Estrogen receptor alpha: Impact of ligands on intracellular shuttling and turnover rate in breast cancer cells

Current Cancer Drug Targets

Volumn 6, Issue 1, 2006, Pages 39-64

  Leclercq, Guy ^a   Lacroix, Marc ^a   Laïos, Ioanna ^a   Laurent, Guy ^b  

^a JULES BORDET INSTITUTE   (Belgium)

^b UNIVERSITY OF MONS   (Belgium)

Author keywords

Breast cancer; Estrogen receptor ; Proteasome; Shuttling; Signal transduction; Trafficking; Transcription; Turnover

Indexed keywords

11 [4 (2 DIMETHYLAMINOETHOXY)PHENYL]ESTRADIOL; 11 [4 [[5 [(4,4,5,5,5 PENTAFLUOROPENTYL)SULFONYL]PENTYL]OXY]PHENYL] ESTRADIOL; 11 [4 [[5 [(4,4,5,5,5 PENTAFLUOROPENTYL)SULFONYL]PENTYL]OXY]PHENYL]ESTRADIOL; 2,3 DIARYLIMIDAZOLINE; AMINO ACID; ANSAMYCIN DERIVATIVE; ANTIESTROGEN; BENZYLOXYCARBONYLLEUCYLLEUCYLLEUCINAL; CALPASTATIN; COUMESTROL; CYCLOFENIL; DIETHYLSTILBESTROL; ESTRADIOL; ESTROGEN RECEPTOR ALPHA; FULVESTRANT; GELDANAMYCIN; GENISTEIN; GROWTH FACTOR; HEAT SHOCK PROTEIN 90 INHIBITOR; LEPTOMYCIN B; LIGAND; N BUTYL 11 (3,17BETA DIHYDROXYESTRA 1,3,5(10) TRIEN 7ALPHA YL) N METHYLUNDECANAMIDE; PIPERAZINE DERIVATIVE; PROTEASOME; PROTEASOME INHIBITOR; RADICICOL; RALOXIFENE; TAMOXIFEN; TRANSCRIPTION FACTOR; UNCLASSIFIED DRUG; UNINDEXED DRUG; ZK 164015;

BREAST CANCER; CANCER CELL CULTURE; CELL DIFFERENTIATION; CELL HETEROGENEITY; CELL MEMBRANE; CELL NUCLEUS; CELL PROLIFERATION; CONFORMATION; CYTOPLASM; DATA ANALYSIS; DNA BINDING; DRUG DESIGN; GENE CONTROL; GENE EXPRESSION; GENE FUNCTION; GENE STRUCTURE; GENOME; HUMAN; LIGAND BINDING; MEMBRANE TRANSPORT; MICROSOME; NONHUMAN; PROMOTER REGION; PROTEIN TRANSPORT; REVIEW; TRANSACTIVATION; TRANSCRIPTION INITIATION; ANIMAL; BREAST TUMOR; DRUG EFFECT; FEMALE; GENETICS; METABOLISM;

ANIMALS; BREAST NEOPLASMS; ESTROGEN RECEPTOR ALPHA; FEMALE; HUMANS; LIGANDS;

EID: 33644871076     PISSN: 15680096     EISSN: None     Source Type: Journal    
DOI: 10.2174/156800906775471716     Document Type: Review

References (216)

1. Enmark, E.; Pelto-Huikko, M.; Grandien, K.; Lagercrantz, S.; Lagercrantz, J.; Fried, G.; Nordenskjold, M.; Gustafsson, J. A. Human Estrogen Receptor Beta-Gene Structure, Chromosomal Localization, and Expression Pattern. J. Clin. Endocrinol. Metab. 1997, 82, 4258-4265.
2. Beato, M.; Herrlich, P.; Schutz, G. Steroid Hormone Receptors: Many Actors in Search of a Plot. Cell 1995, 83, 851-857.
3. Tsai, M. J.; O'Malley, B. W. Molecular Mechanisms of Action of Steroid/Thyroid Receptor Superfamily Members. Ann. Rev. Biochem. 1994, 63, 451-486.
4. Ignar-Trowbridge, D. M.; Nelson, K. G.; Bidwell, M. C.; Curtis, S. W.; Washburn, T. F.; McLachlan, J. A.; Korach, K. S. Coupling of Dual Signaling Pathways: Epidermal Growth Factor Action Involves the Estrogen Receptor. Proc. Natl. Acad. Sci. USA 1992, 89, 4658-4662.
5. Aronica, S. M.; Katzenellenbogen, B. S. 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-I. Mol. Endocrinol. 1993, 7, 743-752.
6. Smith, C. L.; Conneely, O. M.; O'Malley, B. W. Modulation of the Ligand-Independent Activation of the Human Estrogen Receptor by Hormone and Antihormone. Proc. Natl. Acad. Sci. USA 1993, 90, 6120-6124.
7. Driggers, P. H.; Segars, J. H. Estrogen Action and Cytoplasmic Signaling Pathways. Part II: the Role of Growth Factors and Phosphorylation in Estrogen Signaling. Trends Endocrinol. Metab. 2002, 13, 422-427.
8. Levin, E. R. Cellular Functions of Plasma Membrane Estrogen Receptors. Steroids 2002, 67, 471-475.
9. Watson, C. S.; Campbell, C. H.; Gametchu, B. The Dynamic and Elusive Membrane Estrogen Receptor-Alpha. Steroids 2002, 67, 429-437.
10. Santen, R. J.; Song, R. X.; McPherson, R.; Kumar, R.; Adam, L.; Jeng, M. H.; Yue, W. The Role of Mitogen-Activated Protein (MAP) Kinase in Breast Cancer. J. Steroid Biochem. Mol. Biol. 2002, 80, 239-256.
11. Levin, E. R. Bidirectional Signaling Between the Estrogen Receptor and the Epidermal Growth Factor Receptor. Mol. Endocrinol. 2003, 17, 309-317.
12. Freeman, B. C.; Yamamoto, K. R. Continuous Recycling: a Mechanism for Modulatory Signal Transduction. Trends Biochem. Sci. 2001, 26, 285-290.
13. Hager, G. L.; Lim, C. S.; Elbi, C.; Baumann, C. T. Trafficking of Nuclear Receptors in Living Cells. J. Steroid Biochem. Mol. Biol. 2000, 74, 249-254.
14. Stenoien, D. L.; Mancini, M. G.; Patel, K.; Allegretto, E. A.; Smith, C. L.; Mancini, M. A. Subnuclear Trafficking of Estrogen Receptor-Alpha and Steroid Receptor Coactivator-1. Mol. Endocrinol. 2000, 14, 518-534.
15. Stenoien, D. L.; Patel, K.; Mancini, M. G.; Dutertre, M.; Smith, C. L.; O'Malley, B. W.; Mancini, M. A. FRAP Reveals That Mobility of Oestrogen Receptor-Alpha Is Ligand- and Proteasome-Dependent. Nat. Cell Biol. 2001, 3, 15-23.
16. Maruvada, P.; Baumann, C. T.; Hager, G. L.; Yen, P. M. Dynamic Shuttling and Intranuclear Mobility of Nuclear Hormone Receptors. J. Biol. Chem. 2003, 278, 12425-12432.
17. Elbi, C.; Walker, D. A.; Romero, G.; Sullivan, W. P.; Toft, D. O.; Hager, G. L.; DeFranco, D. B. Molecular Chaperones Function As Steroid Receptor Nuclear Mobility Factors. Proc. Natl. Acad. Sci. USA 2004, 101, 2876-2881.
18. Maruvada, P.; Dmitrieva, N. I.; East-Palmer, J.; Yen, P. M. Cell Cycle-Dependent Expression of Thyroid Hormone Receptor-Beta Is a Mechanism for Variable Hormone Sensitivity. Mol. Biol. Cell 2004, 15, 1895-1903.
19. Lonard, D. M.; Nawaz, Z.; Smith, C. L.; O'Malley, B. W. The 26S Proteasome Is Required for Estrogen Receptor-Alpha and Coactivator Turnover and for Efficient Estrogen Receptor-Alpha Transactivation. Mol. Cell 2000, 5, 939-948.
20. Nawaz, Z.; O'Malley, B. W. Urban Renewal in the Nucleus: Is Protein Turnover by Proteasomes Absolutely Required for Nuclear Receptor-Regulated Transcription? Mol. Endocrinol. 2004, 18, 493-499.
21. Jordan, V. C. Antiestrogens and Selective Estrogen Receptor Modulators As Multifunctional Medicines. 1. Receptor Interactions. J. Med. Chem. 2003, 46, 883-908.
22. Jordan, V. C. Antiestrogens and Selective Estrogen Receptor Modulators As Multifunctional Medicines. 2. Clinical Considerations and New Agents. J. Med. Chem. 2003, 46, 1081-1111.
23. Meegan, M. J.; Lloyd, D. G. Advances in the Science of Estrogen Receptor Modulation. Curr. Med. Chem. 2003, 10, 181-210.
24. O'Regan, R. M.; Jordan, V. C. The Evolution of Tamoxifen Therapy in Breast Cancer: Selective Oestrogen-Receptor Modulators and Downregulators. Lancet Oncol. 2002, 3, 207-214.
25. Robertson, J. F. Selective Oestrogen Receptor Modulators/New Antioestrogens: a Clinical Perspective. Cancer Treat. Rev. 2004, 30, 695-706.
26. Ettinger, B.; Black, D. M.; Mitlak, B. H.; Knickerbocker, R. K.; Nickelsen, T.; Genant, H. K.; Christiansen, C.; Delmas, P. D.; Zanchetta, J. R.; Stakkestad, J.; Gluer, C. C.; Krueger, K.; Cohen, F. J.; Eckert, S.; Ensrud, K. E.; Avioli, L. V.; Lips, P.; Cummings, S. R. Reduction of Vertebral Fracture Risk in Postmenopausal Women With Osteoporosis Treated With Raloxifene: Results From a 3-Year Randomized Clinical Trial. Multiple Outcomes of Raloxifene Evaluation (MORE) Investigators. JAMA 1999, 282, 637-645.
27. Kalidas, M.; Hilsenbeck, S.; Brown, P. Defining the Role of Raloxifene for the Prevention of Breast Cancer. J. Natl. Cancer Inst. 2004, 96, 1731-1733.
28. McGuire, W. L. Hormone Receptors: Their Role in Predicting Prognosis and Response to Endocrine Therapy. Semin. Oncol. 1978, 5, 428-433.
29. Encarnacion, C. A.; Fuqua, S. A. Estrogen Receptor Variants in Breast Cancer. Cancer Treat. Res. 1994, 71, 97-109.
30. Murphy, L. C.; Dotzlaw, H.; Leygue, E.; Douglas, D.; Coutts, A.; Watson, P. H. Estrogen Receptor Variants and Mutations. J. Steroid Biochem. Mol. Biol. 1997, 62, 363-372.
31. Clark, J. H.; Peck, E. J. Jr. Female Sex Steroids: Receptors and Function. Monogr. Endocrinol. 1979, 14-I-XII, 1-245.
32. Korach, K. S.; Hillisch, A.; Fritzemeier K. H. E.; Eds.; New Molecular Mechanisms of Estrogen Action and Their Impact on Future Perspectives in Estrogen Therapy. Ernst Schering Research Foundation, Workshop 46. Springer, Berlin, 2004.
33. von Angerer, E.; Ed.; The Estrogen Receptor As a Target for Rational Drug Design; R. G. Landes Company: Austin, TX, 1995.
34. Maaroufi, Y.; Cleeren, A.; Leclercq, G. Inhibition of Estradiol Binding to Its Receptor by the Cupric Ion. J. Biol. Inorganic Chem. 1998, 5, 508-514.
35. Martin, M. B.; Reiter, R.; Pham, T.; Avellanet, Y. R.; Camara, J.; Lahm, M.; Pentecost, E.; Pratap, K.; Gilmore, B. A.; Divekar, S.; Dagata, R. S.; Bull, J. L.; Stoica, A. Estrogen-Like Activity of Metals in MCF-7 Breast Cancer Cells. Endocrinology 2003, 144, 2425-2436.
36. Johnson, M. D.; Kenney, N.; Stoica, A.; Hilakivi-Clarke, L.; Singh, B.; Chepko, G.; Clarke, R.; Sholler, P. F.; Lirio, A. A.; Foss, C.; Reiter, R.; Trock, B.; Paik, S.; Martin, M. B. Cadmium Mimics the in vivo Effects of Estrogen in the Uterus and Mammary Gland. Nat. Med. 2003, 9, 1081-1084.
37. Anstead, G. M.; Carlson, K. E.; Katzenellenbogen, J. A. The Estradiol Pharmacophore: Ligand Structure-Estrogen Receptor Binding Affinity Relationships and a Model for the Receptor Binding Site. Steroids 1997, 62, 268-303.
38. Fink, B. E.; Mortensen, D. S.; Stauffer, S. R.; Aron, Z. D.; Katzenellenbogen, J. A. Novel Structural Templates for Estrogen-Receptor Ligands and Prospects for Combinatorial Synthesis of Estrogens. Chem. Biol. 1999, 6, 205-219.
39. Jacquot, Y.; Rojas, C.; Refouvelet, B.; Robert, J. F.; Leclercq, G.; Xicluna, A. Recent Advances in the Development of Phytoestrogens and Derivatives: an Update of the Promising Perspectives in the Prevention of Postmenopausal Diseases. Mini Rev. Med. Chem. 2003, 3, 387-400.
40. Brzozowski, A. M.; Pike, A. C.; Dauter, Z.; Hubbard, R. E.; Bonn, T.; Engstrom, O.; Ohman, L.; Greene, G. L.; Gustafsson, J. A.; Carlquist, M. Molecular Basis of Agonism and Antagonism in the Oestrogen Receptor. Nature 1997, 389, 753-758.
41. Gust, R.; Keilitz, R.; Schmidt, K.; von Rauch, M. (4R,5S)/(4S,5R)-4,5- Bis(4-Hydroxyphenyl)-2-Imidazolines: Ligands for the Estrogen Receptor With a Novel Binding Mode. J. Med. Chem. 2002, 45, 3356-3365.
42. Gust, R.; Keilitz, R.; Schmidt, K. Synthesis, Structural Evaluation, and Estrogen Receptor Interaction of 2,3-Diarylpiperazines. J. Med. Chem. 2002, 45, 2325-2337.
43. Shiau, A. K.; Barstad, D.; Loria, P. M.; Cheng, L.; Kushner, P. J.; Agard, D. A.; Greene, G. L. The Structural Basis of Estrogen Receptor/Coactivator Recognition and the Antagonism of This Interaction by Tamoxifen. Cell 1998, 95, 927-937.
44. Kekenes-Huskey, P. M.; Muegge, I.; von Rauch, M.; Gust, R.; Knapp, E. W. A Molecular Docking Study of Estrogenically Active Compounds With 1,2-Diarylethane and 1,2-Diarylethene Pharmacophores. Bioorg. Med. Chem. 2004, 12, 6527-6537.
45. Jordan, V. C.; Schafer, J. M.; Levenson, A. S.; Liu, H.; Pease, K. M.; Simons, L. A.; Zapf, J. W. Molecular Classification of Estrogens. Cancer Res. 2001, 61, 6619-6623.
46. Bowler, J.; Lilley, T. J.; Pittam, J. D.; Wakeling, A. E. Novel Steroidal Pure Antiestrogens. Steroids 1989, 54, 71-99.
47. Wakeling, A. E.; Dukes, M.; Bowler, J. A Potent Specific Pure Antiestrogen with Clinical Potential. Cancer Res. 1991, 51, 3867-3873.
48. Van de Velde, P.; Nique, F.; Bouchoux, F.; Bremaud, J.; Hameau, M. C.; Lucas, D.; Moratille, C.; Viet, S.; Philibert, D.; Teutsch, G. RU 58,668, a New Pure Antiestrogen Inducing a Regression of Human Mammary Carcinoma Implanted in Nude Mice. J. Steroid Biochem. Mol. Biol. 1994, 48, 187-196.
49. von Angerer, E.; Knebel, N.; Kager, M.; Ganss, B. 1-(Aminoalkyl)-2- Phenylindoles As Novel Pure Estrogen Antagonists. J. Med. Chem. 1990, 33, 2635-2640.
50. Pike, A. C.; Brzozowski, A. M.; Walton, J.; Hubbard, R. E.; Thorsell, A. G.; Li, Y. L.; Gustafsson, J. A.; Carlquist, M. Structural Insights into the Mode of Action of a Pure Antiestrogen. Structure (Camb.) 2001, 9, 145-153.
51. Jordan, V. C.; Lieberman, M. E.; Cormier, E.; Koch, R.; Bagley, J. R.; Ruenitz, P. C. Structural Requirements for the Pharmacological Activity of Nonsteroidal Antiestrogens in vitro. Mol. Pharmacol. 1984, 26, 272-278.
52. Robertson, D. W.; Katzenellenbogen, J. A.; Hayes, J. R.; Katzenellenbogen, B. S. Antiestrogen Basicity - Activity Relationships: a Comparison of the Estrogen Receptor Binding and Antiuterotrophic Potencies of Several Analogues of (Z)-1,2-Diphenyl-1- [4- [2- (Dimethylamino) Ethoxy] Phenyl] -1-Butene (Tamoxifen, Nolvadex) Having Altered Basicity. J. Med. Chem. 1982, 25, 167-171.
53. Menasce, L. P.; White, G. R.; Harrison, C. J.; Boyle, J. M. Localization of the Estrogen Receptor Locus (ESR) to Chromosome 6q25.1 by FISH and a Simple Post-FISH Banding Technique. Genomics 1993, 17, 263-265.
54. Ponglikitmongkol, M.; Green, S.; Chambon, P. Genomic Organization of the Human Oestrogen Receptor Gene. EMBO J. 1988, 7, 3385-3388.
55. Kos, M.; Reid, G.; Denger, S.; Gannon, F. Minireview: Genomic Organization of the Human ERalpha Gene Promoter Region. Mol. Endocrinol. 2001, 15, 2057-2063.
56. Grandien, K. F.; Berkenstam, A.; Nilsson, S.; Gustafsson, J. A. Localization of DNase I Hypersensitive Sites in the Human Oestrogen Receptor Gene Correlates With the Transcriptional Activity of Two Differentially Used Promoters. J. Mol. Endocrinol. 1993, 10, 269-277.
57. Grandien, K.; Backdahl, M.; Ljunggren, O.; Gustafsson, J. A.; Berkenstam, A. Estrogen Target Tissue Determines Alternative Promoter Utilization of the Human Estrogen Receptor Gene in Osteoblasts and Tumor Cell Lines. Endocrinology 1995, 136, 2223-2229.
58. Weigel, R. J.; Crooks, D. L.; Iglehart, J. D.; deConinck, E. C. Quantitative Analysis of the Transcriptional Start Sites of Estrogen Receptor in Breast Carcinoma. Cell Growth Differ. 1995, 6, 707-711.
59. Hori, M.; Iwasaki, M.; Shimazaki, J.; Inagawa, S.; Itabashi, M. Assessment of Hypermethylated DNA in Two Promoter Regions of the Estrogen Receptor Alpha Gene in Human Endometrial Diseases. Gynecol. Oncol. 2000, 76, 89-96.
60. Widschwendter, M.; Jiang, G.; Woods, C.; Muller, H. M.; Fiegl, H.; Goebel, G.; Marth, C.; Muller-Holzner, E.; Zeimet, A. G.; Laird, P. W.; Ehrlich, M. DNA Hypomethylation and Ovarian Cancer Biology. Cancer Res. 2004, 64, 4472-4480.
61. Redeuilh, G.; Moncharmont, B.; Secco, C.; Baulieu, E. E. Subunit Composition of the Molybdate-Stabilized "8-9 S" Nontransformed Estradiol Receptor Purified From Calf Uterus. J. Biol. Chem. 1987, 262, 6969-6975.
62. Dittmar, K. D.; Hutchison, K. A.; Owens-Grillo, J. K.; Pratt, W. B. Reconstitution of the Steroid Receptor.Hsp90 Heterocomplex Assembly System of Rabbit Reticulocyte Lysate. J. Biol. Chem. 1996, 271, 12833-12839.
63. Pratt, W. B.; Toft, D. O. Regulation of Signaling Protein Function and Trafficking by the Hsp90/Hsp70-Based Chaperone Machinery. Exp. Biol. Med. (Maywood.) 2003, 228, 111-133.
64. Richter, K.; Buchner, J. Hsp90: Chaperoning Signal Transduction. J. Cell Physiol. 2001, 188, 281-290.
65. Wegele, H.; Muller, L.; Buchner, J. Hsp70 and Hsp90 - a Relay Team for Protein Folding. Rev. Physiol. Biochem. Pharmacol. 2004, 151, 1-44.
66. Knoblauch, R.; Garabedian, M. J. Role for Hsp90-Associated Cochaperone P23 in Estrogen Receptor Signal Transduction. Mol. Cell Biol. 1999, 19, 3748-3759.
67. Fliss, A. E.; Benzeno, S.; Rao, J.; Caplan, A. J. Control of Estrogen Receptor Ligand Binding by Hsp90. J. Steroid Biochem. Mol. Biol. 2000, 72, 223-230.
68. Isaacs, J. S.; Xu, W.; Neckers, L. Heat Shock Protein 90 as a Molecular Target for Cancer Therapeutics. Cancer Cell 2003, 3, 213-217.
69. Uehara, Y. Natural Product Origins of Hsp90 Inhibitors. Curr. Cancer Drug Targets 2003, 3, 325-330.
70. Chiosis, G.; Vilenchik, M.; Kim, J.; Solit, D. Hsp90: the Vulnerable Chaperone. Drug Discov. Today 2004, 9, 881-888.
71. Bagatell, R.; Khan, O.; Paine-Murrieta, G.; Taylor, C. W.; Akinaga, S.; Whitesell, L. Destabilization of Steroid Receptors by Heat Shock Protein 90-Binding Drugs: a Ligand-Independent Approach to Hormonal Therapy of Breast Cancer. Clin. Cancer Res. 2001, 7, 2076-2084.
72. Beliakoff, J.; Bagatell, R.; Paine-Murrieta, G.; Taylor, C. W.; Lykkesfeldt, A. E.; Whitesell, L. Hormone-Refractory Breast Cancer Remains Sensitive to the Antitumor Activity of Heat Shock Protein 90 Inhibitors. Clin. Cancer Res. 2003, 9, 4961-4971.
73. Lee, M. O.; Kim, E. O.; Kwon, H. J.; Kim, Y. M.; Kang, H. J.; Kang, H.; Lee, J. E. Radicicol Represses the Transcriptional Function of the Estrogen Receptor by Suppressing the Stabilization of the Receptor by Heat Shock Protein 90. Mol. Cell Endocrinol. 2002, 188, 47-54.
74. Gougelet, A.; Bouclier, C.; Marsaud, V.; Maillard, S.; Mueller, S. O.; Korach, K. S.; Renoir, J. M. Estrogen Receptor Alpha and Beta Subtype Expression and Transactivation Capacity Are Differentially Affected by Receptor-, Hsp90- and Immunophilin-Ligands in Human Breast Cancer Cell. J. Steroid. Biochem. Mol. Biol. 2005, in press.
75. Nonclercq, D.; Journe, F.; Body, J. J.; Leclercq, G.; Laurent, G. Ligand-Independent and Agonist-Mediated Degradation of Estrogen Receptor-Alpha in Breast Carcinoma Cells: Evidence for Distinct Degradative Pathways. Mol. Cell Endocrinol. 2004, 227, 53-65.
76. Czar, M. J.; Galigniana, M. D.; Silverstein, A. M.; Pratt, W. B. Geldanamycin, a Heat Shock Protein 90-Binding Benzoquinone Ansamycin, Inhibits Steroid-Dependent Translocation of the Glucocorticoid Receptor From the Cytoplasm to the Nucleus. Biochemistry 1997, 36, 7776-7785.
77. Kawata, M.; Matsuda, K.; Nishi, M.; Ogawa, H.; Ochiai, I. Intracellular Dynamics of Steroid Hormone Receptor. Neurosci. Res. 2001, 40, 197-203.
78. Marino, M.; Acconcia, F.; Trentalance, A. Biphasic Estradiol-Induced AKT Phosphorylation Is Modulated by PTEN Via MAP Kinase in HepG2 Cells. Mol. Biol. Cell 2003, 14, 2583-2591.
79. Boyan, B. D.; Sylvia, V. L.; Frambach, T.; Lohmann, C. H.; Dietl, J.; Dean, D. D.; Schwartz, Z. Estrogen-Dependent Rapid Activation of Protein Kinase C in Estrogen Receptor-Positive MCF-7 Breast Cancer Cells and Estrogen Receptor-Negative HCC38 Cells Is Membrane-Mediated and Inhibited by Tamoxifen. Endocrinology 2003, 144, 1812-1824.
80. Razandi, M.; Pedram, A.; Park, S. T.; Levin, E. R. Proximal Events in Signaling by Plasma Membrane Estrogen Receptors. J. Biol. Chem. 2003, 278, 2701-2712.
81. Razandi, M.; Pedram, A.; Merchenthaler, I.; Greene, G. L.; Levin, E. R. Plasma Membrane Estrogen Receptors Exist and Functions As Dimers. Mol. Endocrinol. 2004, 18, 2854-2865.
82. Thomas, P.; Pang, Y.; Filardo, E. J.; Dong, J. Identity of an Estrogen Membrane Receptor Coupled to a G Protein in Human Breast Cancer Cells. Endocrinology 2005, 146, 624-632.
83. Razandi, M.; Oh, P.; Pedram, A.; Schnitzer, J.; Levin, E. R. ERs Associate With and Regulate the Production of Caveolin: Implications for Signaling and Cellular Actions. Mol. Endocrinol. 2002, 16, 100-115.
84. Razandi, M.; Alton, G.; Pedram, A.; Ghonshani, S.; Webb, P.; Levin, E. R. Identification of a Structural Determinant Necessary for the Localization and Function of Estrogen Receptor Alpha at the Plasma Membrane. Mol. Cell Biol. 2003, 23, 1633-1646.
85. Acconcia, F.; Ascenzi, P.; Fabozzi, G.; Visca, P.; Marino, M. S-Palmitoylation Modulates Human Estrogen Receptor-Alpha Functions. Biochem. Biophys. Res. Commun. 2004, 316, 878-883.
86. Acconcia, F.; Ascenzi, P.; Bocedi, A.; Spisni, E.; Tomasi, V.; Trentalance, A.; Visca, P.; Marino, M. Palmitoylation-Dependent Estrogen Receptor Alpha Membrane Localization: Regulation by 17beta-Estradiol. Mol. Biol. Cell 2005, 16, 231-237.
87. Song, R. X.; Barnes, C. J.; Zhang, Z.; Bao, Y.; Kumar, R.; Santen, R. J. The Role of Shc and Insulin-Like Growth Factor 1 Receptor in Mediating the Translocation of Estrogen Receptor Alpha to the Plasma Membrane. Proc. Natl. Acad. Sci. USA 2004, 101, 2076-2081.
88. Little, M.; Szendro, P. I.; Jungblut, P. W. Hormone-Mediated Dimerization of Microsomal Estradiol Receptor. Hoppe Seylers. Z. Physiol. Chem. 1973, 354, 1599-1610.
89. Watson, G. H.; Muldoon, T. G. Specific Binding of Estrogen and Estrogen-Receptor Complex by Microsomes From Estrogen-Responsive Tissues of the Rat. Endocrinology 1985, 117, 1341-1349.
90. Zhou, Y.; Chorich, L. P.; Mahesh, V. B.; Ogle, T. F. Regulation of Estrogen Receptor Protein and Messenger Ribonucleic Acid by Estradiol and Progesterone in Rat Uterus. J. Steroid Biochem. Mol. Biol. 1993, 46, 687-698.
91. DeFranco, D. B.; Ramakrishnan, C.; Tang, Y. Molecular Chaperones and Subcellular Trafficking of Steroid Receptors. J. Steroid Biochem. Mol. Biol. 1998, 65, 51-58.
92. Savory, J. G.; Hsu, B.; Laquian, I. R.; Giffin, W.; Reich, T.; Hache, R. J.; Lefebvre, Y. A. Discrimination Between NL1- and NL2-Mediated Nuclear Localization of the Glucocorticoid Receptor. Mol. Cell Biol. 1999, 19, 1025-1037.
93. Ozanne, D. M.; Brady, M. E.; Cook, S.; Gaughan, L.; Neal, D. E.; Robson, C. N. Androgen Receptor Nuclear Translocation Is Facilitated by the F-Actin Cross-Linking Protein Filamin. Mol. Endocrinol. 2000, 14, 1618-1626.
94. Dauvois, S.; White, R.; Parker, M. G. The Antiestrogen ICI 182780 Disrupts Estrogen Receptor Nucleocytoplasmic Shuttling. J. Cell Sci. 1993, 106, 1377-1388.
95. Devin-Leclerc, J.; Meng, X.; Delahaye, F.; Leclerc, P.; Baulieu, E. E.; Catelli, M. G. 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. 1998, 12, 842-854.
96. Pratt, W. B.; Galigniana, M. D.; Harrell, J. M.; DeFranco, D. B. Role of Hsp90 and the Hsp90-Binding Immunophilins in Signalling Protein Movement. Cell Signal. 2004, 16, 857-872.
97. Mallik, R.; Gross, S. P. Molecular Motors: Strategies to Get Along. Curr. Biol. 2004, 14, R971-R982.
98. Harrell, J. M.; Murphy, P. J.; Morishima, Y.; Chen, H.; Mansfield, J. F.; Galigniana, M. D.; Pratt, W. B. Evidence for Glucocorticoid Receptor Transport on Microtubules by Dynein. J. Biol. Chem. 2004, 279, 54647-54654.
99. Pemberton, L. F.; Paschal, B. M. Mechanisms of Receptor-Mediated Nuclear Import and Nuclear Export. Traffic 2005, 6, 187-198.
100. Macara, I. G. Transport into and Out of the Nucleus. Microbiol. Mol. Biol. Rev. 2001, 65, 570-594.
101. Kau, T. R.; Silver, P. A. Nuclear Transport As a Target for Cell Growth. Drug Discov. Today 2003, 8, 78-85.
102. Liu, J.; DeFranco, D. B. Protracted Nuclear Export of Glucocorticoid Receptor Limits Its Turnover and Does Not Require the Exportin 1/CRM1-Directed Nuclear Export Pathway. Mol. Endocrinol. 2000, 14, 40-51.
103. Itoh, M.; Adachi, M.; Yasui, H.; Takekawa, M.; Tanaka, H.; Imai, K. Nuclear Export of Glucocorticoid Receptor Is Enhanced by C-Jun N-Terminal Kinase-Mediated Phosphorylation. Mol. Endocrinol. 2002, 16, 2382-2392.
104. Black, B. E.; Holaska, J. M.; Rastinejad, F.; Paschal, B. M. DNA Binding Domains in Diverse Nuclear Receptors Function As Nuclear Export Signals. Curr. Biol. 2001, 11, 1749-1758.
105. Holaska, J. M.; Black, B. E.; Rastinejad, F.; Paschal, B. M. Ca2+-Dependent Nuclear Export Mediated by Calreticulin. Mol. Cell Biol. 2002, 22, 6286-6297.
106. Rossini, G. P. The Quaternary Structures of Untransformed Steroid Hormone Receptors: an Open Issue. J. Theor. Biol. 1994, 166, 339-353.
107. Krust, A.; Green, S.; Argos, P.; Kumar, V.; Walter, P.; Bornert, J. M.; Chambon, P. The Chicken Oestrogen Receptor Sequence: Homology With V-ErbA and the Human Oestrogen and Glucocorticoid Receptors. EMBO J. 1986, 5, 891-897.
108. Schwartz, J. A.; Zhong, L.; Deighton-Collins, S.; Zhao, C.; Skafar, D. F. Mutations Targeted to a Predicted Helix in the Extreme Carboxyl-Terminal Region of the Human Estrogen Receptor-Alpha Alter Its Response to Estradiol and 4-Hydroxytamoxifen. J. Biol. Chem. 2002, 277, 13202-13209.
109. Wang, Y.; Cheng, C. H. ERalpha and STAT5a Cross-Talk: Interaction Through C-Terminal Portions of the Proteins Decreases STAT5a Phosphorylation, Nuclear Translocation and DNA-Binding. FEBS Lett. 2004, 572, 238-244.
110. Peters, G. A.; Khan, S. A. Estrogen Receptor Domains E and F: Role in Dimerization and Interaction With Coactivator RIP-140. Mol. Endocrinol. 1999, 13, 286-296.
111. Auricchio, F. Phosphorylation of Steroid Receptors. J. Steroid Biochem. 1989, 32, 613-622.
112. Le Goff, P.; Montano, M. M.; Schodin, D. J.; Katzenellenbogen, B. S. Phosphorylation of the Human Estrogen Receptor. Identification of Hormone-Regulated Sites and Examination of Their Influence on Transcriptional Activity. J. Biol. Chem. 1994, 269, 4458-4466.
113. Arnold, S. F.; Obourn, J. D.; Jaffe, H.; Notides, A. C. Phosphorylation of the Human Estrogen Receptor by Mitogen-Activated Protein Kinase and Casein Kinase II: Consequence on DNA Binding. J. Steroid Biochem. Mol. Biol. 1995, 55, 163-172.
114. Ali, S.; Metzger, D.; Bornert, J. M.; Chambon, P. Modulation of Transcriptional Activation by Ligand-Dependent Phosphorylation of the Human Oestrogen Receptor A/B Region. EMBO J. 1993, 12, 1153-1160.
115. Wang, C.; Fu, M.; Angeletti, R. H.; Siconolfi-Baez, L.; Reutens, A. T.; Albanese, C.; Lisanti, M. P.; Katzenellenbogen, B. S.; Kato, S.; Hopp, T.; Fuqua, S. A.; Lopez, G. N.; Kushner, P. J.; Pestell, R. G. Direct Acetylation of the Estrogen Receptor Alpha Hinge Region by P300 Regulates Transactivation and Hormone Sensitivity. J. Biol. Chem. 2001, 276, 18375-18383.
116. Kushner, P. J.; Agard, D. A.; Greene, G. L.; Scanlan, T. S.; Shiau, A. K.; Uht, R. M.; Webb, P. Estrogen Receptor Pathways to AP-1. J. Steroid Biochem. Mol. Biol. 2000, 74, 311-317.
117. Paech, K.; Webb, P.; Kuiper, G. G.; Nilsson, S.; Gustafsson, J.; Kushner, P. J.; Scanlan, T. S. Differential Ligand Activation of Estrogen Receptors ERalpha and ERbeta at AP1 Sites. Science 1997, 277, 1508-1510.
118. Kingston, R. E.; Narlikar, G. J. ATP-Dependent Remodeling and Acetylation As Regulators of Chromatin Fluidity. Genes Dev. 1999, 13, 2339-2352.
119. Eberharter, A.; Becker, P. B. Histone Acetylation: a Switch Between Repressive and Permissive Chromatin. Second in Review Series on Chromatin Dynamics. EMBO Rep. 2002, 3, 224-229.
120. McKenna, N. J.; O'Malley, B. W. Minireview: Nuclear Receptor Coactivators - an Update. Endocrinology 2002, 143, 2461-2465.
121. Xu, J.; Li, Q. Review of the in vivo Functions of the P160 Steroid Receptor Coactivator Family. Mol. Endocrinol. 2003, 17, 1681-1692.
122. Reid, G.; Hubner, M. R.; Metivier, R.; Brand, H.; Denger, S.; Manu, D.; Beaudouin, J.; Ellenberg, J.; Gannon, F. Cyclic, Proteasome-Mediated Turnover of Unliganded and Liganded ERalpha on Responsive Promoters Is an Integral Feature of Estrogen Signaling. Mol. Cell 2003, 11, 695-707.
123. Metivier, R.; Penot, G.; Hubner, M. R.; Reid, G.; Brand, H.; Kos, M.; Gannon, F. Estrogen Receptor-Alpha Directs Ordered, Cyclical, and Combinatorial Recruitment of Cofactors on a Natural Target Promoter. Cell 2003, 115, 751-763.
124. Dobrzycka, K. M.; Townson, S. M.; Jiang, S.; Oesterreich, S. Estrogen Receptor Corepressors - a Role in Human Breast Cancer? Endocr. Relat. Cancer 2003, 10, 517-536.
125. de Ruijter, A. J.; van Gennip, A. H.; Caron, H. N.; Kemp, S.; van Kuilenburg, A. B. Histone Deacetylases (HDACs): Characterization of the Classical HDAC Family. Biochem. J. 2003, 370, 737-749.
126. Power, R. F.; Mani, S. K.; Codina, J.; Conneely, O. M.; O'Malley, B. W. Dopaminergic and Ligand-Independent Activation of Steroid Hormone Receptors. Science 1991, 254, 1636-1639.
127. Ignar-Trowbridge, D. M.; Pimentel, M.; Parker, M. G.; McLachlan, J. A.; Korach, K. S. 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.
128. Aronica, S. M.; Katzenellenbogen, B. S. Progesterone Receptor Regulation in Uterine Cells: Stimulation by Estrogen, Cyclic Adenosine 3',5'-Monophosphate, and Insulin-Like Growth Factor I and Suppression by Antiestrogens and Protein Kinase Inhibitors. Endocrinology 1991, 128, 2045-2052.
129. Cho, H.; Katzenellenbogen, B. S. Synergistic Activation of Estrogen Receptor-Mediated Transcription by Estradiol and Protein Kinase Activators. Mol. Endocrinol. 1993, 7, 441-452.
130. Ince, B. A.; Montano, M. M.; Katzenellenbogen, B. S. Activation of Transcriptionally Inactive Human Estrogen Receptors by Cyclic Adenosine 3',5'-Monophosphate and Ligands Including Antiestrogens. Mol. Endocrinol. 1994, 8, 1397-1406.
131. Chen, D.; Washbrook, E.; Sarwar, N.; Bates, G. J.; Pace, P. E.; Thirunuvakkarasu, V.; Taylor, J.; Epstein, R. J.; Fuller-Pace, F. V.; Egly, J. M.; Coombes, R. C.; Ali, S. Phosphorylation of Human Estrogen Receptor Alpha at Serine 118 by Two Distinct Signal Transduction Pathways Revealed by Phosphorylation-Specific Antisera. Oncogene 2002, 21, 4921-4931.
132. Hall, J. M.; Couse, J. F.; Korach, K. S. The Multifaceted Mechanisms of Estradiol and Estrogen Receptor Signaling. J. Biol. Chem. 2001, 276, 36869-36872.
133. Toran-Allerand, C. D. Minireview: A Plethora of Estrogen Receptors in the Brain: Where Will It End? Endocrinology 2004, 145, 1069-1074.
134. Seo, H. S.; Leclercq, G. Evaluation of Potential Implication of Membrane Estrogen Binding Sites on ERE-Dependent Transcriptional Activity and Intracellular Estrogen Receptor-Alpha Regulation in MCF-7 Breast Cancer Cells. J. Steroid Biochem. Mol. Biol. 2002, 80, 109-123.
135. Hershko, A.; Ciechanover, A. The Ubiquitin System. Ann. Rev. Biochem. 1998, 67, 425-479.
136. Deshaies, R. J. SCF and Cullin/Ring H2-Based Ubiquitin Ligases. Ann. Rev. Cell Dev. Biol. 1999, 15, 435-467.
137. Imhof, M. O.; McDonnell, D. P. Yeast RSP5 and Its Human Homolog HRPF1 Potentiate Hormone-Dependent Activation of Transcription by Human Progesterone and Glucocorticoid Receptors. Mol. Cell Biol. 1996, 16, 2594-2605.
138. Nawaz, Z.; Lonard, D. M.; Smith, C. L.; Lev-Lehman, E.; Tsai, S. Y.; Tsai, M. J.; O'Malley, B. W. The Angelman Syndrome-Associated Protein, E6-AP, Is a Coactivator for the Nuclear Hormone Receptor Superfamily. Mol. Cell Biol. 1999, 19, 1182-1189.
139. Yan, F.; Gao, X.; Lonard, D. M.; Nawaz, Z. Specific Ubiquitin-Conjugating Enzymes Promote Degradation of Specific Nuclear Receptor Coactivators. Mol. Endocrinol. 2003, 17, 1315-1331.
140. Shang, Y.; Hu, X.; DiRenzo, J.; Lazar, M. A.; Brown, M. Cofactor Dynamics and Sufficiency in Estrogen Receptor-Regulated Transcription. Cell 2000, 103, 843-852.
141. van Hoorn, W. P. Identification of a Second Binding Site in the Estrogen Receptor. J. Med. Chem. 2002, 45, 584-589.
142. Norman, A. W.; Mizwicki, M. T.; Norman, D. P. Steroid-Hormone Rapid Actions, Membrane Receptors and a Conformational Ensemble Model. Nat. Rev. Drug Discov. 2004, 3, 27-41.
143. Mizwicki, M. T.; Keidel, D.; Bula, C. M.; Bishop, J. E.; Zanello, L. P.; Wurtz, J. M.; Moras, D.; Norman, A. W. Identification of an Alternative Ligand-Binding Pocket in the Nuclear Vitamin D Receptor and Its Functional Importance in 1alpha,25(OH)2-Vitamin D3 Signaling. Proc. Natl. Acad. Sci. USA 2004, 101, 12876-12881.
144. Tanenbaum, D. M.; Wang, Y.; Williams, S. P.; Sigler, P. B. Crystallographic Comparison of the Estrogen and Progesterone Receptor's Ligand Binding Domains. Proc. Natl. Acad. Sci. USA 1998, 95, 5998-6003.
145. Tanenbaum, D. M.; Wang, Y.; Williams, S. P.; Sigler, P. B. Crystallographic Comparison of the Estrogen and Progesterone Receptor's Ligand Binding Domains. Proc. Natl. Acad. Sci. USA 1998, 95, 5998-6003.
146. Bentrem, D.; Fox, J. E.; Pearce, S. T.; Liu, H.; Pappas, S.; Kupfer, D.; Zapf, J. W.; Jordan, V. C. Distinct Molecular Conformations of the Estrogen Receptor Alpha Complex Exploited by Environmental Estrogens. Cancer Res. 2003, 63, 7490-7496.
147. Iannone, M. A.; Simmons, C. A.; Kadwell, S. H.; Svoboda, D. L.; Vanderwall, D. E.; Deng, S. J.; Consler, T. G.; Shearin, J.; Gray, J. G.; Pearce, K. H. Correlation Between in vitro Peptide Binding Profiles and Cellular Activities for Estrogen Receptor-Modulating Compounds. Mol. Endocrinol. 2004, 18, 1064-1081.
148. MacGregor, S. J.; Liu, H.; Bentrem, D. J.; Zapf, J. W.; Jordan, V. C. 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. 2000, 60, 5097-5105.
149. Liu, H.; Lee, E. S.; Deb Los, R. A.; Zapf, J. W.; Jordan, V. C. Silencing and Reactivation of the Selective Estrogen Receptor Modulator-Estrogen Receptor Alpha Complex. Cancer Res. 2001, 61, 3632-3639.
150. Liu, H.; Park, W. C.; Bentrem, D. J.; McKian, K. P.; Reyes, A. L.; Loweth, J. A.; Schafer, J. M.; Zapf, J. W.; Jordan, V. C. Structure-Function Relationships of the Raloxifene-Estrogen Receptor-Alpha Complex for Regulating Transforming Growth Factor-Alpha Expression in Breast Cancer Cells. J. Biol. Chem. 2002, 277, 9189-9198.
151. Gust, R.; Keilitz, R.; Schmidt, K. Investigations of New Lead Structures for the Design of Selective Estrogen Receptor Modulators. J. Med. Chem. 2001, 44, 1963-1970.
152. Paige, L. A.; Christensen, D. J.; Gron, H.; Norris, J. D.; Gottlin, E. B.; Padilla, K. M.; Chang, C. Y.; Ballas, L. M.; Hamilton, P. T.; McDonnell, D. P.; Fowlkes, D. M. Estrogen Receptor (ER) Modulators Each Induce Distinct Conformational Changes in ER Alpha and ER Beta. Proc. Natl. Acad. Sci. USA 1999, 96, 3999-4004.
153. Norris, J. D.; Paige, L. A.; Christensen, D. J.; Chang, C. Y.; Huacani, M. R.; Fan, D.; Hamilton, P. T.; Fowlkes, D. M.; McDonnell, D. P. Peptide Antagonists of the Human Estrogen Receptor. Science 1999, 285, 744-746.
154. Bapat, A. R.; Frail, D. E. Full-Length Estrogen Receptor Alpha and Its Ligand-Binding Domain Adopt Different Conformations Upon Binding Ligand. J. Steroid Biochem. Mol. Biol. 2003, 86, 143-149.
155. McDonnell, D. P.; Clemm, D. L.; Hermann, T.; Goldman, M. E.; Pike, J. W. Analysis of Estrogen Receptor Function in vitro Reveals Three Distinct Classes of Antiestrogens. Mol. Endocrinol. 1995, 9, 659-669.
156. Luck, L. A.; Barse, J. L.; Luck, A. M.; Peck, C. H. Conformational Changes in the Human Estrogen Receptor Observed by (19)F NMR. Biochem. Biophys. Res. Commun. 2000, 270, 988-991.
157. Hurth, K. M.; Nilges, M. J.; Carlson, K. E.; Tamrazi, A.; Belford, R. L.; Katzenellenbogen, J. A. Ligand-Induced Changes in Estrogen Receptor Conformation As Measured by Site-Directed Spin Labeling. Biochemistry 2004, 43, 1891-1907.
158. Fawell, S. E.; White, R.; Hoare, S.; Sydenham, M.; Page, M.; Parker, M. G. Inhibition of Estrogen Receptor-DNA Binding by the "Pure" Antiestrogen ICI 164,384 Appears to Be Mediated by Impaired Receptor Dimerization. Proc. Natl. Acad. Sci. USA 1990, 87, 6883-6887.
159. Leclercq, G. Molecular Forms of the Estrogen Receptor in Breast Cancer. J. Steroid Biochem. Mol. Biol. 2002, 80, 259-272.
160. Horigome, T.; Ogata, F.; Golding, T. S.; Korach, K. S. Estradiol-Stimulated Proteolytic Cleavage of the Estrogen Receptor in Mouse Uterus. Endocrinology 1988, 123, 2540-2548.
161. Trivedi, S.; Piccart, M.; Muquardt, C.; Gilot, N.; Hadiy, S.; Patel, D.; Leclercq, G. Tamoxifen Aziridine Labeling of the Estrogen Receptor-Potential Utility in Detecting Biologically Aggressive Breast Tumors. Breast Cancer Res. Treat. 1996, 40, 231-241.
162. Piccart, M. J.; Trivedi, S.; Maaroufi, Y.; Debbaudt, A.; Veenstra, S.; Leclercq, G. Evolution Towards Hormone Independence of the MXT Mouse Mammary Tumor Is Associated With a Gradual Change in Its Estrogen Receptor Molecular Polymorphism. Cancer Biochem. Biophys. 1998, 16, 169-182.
163. Leclercq, G.; Heuson, J. C.; Deboel, M. C.; Mattheiem, W. H. Oestrogen Receptors in Breast Cancer: a Changing Concept. Br. Med. J. 1975, 1, 185-189.
164. Leclercq, G.; Bojar, H.; Goussard, J.; Nicholson, R. I.; Pichon, M. F.; Piffanelli, A.; Pousette, A.; Thorpe, S.; Lonsdorfer, M. Abbott Monoclonal Enzyme Immunoassay Measurement of Estrogen Receptors in Human Breast Cancer: a European Multicenter Study. Cancer Res. 1986, 46, 4233s-4236s.
165. Heuson, J. C.; Longeval, E.; Mattheiem, W. H.; Deboel, M. C.; Sylvester, R. J.; Leclercq, G. Significance of Quantitative Assessment of Estrogen Receptors for Endocrine Therapy in Advanced Breast Cancer. Cancer 1977, 39, 1971-1977.
166. Lacroix, M.; Querton, G.; Hennebert, P.; Larsimont, D.; Leclercq, G. Estrogen Receptor Analysis in Primary Breast Tumors by Ligand-Binding Assay, Immunocytochemical Assay, and Northern Blot: a Comparison. Breast Cancer Res. Treat. 2001, 67, 263-271.
167. Lacroix, M.; Leclercq, G. Relevance of Breast Cancer Cell Lines As Models for Breast Tumours: an Update. Breast Cancer Res. Treat. 2004, 83, 249-289.
168. Lacroix, M.; Toillon, R. A.; Leclercq, G. Stable 'Portrait' of Breast Tumors During Progression: Data From Biology, Pathology and Genetics. Endocr. Relat. Cancer 2004, 11, 497-522.
169. McPherson, L. A.; Baichwal, V. R.; Weigel, R. J. Identification of ERF-1 As a Member of the AP2 Transcription Factor Family. Proc. Natl. Acad. Sci. USA 1997, 94, 4342-4347.
170. McPherson, L. A.; Weigel, R. J. AP2alpha and AP2gamma: a Comparison of Binding Site Specificity and Trans-Activation of the Estrogen Receptor Promoter and Single Site Promoter Constructs. Nucl. Acids Res. 1999, 27, 4040-4049.
171. Schuur, E. R.; McPherson, L. A.; Yang, G. P.; Weigel, R. J. Genomic Structure of the Promoters of the Human Estrogen Receptor-Alpha Gene Demonstrate Changes in Chromatin Structure Induced by AP2gamma. J. Biol. Chem. 2001, 276, 15519-15526.
172. deGraffenried, L. A.; Hilsenbeck, S. G.; Fuqua, S. A. Sp1 Is Essential for Estrogen Receptor Alpha Gene Transcription. J. Steroid Biochem. Mol. Biol. 2002, 82, 7-18.
173. deGraffenried, L. A.; Hopp, T. A.; Valente, A. J.; Clark, R. A.; Fuqua, S. A. Regulation of the Estrogen Receptor Alpha Minimal Promoter by Sp1, USF-1 and ERalpha. Breast Cancer Res. Treat. 2004, 85, 111-120.
174. Saceda, M.; Lindsey, R. K.; Solomon, H.; Angeloni, S. V.; Martin, M. B. Estradiol Regulates Estrogen Receptor mRNA Stability. J. Steroid Biochem. Mol. Biol. 1998, 66, 113-120.
175. Flouriot, G.; Pakdel, F.; Valotaire, Y. Transcriptional and Post-Transcriptional Regulation of Rainbow Trout Estrogen Receptor and Vitellogenin Gene Expression. Mol. Cell Endocrinol. 1996, 124, 173-183.
176. Mitchell, D. C.; Ing, N. H. Estradiol Stabilizes Estrogen Receptor Messenger Ribonucleic Acid in Sheep Endometrium Via Discrete Sequence Elements in Its 3′-Untranslated Region. Mol. Endocrinol. 2003, 17, 562-574.
177. Farnell, Y. Z.; Ing, N. H. The Effects of Estradiol and Selective Estrogen Receptor Modulators on Gene Expression and Messenger RNA Stability in Immortalized Sheep Endometrial Stromal Cells and Human Endometrial Adenocarcinoma Cells. J. Steroid Biochem. Mol. Biol. 2003, 84, 453-461.
178. Pentecost, B. T.; Song, R.; Luo, M.; DePasquale, J. A.; Fasco, M. J. Upstream Regions of the Estrogen Receptor Alpha Proximal Promoter Transcript Regulate ER Protein Expression Through a Translational Mechanism. Mol. Cell Endocrinol. 2005, 229, 83-94.
179. Roodi, N.; Bailey, L. R.; Kao, W. Y.; Verrier, C. S.; Yee, C. J.; Dupont, W. D.; Parl, F. F. Estrogen Receptor Gene Analysis in Estrogen Receptor-Positive and Receptor-Negative Primary Breast Cancer. J. Natl. Cancer Inst. 1995, 87, 446-451.
180. Koh, E. H.; Ro, J.; Wildrick, D. M.; Hortobagyi, G. N.; Blick, M. Analysis of the Estrogen Receptor Gene Structure in Human Breast Cancer. Anticancer Res. 1989, 9, 1841-1845.
181. Parl, F. F.; Cavener, D. R.; Dupont, W. D. Genomic DNA Analysis of the Estrogen Receptor Gene in Breast Cancer. Breast Cancer Res. Treat. 1989, 14, 57-64.
182. Read, L. D.; Greene, G. L.; Katzenellenbogen, B. S. Regulation of Estrogen Receptor Messenger Ribonucleic Acid and Protein Levels in Human Breast Cancer Cell Lines by Sex Steroid Hormones, Their Antagonists, and Growth Factors. Mol. Endocrinol. 1989, 3, 295-304.
183. Journe, F.; Body, J. J.; Leclercq, G.; Nonclercq, D.; Laurent, G. Estrogen Responsiveness of IBEP-2, a New Human Cell Line Derived From Breast Carcinoma. Breast Cancer Res. Treat. 2004, 86, 39-53.
184. Levenson, A. S.; Jordan, V. C. MCF-7: the First Hormone-Responsive Breast Cancer Cell Line. Cancer Res. 1997, 57, 3071-3078.
185. Alarid, E. T.; Bakopoulos, N.; Solodin, N. Proteasome-Mediated Proteolysis of Estrogen Receptor: a Novel Component in Autologous Down-Regulation. Mol. Endocrinol. 1999, 13, 1522-1534.
186. El Khissiin, A.; Leclercq, G. Implication of Proteasome in Estrogen Receptor Degradation. FEBS Lett. 1999, 448, 160-166.
187. Nawaz, Z.; Lonard, D. M.; Dennis, A. P.; Smith, C. L.; O'Malley, B. W. Proteasome-Dependent Degradation of the Human Estrogen Receptor. Proc. Natl. Acad. Sci. USA 1999, 96, 1858-1862.
188. Laios, I.; Journé, F.; Nonclercq, D.; Salazar Vidal, D.; Toillon, R. A.; Laurent, G.; Leclercq, G. Role of the Proteasome in the Regulation of Estrogen Receptor Alpha Turnover and Function in MCF-7 Breast Carcinoma Cells. J. Steroid Biochem. Mol. Biol. 2005, 94, 347-359.
189. Wijayaratne, A. L.; McDonnell, D. P. 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. 2001, 276, 35684-35692.
190. Fan, M.; Bigsby, R. M.; Nephew, K. P. The NEDD8 Pathway Is Required for Proteasome-Mediated Degradation of Human Estrogen Receptor (ER)-Alpha and Essential for the Antiproliferative Activity of ICI 182,780 in ERalpha-Positive Breast Cancer Cells. Mol. Endocrinol. 2003, 17, 356-365.
191. Seo, H. S.; Journe, F.; Larsimont, D.; Sotiriou, C.; Leclercq, G. Decrease of Estrogen Receptor Expression and Associated ERE-Dependent Transcription in MCF-7 Breast Cancer Cells After Oligomycin Treatment. Steroids 2003, 68, 257-269.
192. Seo, H. S.; Larsimont, D.; Querton, G.; El Khissiin, A.; Laios, I.; Legros, N.; Leclercq, G. Estrogenic and Anti-Estrogenic Regulation of Estrogen Receptor in MCF-7 Breast-Cancer Cells: Comparison of Immunocytochemical Data With Biochemical Measurements. Int. J. Cancer 1998, 78, 760-765.
193. Saceda, M.; Lippman, M. E.; Chambon, P.; Lindsey, R. L.; Ponglikitmongkol, M.; Puente, M.; Martin, M. B. Regulation of the Estrogen Receptor in MCF-7 Cells by Estradiol. Mol. Endocrinol. 1988, 2, 1157-1162.
194. Berthois, Y.; Dong, X. F.; Roux-Dossetto, M.; Martin, P. M. Expression of Estrogen Receptor and Its Messenger Ribonucleic Acid in the MCF-7 Cell Line: Multiparametric Analysis of Its Processing and Regulation by Estrogen. Mol. Cell Endocrinol. 1990, 74, 11-20.
195. Borras, M.; Hardy, L.; Lempereur, F.; el Khissiin, A. H.; Legros, N.; Gol-Winkler, R.; Leclercq, G. Estradiol-Induced Down-Regulation of Estrogen Receptor. Effect of Various Modulators of Protein Synthesis and Expression. J. Steroid Biochem. Mol. Biol. 1994, 48, 325-336.
196. Jin, L.; Borras, M.; Lacroix, M.; Legros, N.; Leclercq, G. Antiestrogenic Activity of Two 11 Beta-Estradiol Derivatives on MCF-7 Breast Cancer Cells. Steroids 1995, 60, 512-518.
197. Pink, J. J.; Jordan, V. C. Models of Estrogen Receptor Regulation by Estrogens and Antiestrogens in Breast Cancer Cell Lines. Cancer Res. 1996, 56, 2321-2330.
198. Kiang, D. T.; Kollander, R. E.; Thomas, T.; Kennedy, B. J. Up-Regulation of Estrogen Receptors by Nonsteroidal Antiestrogens in Human Breast Cancer. Cancer Res. 1989, 49, 5312-5316.
199. Laios, I.; Journe, F.; Laurent, G.; Nonclercq, D.; Toillon, R. A.; Seo, H. S.; Leclercq, G. Mechanisms Governing the Accumulation of Estrogen Receptor Alpha in MCF-7 Breast Cancer Cells Treated With Hydroxytamoxifen and Related Antiestrogens. J. Steroid Biochem. Mol. Biol. 2003, 87, 207-221.
200. Pearce, S. T.; Liu, H.; Jordan, V. C. Modulation of Estrogen Receptor Alpha Function and Stability by Tamoxifen and a Critical Amino Acid (Asp-538) in Helix 12. J. Biol. Chem. 2003, 278, 7630-7638.
201. Gyling, M.; Leclercq, G. Estrogen and Antiestrogen Interaction With Estrogen Receptor of MCF-7 Cells - Relationship Between Processing and Estrogenicity. J. Steroid Biochem. 1988, 29, 1-8.
202. Seo, H. S.; Larsimont, D.; Ma, Y.; Laios, I.; Leclercq, G. Regulation of Estrogen Receptor Levels by Ligand-Induced Release of Compound(s) in MCF-7 Cells. Mol. Cell Endocrinol. 2000, 164, 19-29.
203. Marsaud, V.; Gougelet, A.; Maillard, S.; Renoir, J. M. Various Phosphorylation Pathways, Depending on Agonist and Antagonist Binding to Endogenous Estrogen Receptor Alpha (ERalpha), Differentially Affect ERalpha Extractability, Proteasome-Mediated Stability, and Transcriptional Activity in Human Breast Cancer Cells. Mol. Endocrinol. 2003, 17, 2013-2027.
204. Borras, M.; Laios, I.; El Khissiin, A.; Seo, H. S.; Lempereur, F.; Legros, N.; Leclercq, G. Estrogenic and Antiestrogenic Regulation of the Half-Life of Covalently Labeled Estrogen Receptor in MCF-7 Breast Cancer Cells. J. Steroid Biochem. Mol. Biol. 1996, 57, 203-213.
205. Awais, M.; Sato, M.; Sasaki, K.; Umezawa, Y. A Genetically Encoded Fluorescent Indicator Capable of Discriminating Estrogen Agonists From Antagonists in Living Cells. Anal. Chem. 2004, 76, 2181-2186.
206. Ozers, M. S.; Ervin, K. M.; Steffen, C. L.; Fronczak, J. A.; Lebakken, C. S.; Carnahan, K. A.; Lowery, R. G.; Burke, T. J. Analysis of Ligand-Dependent Recruitment of Coactivator Peptides to Estrogen Receptor Using Fluorescence Polarization. Mol. Endocrinol. 2005, 19, 25-34.
207. Rodriguez, A. L.; Tamrazi, A.; Collins, M. L.; Katzenellenbogen, J. A. Design, Synthesis, and in vitro Biological Evaluation of Small Molecule Inhibitors of Estrogen Receptor Alpha Coactivator Binding. J. Med. Chem. 2004, 47, 600-611.
208. Geistlinger, T. R.; McReynolds, A. C.; Guy, R. K. Ligand-Selective Inhibition of the Interaction of Steroid Receptor Coactivators and Estrogen Receptor Isoforms. Chem. Biol. 2004, 11, 273-281.
209. Shao, D.; Berrodin, T. J.; Manas, E.; Hauze, D.; Powers, R.; Bapat, A.; Gonder, D.; Winneker, R. C.; Frail, D. E. Identification of Novel Estrogen Receptor Alpha Antagonists. J. Steroid Biochem. Mol. Biol. 2004, 88, 351-360.
210. Xu, H. E.; Stanley, T. B.; Montana, V. G.; Lambert, M. H.; Shearer, B. G.; Cobb, J. E.; McKee, D. D.; Galardi, C. M.; Plunket, K. D.; Nolte, R. T.; Parks, D. J.; Moore, J. T.; Kliewer, S. A.; Willson, T. M.; Stimmel, J. B. Structural Basis for Antagonist-Mediated Recruitment of Nuclear Co-Repressors by PPARalpha. Nature 2002, 415, 813-817.
211. Zhang, D.; Baek, S. H.; Ho, A.; Lee, H.; Jeong, Y. S.; Kim, K. Targeted Degradation of Proteins by Small Molecules: a Novel Tool for Functional Proteomics. Comb. Chem. High Throughput. Screen. 2004, 7, 689-697.
212. Howell, A.; Dowsett, M. Endocrinology and Hormone Therapy in Breast Cancer: Aromatase Inhibitors Versus Antioestrogens. Breast Cancer Res. 2004, 6, 269-274.
213. Brueggemeier, R. W.; Hackett, J. C.; Diaz-Cruz, E. S. Aromatase Inhibitors in the Treatment of Breast Cancer. Endocr. Rev. 2005, 26, 331-345.
214. Nagaich, A. K.; Walker, D. A.; Wolford, R.; Hager, G. L. Rapid periodic binding and displacement of the glucocorticoid receptor during chromatin remodeling. Mol. Cell 2004, 14, 163-174.
215. Paridaens, R.; Heuson, J. C.; Julien, J. P.; Veyret, C.; Van Zyl, J.; Klijn, J. G.; Sylvester, R.; Mignolet, F. Assessment of Estrogenic Recruitment Before Chemotherapy in Advanced Breast Cancer: a Double-Blind Randomized Study. European Organization for Research and Treatment of Cancer Breast Cancer Cooperative Group. J. Clin. Oncol. 1993, 11, 1723-1728.
216. Toillon, R. A.; Magné, N.; Laïos, I.; Lacroix, M.; Duvillier, H.; Lagneaux, L.; Devriendt, D.; Van Houtte, P.; Leclercq, G. Interaction Between Estrogen Receptor Alpha, Ionizing Radiation and (Anti-) Estrogens in Breast Cancer Cells. Breast Cancer Res. Treat. 2005, 93, 207-215.