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Journal of Cell Science, Vol 106, Issue 4 1377-1388, Copyright © 1993 by Company of Biologists


JOURNAL ARTICLES

The antiestrogen ICI 182780 disrupts estrogen receptor nucleocytoplasmic shuttling

S Dauvois, R White and MG Parker
Molecular Endocrinology Laboratory, Imperial Cancer Research Fund, Lincoln's Inn Fields, London, UK.

The mouse estrogen receptor was shown to be constantly shuttling between the nucleus and cytoplasm although under steady-state conditions it is detected predominantly in the cell nucleus in both the absence and presence of estradiol. Shuttling was demonstrated by monitoring the transfer of protein between nuclei in heterokaryons and by examining the subcellular distribution of mutant receptors. In the presence of the partial antiestrogen 4-hydroxytamoxifen the receptor was retained in the nucleus whereas it accumulated in the cytoplasm when cells were treated with the pure antiestrogen ICI 182780. The effect of the pure antiestrogen was to inhibit nucleocytoplasmic shuttling of the receptor by blocking its nuclear uptake. Thus although ligand binding is not required by the estrogen receptor to undergo nucleocytoplasmic shuttling, this process can be disrupted by the binding of a pure antiestrogen.
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Proteasome-Mediated Proteolysis of Estrogen Receptor: A Novel Component in Autologous Down-Regulation
Mol. Endocrinol., September 1, 1999; 13(9): 1522 - 1534.
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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.
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J. Biol. Chem.Home page
M. D. Galigniana, P. R. Housley, D. B. DeFranco, and W. B. Pratt
Inhibition of Glucocorticoid Receptor Nucleocytoplasmic Shuttling by Okadaic Acid Requires Intact Cytoskeleton
J. Biol. Chem., June 4, 1999; 274(23): 16222 - 16227.
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CarcinogenesisHome page
W. G.R. Angus, M. C. Larsen, and C. R. Jefcoate
Expression of CYP1A1 and CYP1B1 depends on cell-specific factors in human breast cancer cell lines: role of estrogen receptor status
Carcinogenesis, June 1, 1999; 20(6): 947 - 955.
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Mol. Endocrinol.Home page
C. C. Zhang, S. Krieg, and D. J. Shapiro
HMG-1 Stimulates Estrogen Response Element Binding by Estrogen Receptor from Stably Transfected HeLa Cells
Mol. Endocrinol., April 1, 1999; 13(4): 632 - 643.
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Mol. Endocrinol.Home page
J. Liu and D. B. DeFranco
Chromatin Recycling of Glucocorticoid Receptors: Implications for Multiple Roles of Heat Shock Protein 90
Mol. Endocrinol., March 1, 1999; 13(3): 355 - 365.
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Mol. Cell. Biol.Home page
J. G. A. Savory, B. Hsu, I. R. Laquian, W. Giffin, T. Reich, R. J. G. Hache, and Y. A. Lefebvre
Discrimination between NL1- and NL2-Mediated Nuclear Localization of the Glucocorticoid Receptor
Mol. Cell. Biol., February 1, 1999; 19(2): 1025 - 1037.
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Mol. Biol. CellHome page
H. Htun, L. T. Holth, D. Walker, J. R. Davie, and G. L. Hager
Direct Visualization of the Human Estrogen Receptor alpha  Reveals a Role for Ligand in the Nuclear Distribution of the Receptor
Mol. Biol. Cell, February 1, 1999; 10(2): 471 - 486.
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J. Biol. Chem.Home page
R. J. G. Hache, R. Tse, T. Reich, J. G. A. Savory, and Y. A. Lefebvre
Nucleocytoplasmic Trafficking of Steroid-free Glucocorticoid Receptor
J. Biol. Chem., January 15, 1999; 274(3): 1432 - 1439.
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Cancer Res.Home page
Z. Nawaz, G. M. Stancel, and S. M. Hyder
The Pure Antiestrogen ICI 182,780 Inhibits Progestin-induced Transcription
Cancer Res., January 1, 1999; 59(2): 372 - 376.
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Mol. Endocrinol.Home page
M. D. Galigniana, J. L. Scruggs, J. Herrington, M. J. Welsh, C. Carter-Su, P. R. Housley, and W. B. Pratt
Heat Shock Protein 90-Dependent (Geldanamycin-Inhibited) Movement of the Glucocorticoid Receptor through the Cytoplasm to the Nucleus Requires Intact Cytoskeleton
Mol. Endocrinol., December 1, 1998; 12(12): 1903 - 1913.
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Mol. Endocrinol.Home page
R. K. Tyagi, L. Amazit, P. Lescop, E. Milgrom, and A. Guiochon-Mantel
Mechanisms of Progesterone Receptor Export from Nuclei: Role of Nuclear Localization Signal, Nuclear Export Signal, and Ran Guanosine Triphosphate
Mol. Endocrinol., November 1, 1998; 12(11): 1684 - 1695.
[Abstract] [Full Text]


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EndocrinologyHome page
S. Migliaccio, T. F. Washburn, S. Fillo, H. Rivera, A. Teti, K. S. Korach, and W. C. Wetsel
Modulation of Estrogen Receptor Levels in Mouse Uterus by Protein Kinase C Isoenzymes
Endocrinology, November 1, 1998; 139(11): 4598 - 4606.
[Abstract] [Full Text] [PDF]


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Mol. Endocrinol.Home page
J. Devin-Leclerc, X. Meng, F. Delahaye, P. Leclerc, E.-E. Baulieu, and M.-G. Catelli
Interaction and Dissociation by Ligands of Estrogen Receptor and Hsp90: The Antiestrogen RU 58668 Induces a Protein Synthesis-Dependent Clustering of the Receptor in the Cytoplasm
Mol. Endocrinol., June 1, 1998; 12(6): 842 - 854.
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Pharmacol. Rev.Home page
J. I. Macgregor and V. C. Jordan
Basic Guide to the Mechanisms of Antiestrogen Action
Pharmacol. Rev., June 1, 1998; 50(2): 151 - 196.
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The OncologistHome page
K. Yao and V. C. Jordan
Questions about Tamoxifen and the Future Use of Antiestrogens
Oncologist, April 1, 1998; 3(2): 104 - 110.
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J. Biol. Chem.Home page
G. F. Sewack and U. Hansen
Nucleosome Positioning and Transcription-associated Chromatin Alterations on the Human Estrogen-responsive pS2 Promoter
J. Biol. Chem., December 5, 1997; 272(49): 31118 - 31129.
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J. Biol. Chem.Home page
M. Antoine, K. Reimers, C. Dickson, and P. Kiefer
Fibroblast Growth Factor 3, a Protein with Dual Subcellular Localization, Is Targeted to the Nucleus and Nucleolus by the Concerted Action of Two Nuclear Localization Signals and a Nucleolar Retention Signal
J. Biol. Chem., November 21, 1997; 272(47): 29475 - 29481.
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J. Biol. Chem.Home page
P. Pace, J. Taylor, S. Suntharalingam, R. C. Coombes, and S. Ali
Human Estrogen Receptor beta  Binds DNA in a Manner Similar to and Dimerizes with Estrogen Receptor alpha
J. Biol. Chem., October 10, 1997; 272(41): 25832 - 25838.
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CirculationHome page
N. H. Bjarnason, J. Haarbo, I. Byrjalsen, R. F. Kauffman, and C. Christiansen
Raloxifene Inhibits Aortic Accumulation of Cholesterol in Ovariectomized, Cholesterol-Fed Rabbits
Circulation, September 16, 1997; 96(6): 1964 - 1969.
[Abstract] [Full Text]


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EndocrinologyHome page
T. M. Willson, J. D. Norris, B. L. Wagner, I. Asplin, P. Baer, H. R. Brown, S. A. Jones, B. Henke, H. Sauls, S. Wolfe, et al.
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, September 1, 1997; 138(9): 3901 - 3911.
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Endocr. Rev.Home page
W. B. Pratt and D. O. Toft
Steroid Receptor Interactions with Heat Shock Protein and Immunophilin Chaperones
Endocr. Rev., June 1, 1997; 18(3): 306 - 360.
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JCBHome page
J. Yang, J. Liu, and D. B. DeFranco
Subnuclear Trafficking of Glucocorticoid Receptors In Vitro: Chromatin Recycling and Nuclear Export
J. Cell Biol., May 5, 1997; 137(3): 523 - 538.
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J. Biol. Chem.Home page
J. P. Williams, H. C. Blair, M. A. McKenna, S. E. Jordan, and J. M. McDonald
Regulation of Avian Osteoclastic H[IMAGE]-ATPase and Bone Resorption by Tamoxifen and Calmodulin Antagonists
J. Biol. Chem., May 24, 1996; 271(21): 12488 - 12495.
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J. Biol. Chem.Home page
H. Wang, G. A. Peters, X. Zeng, M. Tang, W. Ip, and S. A. Khan
Yeast Two-hybrid System Demonstrates That Estrogen Receptor Dimerization Is Ligand-dependent in Vivo
J. Biol. Chem., October 6, 1995; 270(40): 23322 - 23329.
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J. Biol. Chem.Home page
L. F. Su, R. Knoblauch, and M. J. Garabedian
Rho GTPases as Modulators of the Estrogen Receptor Transcriptional Response
J. Biol. Chem., January 26, 2001; 276(5): 3231 - 3237.
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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.
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J. Biol. Chem.Home page
M. D. Galigniana, C. Radanyi, J.-M. Renoir, P. R. Housley, and W. B. Pratt
Evidence That the Peptidylprolyl Isomerase Domain of the hsp90-binding Immunophilin FKBP52 Is Involved in Both Dynein Interaction and Glucocorticoid Receptor Movement to the Nucleus
J. Biol. Chem., April 27, 2001; 276(18): 14884 - 14889.
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J. Biol. Chem.Home page
R. A. Campbell, P. Bhat-Nakshatri, N. M. Patel, D. Constantinidou, S. Ali, and H. Nakshatri
Phosphatidylinositol 3-Kinase/AKT-mediated Activation of Estrogen Receptor alpha . A NEW MODEL FOR ANTI-ESTROGEN RESISTANCE
J. Biol. Chem., March 23, 2001; 276(13): 9817 - 9824.
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J. Biol. Chem.Home page
A. L. Wijayaratne and D. P. McDonnell
The Human Estrogen Receptor-alpha Is a Ubiquitinated Protein Whose Stability Is Affected Differentially by Agonists, Antagonists, and Selective Estrogen Receptor Modulators
J. Biol. Chem., September 14, 2001; 276(38): 35684 - 35692.
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Proc. Natl. Acad. Sci. USAHome page
M. W. Dudley, C. Q. Sheeler, H. Wang, and S. Khan
Activation of the human estrogen receptor by the antiestrogens ICI 182,780 and tamoxifen in yeast genetic systems: Implications for their mechanism of action
PNAS, March 28, 2000; 97(7): 3696 - 3701.
[Abstract] [Full Text] [PDF]




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