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Vol. 50, Issue 2, 151-196, June 1998

Basic Guide to the Mechanisms of Antiestrogen Action

Jennifer I. Macgregor and V. Craig Jordana

Robert H. Lurie Comprehensive Cancer Center, Northwestern University Medical School, Chicago, Illinois

I. Introduction
II. Unresolved Issues in 1984
    A. Species Differences
    B. Differences Between Antiestrogens In Vivo and In Vitro
    C. Antiestrogen Binding Sites
III. The Estrogen Receptor
IV. A Second Receptor
V. Estrogen Receptor
    A. Receptor Functions
    B. Estrogen Action
VI. Estrogen Receptor Regulation
    A. Estrogen Withdrawal
    B. Receptor Regulation
    C. Loss of the Receptor
VII. Antiestrogen Classification
    A. Type I
    B. Type II
VIII. Mechanisms of Antiestrogen Action
    A. Receptor Mutation and Antiestrogens
    B. Interactions with Estrogen Response Elements
IX. Antiestrogens and the Cell Cycle
X. Antiestrogens and Growth Factors
    A. Transforming Growth Factor alpha
    B. Transforming Growth Factor beta
    C. Insulin-Like Growth Factor
XI. Clinical Value of Tamoxifen
    A. Contralateral Breast Cancer
    B. Endocrine Function and Tamoxifen
    C. Tamoxifen and Bone
    D. Tamoxifen and Lipids
XII. Complexity of Antiestrogen Action
    A. Estrogen Receptor-Associated Proteins
    B. Antiestrogen Response Elements
XIII. Concerns with Tamoxifen
    A. Uterine Carcinogenesis
    B. Rat Liver Carcinogenesis
    C. Mechanism of Carcinogenesis
    D. Tamoxifen Metabolism
XIV. Drug Resistance Mechanisms
    A. Metabolic Activation
    B. Mutant Receptors
    C. Alternate Pathways
XV. Clinical Application of New Antiestrogens
    A. Tamoxifen Analogs for Breast Cancer
    B. Pure Antiestrogens for Breast Cancer
    C. Targeted Antiestrogens for Osteoporosis
        1. Raloxifene (also referred to in the literature as LY 156, 758, keoxifene, LY 139, 481-HCL, Evista®).
        2. Droloxifene.
        3. Idoxifene.
XVI. New Compounds and New Opportunities
    A. EM-800
    B. Peripheral Selectivity
XVII. Crystallization of the Raloxifene-Estrogen Receptor Complex
XVIII. Summary and Conclusions
Acknowledgments
References

a   Address for correspondence: V. Craig Jordan, Robert H. Lurie Comprehensive Cancer Center, 8258 Olson Pavilion, Northwestern University Medical School, 303 East Chicago Ave., Chicago, IL 60611.

0031-6997/98/5002-0151$03.00/0
PHARMACOLOGICAL REVIEWS
Copyright © 1998 by The American Society for Pharmacology and Experimental Therapeutics


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Endocrinology, June 1, 2001; 142(6): 2409 - 2418.
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 Cancer Res.Home page
H. Liu, E.-S. Lee, A. D. L. Reyes, J. W. Zapf, and V. C. Jordan
Silencing and Reactivation of the Selective Estrogen Receptor Modulator-Estrogen Receptor {{alpha}} Complex
Cancer Res., May 1, 2001; 61(9): 3632 - 3639.
[Abstract] [Full Text]

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 Cancer Res.Home page
A. McDougal, M. Wormke, J. Calvin, and S. Safe
Tamoxifen-induced Antitumorigenic/Antiestrogenic Action Synergized by a Selective Aryl Hydrocarbon Receptor Modulator
Cancer Res., May 1, 2001; 61(10): 3902 - 3907.
[Abstract] [Full Text]

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 FASEB J.Home page
C. M. CHENG, M. COHEN, J. WANG, and C. A. BONDY
Estrogen augments glucose transporter and IGF1 expression in primate cerebral cortex
FASEB J, April 1, 2001; 15(6): 907 - 915.
[Abstract] [Full Text] [PDF]

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 Toxicol SciHome page
K. C. Fertuck, J. B. Matthews, and T. R. Zacharewski
Hydroxylated Benzo[a]pyrene Metabolites Are Responsible for in Vitro Estrogen Receptor-Mediated Gene Expression Induced by Benzo[a]pyrene, but Do Not Elicit Uterotrophic Effects in Vivo
Toxicol. Sci., February 1, 2001; 59(2): 231 - 240.
[Abstract] [Full Text] [PDF]

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 Clin. Cancer Res.Home page
R. Stackievicz, L. Drucker, J. Radnay, Y. Beyth, S. Yarkoni, and I. Cohen
Tamoxifen Modulates Apoptotic Pathways in Primary Endometrial Cell Cultures
Clin. Cancer Res., February 1, 2001; 7(2): 415 - 420.
[Abstract] [Full Text]

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 JCOHome page
P. Fritz, T. E. Murdter, M. Eichelbaum, I. Siegle, M. Weissert, and U. M. Zanger
Microsomal Epoxide Hydrolase Expression as a Predictor of Tamoxifen Response in Primary Breast Cancer: A Retrospective Exploratory Study With Long-Term Follow-Up
J. Clin. Oncol., January 1, 2001; 19(1): 3 - 9.
[Abstract] [Full Text] [PDF]

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 Physiol. Rev.Home page
J. E. Compston
Sex Steroids and Bone
Physiol Rev, January 1, 2001; 81(1): 419 - 447.
[Abstract] [Full Text] [PDF]

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 J. Physiol.Home page
S. B Condliffe, C. M Doolan, and B. J Harvey
17{beta}-Oestradiol acutely regulates Cl- secretion in rat distal colonic epithelium
J. Physiol., January 1, 2001; 530(1): 47 - 54.
[Abstract] [Full Text] [PDF]

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 EndocrinologyHome page
J. L. Bowers, V. V. Tyulmenkov, S. C. Jernigan, and C. M. Klinge
Resveratrol Acts as a Mixed Agonist/Antagonist for Estrogen Receptors {alpha} and {beta}
Endocrinology, October 1, 2000; 141(10): 3657 - 3667.
[Abstract] [Full Text] [PDF]

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 JCOHome page
C. K. Osborne and S. A. W. Fuqua
Selective Estrogen Receptor Modulators: Structure, Function, and Clinical Use
J. Clin. Oncol., September 17, 2000; 18(17): 3172 - 3186.
[Abstract] [Full Text] [PDF]

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 Cancer Res.Home page
J. M. Schafer, H. Liu, D. J. Bentrem, J. W. Zapf, and V. C. Jordan
Allosteric Silencing of Activating Function 1 in the 4-Hydroxytamoxifen Estrogen Receptor Complex Is Induced by Substituting Glycine for Aspartate at Amino Acid 351
Cancer Res., September 1, 2000; 60(18): 5097 - 5105.
[Abstract] [Full Text]

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 FASEB J.Home page
J. ZHOU, S. NG, O. ADESANYA-FAMUIYA, K. ANDERSON, and C. A. BONDY
Testosterone inhibits estrogen-induced mammary epithelial proliferation and suppresses estrogen receptor expression
FASEB J, September 1, 2000; 14(12): 1725 - 1730.
[Abstract] [Full Text]

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 EndocrinologyHome page
I. M. Byrne, L. Flanagan, M. P. R. Tenniswood, and J. Welsh
Identification of a Hormone-Responsive Promoter Immediately Upstream of Exon 1c in the Human Vitamin D Receptor Gene
Endocrinology, August 1, 2000; 141(8): 2829 - 2836.
[Abstract] [Full Text] [PDF]

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 J Natl Cancer Inst MonogrHome page
R. Raftogianis, C. Creveling, R. Weinshilboum, and J. Weisz
Chapter 6: Estrogen Metabolism by Conjugation
J Natl Cancer Inst Monographs, July 1, 2000; 2000(27): 113 - 124.
[Abstract] [Full Text] [PDF]

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 J. Physiol.Home page
C. H Mitchell, K. Peterson-Yantorno, M. Coca-Prados, and M. M Civan
Tamoxifen and ATP synergistically activate Cl- release by cultured bovine pigmented ciliary epithelial cells
J. Physiol., May 15, 2000; 525(1): 183 - 193.
[Abstract] [Full Text] [PDF]

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 J. Biol. Chem.Home page
E. M. Resnick, D. A. Schreihofer, A. Periasamy, and M. A. Shupnik
Truncated Estrogen Receptor Product-1 Suppresses Estrogen Receptor Transactivation by Dimerization with Estrogen Receptors alpha and beta
J. Biol. Chem., March 15, 2000; 275(10): 7158 - 7166.
[Abstract] [Full Text] [PDF]

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 JNCI J Natl Cancer InstHome page
V. C. Jordan
How Is Tamoxifen's Action Subverted?
J Natl Cancer Inst, January 19, 2000; 92(2): 92 - 94.
[Full Text] [PDF]

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 Cancer Res.Home page
S. Ménard, P. Aiello, E. Tagliabue, C. Rumio, P. L. Lollini, M. I. Colnaghi, and A. Balsari
Tamoxifen Chemoprevention of a Hormone-independent Tumor in the Proto-neu Transgenic Mice Model
Cancer Res., January 1, 2000; 60(2): 273 - 275.
[Abstract] [Full Text]

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 Proc. Natl. Acad. Sci. USAHome page
J. An, R. C. J. Ribeiro, P. Webb, J.-A. Gustafsson, P. J. Kushner, J. D. Baxter, and D. C. Leitman
Estradiol repression of tumor necrosis factor-alpha transcription requires estrogen receptor activation function-2 and is enhanced by coactivators
PNAS, December 21, 1999; 96(26): 15161 - 15166.
[Abstract] [Full Text] [PDF]

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 J. Biol. Chem.Home page
K. Ozono, M. Saito, D. Miura, T. Michigami, S. Nakajima, and S. Ishizuka
Analysis of the Molecular Mechanism for the Antagonistic Action of a Novel 1alpha ,25-Dihydroxyvitamin D3 Analogue toward Vitamin D Receptor Function
J. Biol. Chem., November 5, 1999; 274(45): 32376 - 32381.
[Abstract] [Full Text] [PDF]

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 Cancer Res.Home page
V. Speirs, C. Malone, D. S. Walton, M. J. Kerin, and S. L. Atkin
Increased Expression of Estrogen Receptor {{beta}} mRNA in Tamoxifen-resistant Breast Cancer Patients
Cancer Res., November 1, 1999; 59(21): 5421 - 5424.
[Abstract] [Full Text] [PDF]

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 EndocrinologyHome page
S. L. Fitzpatrick, T. J. Berrodin, S. F. Jenkins, D. M. Sindoni, D. C. Deecher, and D. E. Frail
Effect of Estrogen Agonists and Antagonists on Induction of Progesterone Receptor in a Rat Hypothalamic Cell Line
Endocrinology, September 1, 1999; 140(9): 3928 - 3937.
[Abstract] [Full Text]

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 Cancer Res.Home page
J. I. MacGregor Schafer, H. Liu, D. A. Tonetti, and V. C. Jordan
The Interaction of Raloxifene and the Active Metabolite of the Antiestrogen EM-800 (SC 5705) with the Human Estrogen Receptor
Cancer Res., September 1, 1999; 59(17): 4308 - 4313.
[Abstract] [Full Text] [PDF]

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 Cancer Epidemiol. Biomarkers Prev.Home page
F. P. Li and A. S. Whittemore
Genetically Tailored Preventive Strategies: an Effective Plan for the Twenty-first Century?
Cancer Epidemiol. Biomarkers Prev., August 1, 1999; 8(8): 649 - 658.
[Abstract] [Full Text]

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 Endocr. Rev.Home page
V. C. Jordan and M. Morrow
Tamoxifen, Raloxifene, and the Prevention of Breast Cancer
Endocr. Rev., June 1, 1999; 20(3): 253 - 278.
[Abstract] [Full Text]

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 Endocr. Rev.Home page
J. F. Couse and K. S. Korach
Estrogen Receptor Null Mice: What Have We Learned and Where Will They Lead Us?
Endocr. Rev., June 1, 1999; 20(3): 358 - 417.
[Abstract] [Full Text]

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 Hum ReprodHome page
A. Dwivedi, F.W. Bansode, B.S. Setty, and J.D. Dhar
Endometrial steroid receptors during decidualization in rhesus monkey (Macaca mulatta); their modulation by anti-oestrogen CDRI-85/287
Hum. Reprod., April 1, 1999; 14(4): 1090 - 1095.
[Abstract] [Full Text] [PDF]

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 Proc. Natl. Acad. Sci. USAHome page
L. A. Paige, D. J. Christensen, H. Gron, J. D. Norris, E. B. Gottlin, K. M. Padilla, C.-y. Chang, L. M. Ballas, P. T. Hamilton, D. P. McDonnell, et al.
Estrogen receptor (ER) modulators each induce distinct conformational changes in ER alpha  and ER beta
PNAS, March 30, 1999; 96(7): 3999 - 4004.
[Abstract] [Full Text] [PDF]

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 J. Biol. Chem.Home page
J. S. Carroll, O. W. J. Prall, E. A. Musgrove, and R. L. Sutherland
A Pure Estrogen Antagonist Inhibits Cyclin E-Cdk2 Activity in MCF-7 Breast Cancer Cells and Induces Accumulation of p130-E2F4 Complexes Characteristic of Quiescence
J. Biol. Chem., December 1, 2000; 275(49): 38221 - 38229.
[Abstract] [Full Text] [PDF]

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 J. Biol. Chem.Home page
R. V. Weatherman and T. S. Scanlan
Unique Protein Determinants of the Subtype-selective Ligand Responses of the Estrogen Receptors (ERalpha and ERbeta ) at AP-1 Sites
J. Biol. Chem., February 2, 2001; 276(6): 3827 - 3832.
[Abstract] [Full Text] [PDF]

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 J. Biol. Chem.Home page
M. Gangloff, M. Ruff, S. Eiler, S. Duclaud, J. M. Wurtz, and D. Moras
Crystal Structure of a Mutant hERalpha Ligand-binding Domain Reveals Key Structural Features for the Mechanism of Partial Agonism
J. Biol. Chem., April 27, 2001; 276(18): 15059 - 15065.
[Abstract] [Full Text] [PDF]

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 J. Biol. Chem.Home page
H. H. Zhao, R. E. Herrera, E. Coronado-Heinsohn, M. C. Yang, J. H. Ludes-Meyers, K. J. Seybold-Tilson, Z. Nawaz, D. Yee, F. G. Barr, S. G. Diab, et al.
Forkhead Homologue in Rhabdomyosarcoma Functions as a Bifunctional Nuclear Receptor-interacting Protein with Both Coactivator and Corepressor Functions
J. Biol. Chem., July 20, 2001; 276(30): 27907 - 27912.
[Abstract] [Full Text] [PDF]

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 Proc. Natl. Acad. Sci. USAHome page
E. V. Jensen, G. Cheng, C. Palmieri, S. Saji, S. Makela, S. Van Noorden, T. Wahlstrom, M. Warner, R. C. Coombes, and J.-A. Gustafsson
Estrogen receptors and proliferation markers in primary and recurrent breast cancer
PNAS, December 18, 2001; 98(26): 15197 - 15202.
[Abstract] [Full Text] [PDF]


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