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Molecular Endocrinology, Vol 9, 659-669, Copyright © 1995 by Endocrine Society

ARTICLES

Analysis of estrogen receptor function in vitro reveals three distinct classes of antiestrogens

DP McDonnell, DL Clemm, T Hermann, ME Goldman and JW Pike
Department of Pharmacology, Duke University Medical School, Durham, North Carolina 27710, USA.

We have developed a series of in vitro models with which to evaluate the biological activity of estrogen receptor (ER) agonists and antagonists. Using a protease digestion assay we show that the conformational changes induced within ER are distinct for agonists and antagonists. However, this assay is unable to discriminate between pure antagonists like ICI164,384 and partial agonists such as 4-OH tamoxifen or keoxifene. Using a chimeric ER-VP16 construct, we demonstrate that both pure antagonists and partial agonists deliver ER to its DNA target within cells. However, the ability of the DNA-bound receptor to activate transcription in the presence of a given antagonist is dependent on cell and promoter context. These data, suggesting functional differences among ER antagonists, were confirmed by additional experiments demonstrating that their ability to modulate the transcriptional activity of a series of ER mutants is dramatically different. Depending on the cell and promoter context and the particular ER form expressed, 4-OH tamoxifen and the related compound, keoxifene, functioned as partial agonists. Importantly, the transcriptional profiles of these two compounds were dissimilar, suggesting that they are functionally different from each other and from ICI164,384, which does not display agonist activity under any context examined. Our results reveal functional differences between these clinically important antiestrogens and suggest that the distinct biologies manifest by these compounds in vivo relate to their ability to differentially regulate ER function.


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 Nucleic Acids ResHome page
F. G. Petit, Y. Valotaire, and F. Pakdel
The analysis of chimeric human/rainbow trout estrogen receptors reveals amino acid residues outside of P- and D-boxes important for the transactivation function
Nucleic Acids Res., July 15, 2000; 28(14): 2634 - 2642.
[Abstract] [Full Text] [PDF]

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 Mol. Pharmacol.Home page
M. D. Galigniana, G. P. Vicent, G. Piwien-Pilipuk, G. Burton, and C. P. Lantos
Mechanism of Action of the Potent Sodium-Retaining Steroid 11,19-Oxidoprogesterone
Mol. Pharmacol., July 1, 2000; 58(1): 58 - 70.
[Abstract] [Full Text]

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 J Natl Cancer Inst MonogrHome page
R. B. Dickson and G. M. Stancel
Chapter 8: Estrogen Receptor-Mediated Processes in Normal and Cancer Cells
J Natl Cancer Inst Monographs, July 1, 2000; 2000(27): 135 - 145.
[Abstract] [Full Text] [PDF]

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 Mol. Cell. Biol.Home page
P. H. Giangrande, E. A. Kimbrel, D. P. Edwards, and D. P. McDonnell
The Opposing Transcriptional Activities of the Two Isoforms of the Human Progesterone Receptor Are Due to Differential Cofactor Binding
Mol. Cell. Biol., May 1, 2000; 20(9): 3102 - 3115.
[Abstract] [Full Text]

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 Mol. Endocrinol.Home page
A. van den Wijngaard, W. R. Mulder, R. Dijkema, C. J .C. Boersma, S. Mosselman, E. J. J. van Zoelen, and W. Olijve
Antiestrogens Specifically Up-Regulate Bone Morphogenetic Protein-4 Promoter Activity in Human Osteoblastic Cells
Mol. Endocrinol., May 1, 2000; 14(5): 623 - 633.
[Abstract] [Full Text]

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 J. Biol. Chem.Home page
B. Saville, M. Wormke, F. Wang, T. Nguyen, E. Enmark, G. Kuiper, J.-A. Gustafsson, and S. Safe
Ligand-, Cell-, and Estrogen Receptor Subtype (alpha /beta )-dependent Activation at GC-rich (Sp1) Promoter Elements
J. Biol. Chem., February 25, 2000; 275(8): 5379 - 5387.
[Abstract] [Full Text] [PDF]

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 Reproductive SciencesHome page
D. P. McDonnell
Selective Estrogen Receptor Modulators (SERMs): A First Step in the Development of Perfect Hormone Replacement Therapy Regimen
Reproductive Sciences, January 1, 2000; 7(1_suppl): S10 - S15.
[Abstract] [PDF]

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 Mol. Endocrinol.Home page
D. Szapary, Y. Huang, and S. S. Simons Jr.
Opposing Effects of Corepressor and Coactivators in Determining the Dose-Response Curve of Agonists, and Residual Agonist Activity of Antagonists, for Glucocorticoid Receptor-Regulated Gene Expression
Mol. Endocrinol., December 1, 1999; 13(12): 2108 - 2121.
[Abstract] [Full Text]

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 EndocrinologyHome page
K. W. Gaido, L. S. Leonard, S. C. Maness, J. M. Hall, D. P. McDonnell, B. Saville, and S. Safe
Differential Interaction of the Methoxychlor Metabolite 2,2-Bis-(p-Hydroxyphenyl)-1,1,1-Trichloroethane with Estrogen Receptors {alpha} and {beta}
Endocrinology, December 1, 1999; 140(12): 5746 - 5753.
[Abstract] [Full Text]

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 EndocrinologyHome page
A. L. Wijayaratne, S. C. Nagel, L. A. Paige, D. J. Christensen, J. D. Norris, D. M. Fowlkes, and D. P. McDonnell
Comparative Analyses of Mechanistic Differences Among Antiestrogens
Endocrinology, December 1, 1999; 140(12): 5828 - 5840.
[Abstract] [Full Text]

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 Hum ReprodHome page
A. M. Macpherson, D. F. Archer, S. Leslie, D.S. Charnock-Jones, W.K. Makkink, and S. K. Smith
The effect of etonogestrel on VEGF, oestrogen and progesterone receptor immunoreactivity and endothelial cell number in human endometrium
Hum. Reprod., December 1, 1999; 14(12): 3080 - 3087.
[Abstract] [Full Text] [PDF]

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 J. Biol. Chem.Home page
P. S. Jones, E. Parrott, and I. N. H. White
Activation of Transcription by Estrogen Receptor alpha and beta Is Cell Type- and Promoter-dependent
J. Biol. Chem., November 5, 1999; 274(45): 32008 - 32014.
[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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 BMJHome page
D. T Baird and A. F Glasier
Science, medicine, and the future: Contraception
BMJ, October 9, 1999; 319(7215): 969 - 972.
[Full Text]

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 J. Clin. Endocrinol. Metab.Home page
A. Negro-Vilar
Selective Androgen Receptor Modulators (SARMs): A Novel Approach to Androgen Therapy for the New Millennium
J. Clin. Endocrinol. Metab., October 1, 1999; 84(10): 3459 - 3462.
[Full Text] [PDF]

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 Mol. Endocrinol.Home page
P. Webb, P. Nguyen, C. Valentine, G. N. Lopez, G. R. Kwok, E. McInerney, B. S. Katzenellenbogen, E. Enmark, J.-A. Gustafsson, S. Nilsson, et al.
The Estrogen Receptor Enhances AP-1 Activity by Two Distinct Mechanisms with Different Requirements for Receptor Transactivation Functions
Mol. Endocrinol., October 1, 1999; 13(10): 1672 - 1685.
[Abstract] [Full Text]

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 Mol. Cell. Biol.Home page
H. Ma, H. Hong, S.-M. Huang, R. A. Irvine, P. Webb, P. J. Kushner, G. A. Coetzee, and M. R. Stallcup
Multiple Signal Input and Output Domains of the 160-Kilodalton Nuclear Receptor Coactivator Proteins
Mol. Cell. Biol., September 1, 1999; 19(9): 6164 - 6173.
[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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 J. Pharmacol. Exp. Ther.Home page
S. M. Hyder, C. Chiappetta, and G. M. Stancel
Synthetic Estrogen 17alpha -Ethinyl Estradiol Induces Pattern of Uterine Gene Expression Similar to Endogenous Estrogen 17beta -Estradiol
J. Pharmacol. Exp. Ther., August 1, 1999; 290(2): 740 - 747.
[Abstract] [Full Text]

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 Cancer Res.Home page
D. S. Hunter, L. C. Hodges, P. M. Vonier, R. Fuchs-Young, M. M. Gottardis, and C. L. Walker
Estrogen Receptor Activation via Activation Function 2 Predicts Agonism of Xenoestrogens in Normal and Neoplastic Cells of the Uterine Myometrium
Cancer Res., July 1, 1999; 59(13): 3090 - 3099.
[Abstract] [Full Text] [PDF]

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 NEJMHome page
M. E. Mendelsohn and R. H. Karas
The Protective Effects of Estrogen on the Cardiovascular System
N. Engl. J. Med., June 10, 1999; 340(23): 1801 - 1811.
[Full Text] [PDF]

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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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 J. Biol. Chem.Home page
S. Roux, B. Terouanne, B. Couette, M.-E. Rafestin-Oblin, and J.-C. Nicolas
Conformational Change in the Human Glucocorticoid Receptor Induced by Ligand Binding Is Altered by Mutation of Isoleucine 747 by a Threonine
J. Biol. Chem., April 9, 1999; 274(15): 10059 - 10065.
[Abstract] [Full Text] [PDF]

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 Mol. Cell. Biol.Home page
L. H. Milocco, J. A. Haslam, J. Rosen, and H. M. Seidel
Design of Conditionally Active STATs: Insights into STAT Activation and Gene Regulatory Function
Mol. Cell. Biol., April 1, 1999; 19(4): 2913 - 2920.
[Abstract] [Full Text] [PDF]

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 Cell Growth Differ.Home page
S. M. Thacher, S. Nagpal, E. S. Klein, T. Arefieg, G. Krasinski, D. DiSepio, C. Agarwal, A. Johnson, R. L. Eckert, and R. A. S. Chandraratna
Cell Type and Gene-specific Activity of the Retinoid Inverse Agonist AGN 193109: Divergent Effects from Agonist at Retinoic Acid Receptor {{gamma}} in Human Keratinocytes
Cell Growth Differ., April 1, 1999; 10(4): 255 - 262.
[Abstract] [Full Text]

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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
A. Elbrecht, Y. Chen, A. Adams, J. Berger, P. Griffin, T. Klatt, B. Zhang, J. Menke, G. Zhou, R. G. Smith, et al.
L-764406 Is a Partial Agonist of Human Peroxisome Proliferator-activated Receptor gamma . THE ROLE OF CYS313 IN LIGAND BINDING
J. Biol. Chem., March 19, 1999; 274(12): 7913 - 7922.
[Abstract] [Full Text] [PDF]

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 J. Biol. Chem.Home page
J. Berger, M. D. Leibowitz, T. W. Doebber, A. Elbrecht, B. Zhang, G. Zhou, C. Biswas, C. A. Cullinan, N. S. Hayes, Y. Li, et al.
Novel Peroxisome Proliferator-activated Receptor (PPAR) gamma  and PPARdelta Ligands Produce Distinct Biological Effects
J. Biol. Chem., March 5, 1999; 274(10): 6718 - 6725.
[Abstract] [Full Text] [PDF]

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 ANN INTERN MEDHome page
W. Khovidhunkit and D. M. Shoback
Clinical Effects of Raloxifene Hydrochloride in Women
Ann Intern Med, March 2, 1999; 130(5): 431 - 439.
[Abstract] [Full Text] [PDF]

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 EndocrinologyHome page
B. S. McEwen, P. Tanapat, and N. G. Weiland
Inhibition of Dendritic Spine Induction on Hippocampal CA1 Pyramidal Neurons by a Nonsteroidal Estrogen Antagonist in Female Rats
Endocrinology, March 1, 1999; 140(3): 1044 - 1047.
[Abstract] [Full Text]

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 EndocrinologyHome page
B. L. Wagner, G. Pollio, P. Giangrande, J. C. Webster, M. Breslin, D. E. Mais, C. E. Cook, W. V. Vedeckis, J. A. Cidlowski, and D. P. McDonnell
The Novel Progesterone Receptor Antagonists RTI 3021-012 and RTI 3021-022 Exhibit Complex Glucocorticoid Receptor Antagonist Activities: Implications for the Development of Dissociated Antiprogestins
Endocrinology, March 1, 1999; 140(3): 1449 - 1458.
[Abstract] [Full Text]

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 Mol. Cell. Biol.Home page
D. Chen, P. E. Pace, R. C. Coombes, and S. Ali
Phosphorylation of Human Estrogen Receptor alpha  by Protein Kinase A Regulates Dimerization
Mol. Cell. Biol., February 1, 1999; 19(2): 1002 - 1015.
[Abstract] [Full Text] [PDF]


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