-Delgado G, Bringas P, Buckley S, Anderson KD, Warburton D. Nongenomic estrogen action in human lung myofibroblasts, Biochem Biophys Res Commun. 2001;283:661-667.
77. Watters JJ, Chun TY, Kim YN, Bertics PJ, Gorski J, Estrogen modulation of prolactin gene expression requires an intact mitogen-activated protein kinase signal transduction pathway in cultured rat pituitary cells. Mol Endocrinol. 2000;14:1872-1881.
78. de Jager T, Pelzer T, Muller-Botz S, Imam A, Muck J, Neyses L. Mechanisms of estrogen receptor action in the myocardium: Rapid gene activation via the ERK1/2 pathway and serum response elements. J Biol Chem. 2001;276:27873-27880
79. Kahlert S, Nuedling S, van Eickels M, Vetter H, Meyer R, Grohe C. Estrogen receptor α rapidly activates the IGF-1 receptor pathway. J Biol Chem. 2000;275:18447-18453
80. Song RX, McPherson RA, Adam L, Bao Y, Shupnik M, Kumar R, Santen RJ. Linkage of rapid estrogen action to MAPK activation by ERα-Shc association and Shc pathway activation. Mol Endocrinol 2002;16:116-127.
81. Migliaccio A, Di Domenico M, Castoria G, de Falco A, Bontempo P, Nola E, Auricchio F. Tyrosine kinase/p21ras/MAP-kinase pathway activation by estradiol-receptor complex in MCF-7 cells. EMBO J. 1996;15:1292-1300.
82. Migliaccio A, Castoria G, Di Domenico M, de Falco A, Bilancio A, Lombardi M, Barone MV, Ametrano D, Zannini MS, Abbondanza C, Auricchio F. Steroid-induced androgen receptor-oestradiol receptor β-Src complex triggers prostate cancer cell proliferation. EMBO J. 2000;19:5406-5417.
83. Singer CA, Figueroa-Masot XA, Batchelor RH, Dorsa DM. The mitogen-activated protein kinase pathway mediates estrogen neuroprotection after glutamate toxicity in primary cortical neurons. J Neurosci. 1999;19:2455-2463.
84. Brubaker KD, Gay CV. Estrogen stimulates protein tyrosine phosphorylation and Src kinase activity in avian osteoclasts. J Cell Biochem. 1999:76:206-216.
85. Kousteni S, Bellido T, Plotkin LI, O'Brien CA, Bodenner DL, Han L, Han K, DiGregorio GB. Katzenellenbogen JA, Katzenellenbogen BS, Roberson PK, Weinstein RS, Jilka RL, Manolagas SC, Nongenotropic, sex-nonspecific signaling through the estrogen or androgen receptors: Dissociation from transcriptional activity. Cell. 2001;104:719-730
86. Castoria G, Migliaccio A, Bilancio A, Di Domenico M, de Falco A, Lombardi M, Fiorentino R. Varricchio L, Barone MV, Auricchio F. P13-kinase in concert with Src promotes the S-phase entry of oestradiol-stimulated MCF-7 cells. EMBO J. 2001;20:6050-6059.
87. Wong BR, Besser D, Kim N, Arron JR, Vologodskaia M, Hanafusa H, Choi Y. TRANCE, a TNF family member, activates Akt/PKB through a signaling complex involving TRAF6 and c-Src. Mol Cell. 1999;4:1041-1049.
88. Kubota Y, Tanaka T, Kitanaka A, Ohnishi H, Okutani Y, Waki M, Ishida T, Kamano H. Src transduces erythropoietin-induced differentiation signals through phosphatidylinositol 3-kinase. EMBO J. 2001;20:5666-5677.
89. Scheuer J, Malhotra A, Schaible TF, Capasso J, Effects of gonadectomy and hormonal replacement on rat hearts. Circ Res. 1987;61:12-19.
90. van Eickels M, Grohe C, Cleutjens JP, Janssen B J, Wellens HJ, Doevendans PA. 17β-estradiol attenuates the development of pressure-overload hypertrophy. Circulation. 2001;104:1419-1423.
91. Sugden PH, Clerk A. "Stress-responsive" mitogen-activated protein kinases (c-Jun N-terminal kinases and p38 mitogen-activated protein kinases) in the myocardium. Circ Res. 1998;83:345-352.
92. Clerk A, Michael A. Sugden PH. Stimulation of the p38 mitogen-activated protein kinase pathway in neonatal rat ventricular myocytes by the G protein-coupled receptor agonists, endothelin-1 and phenylephrine: A role in cardiac myocyte hypertrophy? J Cell Biol. 1998;142:523-535.
93. Zhang CC, Shapiro DJ. Activation of the p38 mitogen-activated protein kinase pathway by estrogen or by 4-hydroxytamoxifen is coupled to estrogen receptor-induced apoptosis, J Biol Chem. 2000;275:479-486.
94. Mital S, Barbone A, Addonizio LJ, Quaegebeur JM, Mosca RJ, Oz MC, Hintze TH. Endogenous endothelium-derived nitric oxide inhibits myocardial caspase activity: Implications for treatment of end-stage heart failure. J Heart Lung Transplant. 2002;21:576-585.
95. Power RF, Mani SK, Codina J, Conneely OM, O'Malley BW. Dopaminergic and ligand-independent activation of steroid hormone receptors. Science. 1991:254:1636-1639.
96. Smith CL, Conneely OM, O'Malley BW. Modulation of the ligand-independent activation of the human estrogen receptor by hormone and antihormone, Proc Natl Acad Sci USA. 1993;90:6120-6124.
97. Karas RH, Gauer EA, Bieber HE, Baur WE, Mendelsohn ME. Growth factor activation of the estrogen receptor in vascular cells occurs via a mitogen-activated protein kinase-independent pathway. J Clin Invest. 1998;101:2851-2861.
98. Ince BA, Montano MM, Katzenellenbogen BS. Activation of transcriptionally inactive human estrogen receptors by cyclic adenosine 3′,5′-monophosphate and ligands including antiestrogens. Mol Endocrinol. 1994;8:1397-1406.
99. Schlegel A, Wang C, Katzenetlenbogen BS, Pestell RG, Lisanti MP. Caveolin-1 potentiates estrogen receptor a (ERa) signaling: Caveolin-1 drives ligand-independent nuclear translocation and activation of ERα. J Biol Chem. 1999;274:33551-33556.
100. Schlegel A, Wang C, Pestell RG, Lisanti MP. Ligand-independent activation of oestrogen receptor α by caveolin-1. Biochem J. 2001;359:203-210.
101. Neuman E, Ladha MH, Lin N, Upton TM, Miller SJ, DiRenzo J, Pestell RG, Hinds PW, Dowdy SF, Brown M, Ewen ME, Cyclin D1 stimulation of estrogen receptor transcriptional activity independent of cdk4. Mol Cell Biol. 1997;17:5338-5347.
102. Zwijsen RM, Wientjens E, Klompmaker R, van der Sman Srnan J, Bernards R, Michalides RJ. CDK-independent activation of estrogen receptor by cyclin D1. Cell. 1997;88:405-415.
103. Zwijsen RM, Buckle RS, Hijmans EM, Loomans CJ. Bernards R. Ligand-independent recruitment of steroid receptor coactivators to estrogen receptor by cyclin D1 Genes Dev. 1998;12:3488-3498.
104. Trowbridge JM, Rogatsky I, Garabedian MJ. Regulation of estrogen receptor transcriptional enhancement by the cyclin A/Cdk2 complex. Proc Natl Acad Sci U S A. 1997;94:10132-10137.
105. Kato S, Masuhiro Y, Watanabe M, Kobayashi Y, Takeyama KI, Endoh H, Yanagisawa J. Molecular mechanism of a cross-talk between oestrogen and growth factor signalling pathways. Genes Cells. 2000;5:593-601.
106. Bunone G, Briand PA, Miksicek RJ. Picard D. Activation of the unliganded estrogen receptor by EGF involves the MAP kinase pathway and direct phosphorylation. EMBO J. 1996:15:2174-2183.
107. Kato S, Endoh H, Masuhiro Y, Kitamoto T, Uchiyama S, Sasaki H, Masushige S, Gotoh Y, Nishida E, Kawashima H, et al. Activation of the estrogen receptor through phosphorylation by mitogen-activated protein kinase. Science. 1995:270:1491-1494.
108. Endoh H, Maruyama K, Masuhiro Y, Kobayashi Y, Goto M, Tai H, Yanagisawa J, Metzger D, Hashimoto S. Kato S. Purification and identification of p68 RNA helicase acting as a transcriptional coactivator specific for the activation function I of human estrogen receptor α. Mol Cell Biol. 1999;19:5363-5372.
109. Ignar-Trowbridge DM, Teng CT, Ross KA, Parker MG, Korach KS, McLachlan JA. Peptide growth factors elicit estrogen receptordependent transcriptional activation of an estrogen-responsive element. Mol Endocrinol. 1993:7:992-998.
110. Aronica SM, Katzenellenbogen BS. Stimulation of estrogen receptor-mediated transcription and alteration in the phosphorylation state of the rat uterine estrogen receptor by estrogen, cyclic adenosine monophosphate, and insulin-like growth factor-1. Mol Endocrinol. 1993;7:743-752.
111. Ignar-Trowbridge DM, Pimentel M, Parker MG, McLachlan JA, Korach KS. Peptide growth factor cross-talk with the estrogen receptor requires the A/B domain and occurs independently of protein kinase C or estradiol. Endocrinology. 1996;137:1735-1744.
112. Rowan BG, Weigel NL, O'Malley BW. Phosphorylation of steroid receptor coactivator-1: Identification of the phosphorylation sites and phosphorylation through the mitogen-activated protein kinase pathway. J Biol Chem. 2000;275:4475-4483.
113. Martin MB, Franke TF, Stoica GE, Chambon P, Katzenellenbogen BS, Stoica BA, McLemore MS, Olivo SE, Stoica A. A role for Akt in mediating the estrogenic functions of epidermal growth factor and insulin-like growth factor 1 Endocrinology. 2000;141:4503-4511
114. Sun M, Paciga JE. Feldman RI, Yuan Z, Coppola D, Lu YY, Shelley SA, Nicosia SV, Cheng JQ. Phosphatidylinositol-3-OH kinase (PI3K)/AKT2, activated in breast cancer, regulates and is induced by estrogen receptor α (ERα) via interaction between ERα and PI3K. Cancer Res. 2001;61:5985-5991.
115. Feng W. Webb P, Nguyen P,. Liu X, Li J, Karin M, Kushner PJ. Potentiation of estrogen receptor activation function I (AF-1) by Src/JNK through a serine 118-independent pathway. Mol Endocrinol., 2001;15:32-45.
116. Lu Q, Ebling H, Mittler J, Baur WE, Karas RH. MAP kinase mediates growth factor-induced nuclear translocation of estrogen receptor α. FEBS Lett. 2002;516:1-8.
117. Chambliss KL, Shaul PW, Rapid activation of endothelial NO synthase by estrogen: Evidence for a steroid receptor fast-action complex (SRFC) in caveolae. Steroids. 2002;67:413-419.
118. Chambliss KL, Yuhanna IS, Mineo C, Liu P, German Z, Sherman TS, Mendelsohn ME, Anderson RG, Shaul PW. Estrogen receptor α and endothelial nitric oxide synthase are organized into a functional signaling module in caveolae. Circ Res. 2000;87:E44-E52.
119. Kim HP, Lee JY, Jeong JK, Bae SW, Lee HK, Jo I. Nongenomic stimulation of nitric oxide release by estrogen is mediated by estrogen receptor α localized in caveolae. Biochem Biophys Res Commun. 1999;263:257-262.
120. Gratton JP. Fontana J, O'Connor DS, Garcia-Cardena G, McCabe TJ, Sessa WC. Reconstitution of an endothelial nitric-oxide synthase (eNOS), hsp90, and caveolin-1 complex in vitro: Evidence that hsp90 facilitates calmodulin stimulated displacement of eNOS from caveolin-1. J Biol Chem. 2000;275:22268-22272.
121. Feron O, Saldana F, Michel JB, Michel T. The endothelial nitric-oxide synthase-caveolin regulatory cycle. J Biol Chem. 1998;273:3125-3128.
122. Bucci M, Gratton JP, Rudic RD, Acevedo L, Roviezzo F, Cirino G, Sessa WC, In vivo delivery of the caveolin-1 scaffolding domain inhibits nitric oxide synthesis and reduces inflammation., Nat Med. 2000;6:1362-1367.
123. Wyckoff MH, Chambliss KL, Mineo C, Yuhanna IS, Mendelsohn ME, Mumby SM, Shaul PW, Plasma membrane estrogen receptors are coupled to endothelial nitric-oxide synthase through Gα(i). J Biol Chem. 2001;276:27071-27076.
124. Benten WP, Stephan C, Lieberherr M, Wunderlich F. Estradiol signaling via sequestrable surface receptors. Endocrinology. 2001;142:1669-1677.
125. Guo Z, Krucken J, Benten WP, Wunderlich F. Estradiol-induced nongenomic calcium signaling regulates genotropic signaling in macrophages. J Biol Chem. 2002;277:7044-7050.
126. Moss RL, Gu Q. Estrogen: Mechanisms for a rapid action in CA1 hippocampal neurons. Steroids. 1999;64:14-21.
127. Nethrapalli IS, Singh M, Guan X, Guo Q, Lubahn DB, Korach KS. Toran-Allerand CD. Estradiol (E2) elicits SRC phosphorylation in the mouse neocortex: The initial event in E2 activation of the MAPK cascade? Endocrinology. 2001;142:5145-5148.
128. Singh M, Setalo G Jr, Guan X, Frail DE, Toran-Allerand CD. Estrogen-induced activation of the mitogen-activated protein kinase cascade in the cerebral cortex of estrogen receptor-α knock-out mice. J Neurosci. 2000;20:1694-1700.
129. Setalo G Jr, Singh M, Guan X, Toran-Allerand CD. Estradiol-induced phosphorylation of ERK1/2 in explants of the mouse cerebral cortex: The roles of heat shock protein 90 (Hsp90) and MEK2. J Neurobiol. 2002;50:1-12.
130. Osborne CK, Zhao H, Fuqua SA. Selective estrogen receptor modulators: Structure, function, and clinical use. J Clin Oncol. 2000;18:3172-3186.
131. Burger HG. Selective oestrogen receptor modulators. Horm Res. 2000;53(suppl 3):25-29.
132. Williams JK, Wagner JD, Li Z, Golden DL, Adams MR. Tamoxifen inhibits arterial accumulation of LDL degradation products and progression of coronary artery atherosclerosis in monkeys. Arterioscler Thromb Vasc Biol. 1997;17:403-408.
133. Willson TM, Norris JD, Wagner BL, Asplin I, Baer P, Brown HR, Jones SA, Henke B, Sauls H, Wolfe S, Morris DC, McDonnell DP. Dissection of the molecular mechanism of action of GW5638, a novel estrogen receptor ligand, provides insights into the role of estrogen receptor in bone. Endocrinology. 1997;138:3901-3911.
134. Martel C, Provencher L, Li X, St Pierre A, Leblanc G. Gauthier S, Merand Y, Labrie F. Binding characteristics of novel nonsteroidal andestrogens to the rat uterine estrogen receptors. J Steroid Biochem Mol Biol. 1998;64:199-205.
135. Labrie F, Labrie C, Belanger A, Simard J, Giguere V, Tremblay A, Tremblay G. EM-652 (SCH57068), a pure SERM having complete antiestrogenic activity in the mammary gland and endometrium. J Steroid Biochem Mol Biol. 2001;79:213-225.
136. Simoncini T, Varone G, Fornari L, Mannella P, Luisi M. Labrie F, Genazzani AR. Genomic and nongenomic mechanisms of nitric oxide synthesis induction in human endothelial cells by a fourth-generation selective estrogen receptor modulator. Endocrinology. 2002;143:2052-2061.
137. Dardes RC, Schafer JM, Pearce ST, Osipo C, Chen B, Jordan VC. Regulation of estrogen target genes and growth by selective estrogen-receptor modulators in endometrial cancer cells. Gynecol Oncol. 2002;85:498-506.
138. Walsh BW. The effects of estrogen and selective estrogen receptor modulators on cardiovascular risk factors. Ann N Y Acad Sci. 2001;949:163-167.
139. Hisamoto K, Ohmichi M, Kanda Y, Adachi K, Nishio Y, Hayakawa J, Mabuchi S, Takahashi K, Tasaka K, Miyamoto Y, Taniguchi N, Murata Y. Induction of endothelial nitric-oxide synthase phosphorylation by the raloxifene analog LY117018 is differentially mediated by Akt and extracellular signal-regulated protein kinase in vascular endothelial cells. J Biol Chem. 2001;276:47642-47649.
140. Simoncini T, Genazzani AR, Liao JK, Nongenomic mechanisms of endothelial nitric oxide synthase activation by the selective estrogen receptor modulator raloxifene. Circulation. 2002;105:1368-1373.
141. Wassmann S, Laufs U, Stamenkovic D, Linz W, Stasch JP, Ahlbory K, Rosen R, Bohm M, Nickenig G. Raloxifene improves endothelial dysfunction in hypertension by reduced oxidative stress and enhanced nitric oxide production. Circulation. 2002;105:2083-2091.
142. Figtree GA, Lu Y, Webb CM, Collins P. Raloxifene acutely relaxes rabbit coronary arteries in vitro by an estrogen receptor-dependent and nitric oxide-dependent mechanism. Circulation. 1999;100:1095-1101.
143. Katzenellenbogen BS, Choi I, Delage-Mourroux R, Ediger TR, Martini PG, Montano M. Sun J. Weis K, Katzenellenbogen JA. Molecular mechanisms of estrogen action: Selective ligands and receptor pharmacology. J Steroid Biochem Mol Biol. 2000;74:279-285.
144. McDonnell DP, Chang CY, Norris JD. Capitalizing on the complexities of estrogen receptor pharmacology in the quest for the perfect SERM. Ann N Y Acad Sci. 2001;949:16-35.
145. Lee EJ, Jakacka M, Duan WR. Chien PY, Martinson F, Gehm BD, Jameson JL. Adenovirus-directed expression of dominant negative estrogen receptor induces apoptosis in breast cancer cells and regression of tumors in nude mice. Mol Med., 2001;7:773-782.
146. Brzozowski AM, Pike AC, Dauter Z, Hubbard RE, Bonn T, Engstrom O, Ohman L, Greene GL, Gustafsson JA, Carlquist M. Molecular basis of agonism and antagonism in the oestrogen receptor. Nature. 1997;389:753-758.
147. Montano MM, Ekena K, Delage-Mourroux R, Chang W, Martini P, Katzenellenbogen BS. An estrogen receptor-selective coregulator that potentiates the effectiveness of antiestrogens and represses the activity of estrogens. Proc Natl Acad Sci USA. 1999;96:6947-6952.
148. Grady D, Herrington D, Bittner V,. Blumenthal R, Davidson M, Hlatky M, Hsia J, Hulley S, Herd A, Khan S, Newby LK, Waters D, Vittinghoff E, Wenger N. Cardiovascular disease outcomes during 6.8 years of hormone therapy: Heart and Estrogen/Progestin Replacement Study follow-up (HERS II). JAMA. 2002;288:49-57.
149. Fornander T, Rutqvist LE, Cedermark B, Glas U, Mattsson A, Silfversward C, Skoog L, Somell A, Theve T, Wilking N, et al. Adjuvant tamoxifen in early breast cancer: Occurrence of new primary cancers. Lancet. 1989;1:117-120.
150. Dardes RC, O'Regan RM, Gajdos C, Robinson SP, Bentrem D, De Los Reyes A, Jordan VC. Effects of a new clinically relevant antiestrogen (GW5638) related to tamoxifen on breast and endometrial cancer growth in vivo. Clin Cancer Res. 2002:8:1995-2001.
151. Gottardis MM, Jordan VC, Antitumor actions of keoxifene and tamoxifen in the N-nitrosomethylurea-induced rat mammary carcinoma model. Cancer Res. 1987:47:4020-4024.
152. Jordan VC, Gosden B. Inhibition of the uterotropic activity of estrogens and antiestrogens by the short acting antiestrogen LY117018. Endocrinology. 1983;113:463-468.
153. Li X, Takahashi M. Kushida K, Inoue T. The preventive and interventional effects of raloxifene analog (LY117018 HCL) on osteopenia in ovariectomized rats. J Bone Miner Res. 1998;13:1005-1010.