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Coactivator and Corepressor Regulation of the Agonist/Antagonist Activity of the Mixed Antiestrogen, 4-Hydroxytamoxifen

Department of Cell Biology, Baylor College of Medicine, Houston, Texas 77030-3498

Mixed antiestrogens, such as 4-hydroxytamoxifen (4HT), act as either partial agonists or antagonists of estrogen receptor (ER) function in a tissue-, cell-, and promoter-specific manner, suggesting that intracellular factors modulate their ability to regulate transcription. To determine whether coactivators and corepressors have the capacity to modulate the relative agonist/antagonist activity of 4HT, ER-dependent gene expression was measured in the absence or presence of expression vectors for SRC-1 (steroid receptor coactivator-1) or SMRT (silencing mediator of retinoic acid and thyroid hormone receptors). In Hep G2 cells in which 4HT is an agonist, exogenous SRC-1 enhanced estradiol (E₂)- and 4HT-stimulated transcription in a dose-dependent manner, while SMRT overexpression strongly reduced basal and 4HT-stimulated gene expression with no effect on E₂ activity. These observations were not cell- or promoter-specific inasmuch as similar results were obtained in HeLa cells under conditions in which 4HT is an antagonist. A protein-protein interaction assay indicated that the full-length ER binds to SMRT in vitro. To assess whether relative coactivator and corepressor expression within a given cell could modulate the balance of 4HT agonist/antagonist activity, SRC-1 and SMRT were coexpressed. SMRT overexpression blocked SRC-1 coactivation of 4HT-stimulated gene expression and preferentially inhibited 4HT agonist activity whether or not exogenous SRC-1 was present. The cumulative data in this model system indicate that the relative expression of coactivators and corepressors can modulate 4HT regulation of ER transcriptional activity and suggest they could contribute to the tissue-specific ability of mixed antiestrogens to activate or inhibit ER-mediated gene expression.

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				T. Fujita, Y. Kobayashi, O. Wada, Y. Tateishi, L. Kitada, Y. Yamamoto, H. Takashima, A. Murayama, T. Yano, T. Baba, et al. Full Activation of Estrogen Receptor {alpha} Activation Function-1 Induces Proliferation of Breast Cancer Cells J. Biol. Chem., July 11, 2003; 278(29): 26704 - 26714. [Abstract] [Full Text] [PDF]

				C. Zhao, A. Koide, J. Abrams, S. Deighton-Collins, A. Martinez, J. A. Schwartz, S. Koide, and D. F. Skafar Mutation of Leu-536 in Human Estrogen Receptor-{alpha} Alters the Coupling between Ligand Binding, Transcription Activation, and Receptor Conformation J. Biol. Chem., July 11, 2003; 278(29): 27278 - 27286. [Abstract] [Full Text] [PDF]

				M. Dutertre and C. L. Smith Ligand-Independent Interactions of p160/Steroid Receptor Coactivators and CREB-Binding Protein (CBP) with Estrogen Receptor-{alpha}: Regulation by Phosphorylation Sites in the A/B Region Depends on Other Receptor Domains Mol. Endocrinol., July 1, 2003; 17(7): 1296 - 1314. [Abstract] [Full Text] [PDF]

				S. K. Mishra, A. Mazumdar, R. K. Vadlamudi, F. Li, R.-A. Wang, W. Yu, V. C. Jordan, R. J. Santen, and R. Kumar MICoA, a Novel Metastasis-associated Protein 1 (MTA1) Interacting Protein Coactivator, Regulates Estrogen Receptor-{alpha} Transactivation Functions J. Biol. Chem., May 23, 2003; 278(21): 19209 - 19219. [Abstract] [Full Text] [PDF]

				A. Stevens, H. Garside, A. Berry, C. Waters, A. White, and D. Ray Dissociation of Steroid Receptor Coactivator 1 and Nuclear Receptor Corepressor Recruitment to the Human Glucocorticoid Receptor by Modification of the Ligand-Receptor Interface: The Role of Tyrosine 735 Mol. Endocrinol., May 1, 2003; 17(5): 845 - 859. [Abstract] [Full Text] [PDF]

				B. Farboud, H. Hauksdottir, Y. Wu, and M. L. Privalsky Isotype-Restricted Corepressor Recruitment: a Constitutively Closed Helix 12 Conformation in Retinoic Acid Receptors {beta} and {gamma} Interferes with Corepressor Recruitment and Prevents Transcriptional Repression Mol. Cell. Biol., April 15, 2003; 23(8): 2844 - 2858. [Abstract] [Full Text] [PDF]

				E. K. Keeton and M. Brown Coregulator Expression and Breast Cancer: Improving the Predictive Power of Estrogen Receptor {alpha} Clin. Cancer Res., April 1, 2003; 9(4): 1229 - 1230. [Full Text] [PDF]

				I. Girault, F. Lerebours, S. Amarir, S. Tozlu, M. Tubiana-Hulin, R. Lidereau, and I. Bieche Expression Analysis of Estrogen Receptor {alpha} Coregulators in Breast Carcinoma: Evidence That NCOR1 Expression Is Predictive of the Response to Tamoxifen Clin. Cancer Res., April 1, 2003; 9(4): 1259 - 1266. [Abstract] [Full Text] [PDF]

				C. K. Osborne, V. Bardou, T. A. Hopp, G. C. Chamness, S. G. Hilsenbeck, S. A. W. Fuqua, J. Wong, D. C. Allred, G. M. Clark, and R. Schiff Role of the Estrogen Receptor Coactivator AIB1 (SRC-3) and HER-2/neu in Tamoxifen Resistance in Breast Cancer J Natl Cancer Inst, March 5, 2003; 95(5): 353 - 361. [Abstract] [Full Text] [PDF]

				S. F. Doisneau-Sixou, P. Cestac, S. Chouini, J. S. Carroll, A. D. Hamilton, S. M. Sebti, M. Poirot, P. Balaguer, J.-C. Faye, R. L. Sutherland, et al. Contrasting Effects of Prenyltransferase Inhibitors on Estrogen-Dependent Cell Cycle Progression and Estrogen Receptor-Mediated Transcriptional Activity in MCF-7 Cells Endocrinology, March 1, 2003; 144(3): 989 - 998. [Abstract] [Full Text] [PDF]

				B. L. Riggs and L. C. Hartmann Selective Estrogen-Receptor Modulators -- Mechanisms of Action and Application to Clinical Practice N. Engl. J. Med., February 13, 2003; 348(7): 618 - 629. [Full Text] [PDF]

				G. Liao, L.-Y. Chen, A. Zhang, A. Godavarthy, F. Xia, J. C. Ghosh, H. Li, and J. D. Chen Regulation of Androgen Receptor Activity by the Nuclear Receptor Corepressor SMRT J. Biol. Chem., February 7, 2003; 278(7): 5052 - 5061. [Abstract] [Full Text] [PDF]

				R. Schiff, S. Massarweh, J. Shou, and C. K. Osborne Breast Cancer Endocrine Resistance: How Growth Factor Signaling and Estrogen Receptor Coregulators Modulate Response Clin. Cancer Res., January 1, 2003; 9(1): 447s - 454s. [Abstract] [Full Text]

				E. Demirpence, A. Semlali, J. Oliva, P. Balaguer, E. Badia, M.-J. Duchesne, J.-C. Nicolas, and M. Pons An Estrogen-responsive Element-targeted Histone Deacetylase Enzyme Has an Antiestrogen Activity That Differs from That of Hydroxytamoxifen Cancer Res., November 15, 2002; 62(22): 6519 - 6528. [Abstract] [Full Text] [PDF]

				A. N. Moraitis, V. Giguere, and C. C. Thompson Novel Mechanism of Nuclear Receptor Corepressor Interaction Dictated by Activation Function 2 Helix Determinants Mol. Cell. Biol., October 1, 2002; 22(19): 6831 - 6841. [Abstract] [Full Text] [PDF]

				Y.-C. Hu, C.-R. Shyr, W. Che, X.-M. Mu, E. Kim, and C. Chang Suppression of Estrogen Receptor-mediated Transcription and Cell Growth by Interaction with TR2 Orphan Receptor J. Biol. Chem., September 6, 2002; 277(37): 33571 - 33579. [Abstract] [Full Text] [PDF]

				A. Takeshita, M. Taguchi, N. Koibuchi, and Y. Ozawa Putative Role of the Orphan Nuclear Receptor SXR (Steroid and Xenobiotic Receptor) in the Mechanism of CYP3A4 Inhibition by Xenobiotics J. Biol. Chem., August 30, 2002; 277(36): 32453 - 32458. [Abstract] [Full Text] [PDF]

				I. Dussault, M. Lin, K. Hollister, M. Fan, J. Termini, M. A. Sherman, and B. M. Forman A Structural Model of the Constitutive Androstane Receptor Defines Novel Interactions That Mediate Ligand-Independent Activity Mol. Cell. Biol., August 1, 2002; 22(15): 5270 - 5280. [Abstract] [Full Text] [PDF]

				J D Tugwood and C T Montague Biology and toxicology of PPARg ligands Human and Experimental Toxicology, August 1, 2002; 21(8): 429 - 437. [Abstract] [PDF]

				H.-J. Huang, J. D. Norris, and D. P. McDonnell Identification of a Negative Regulatory Surface within Estrogen Receptor {alpha} Provides Evidence in Support of a Role for Corepressors in Regulating Cellular Responses to Agonists and Antagonists Mol. Endocrinol., August 1, 2002; 16(8): 1778 - 1792. [Abstract] [Full Text] [PDF]

				M. Schulz, M. Eggert, A. Baniahmad, A. Dostert, T. Heinzel, and R. Renkawitz RU486-induced Glucocorticoid Receptor Agonism Is Controlled by the Receptor N Terminus and by Corepressor Binding J. Biol. Chem., July 12, 2002; 277(29): 26238 - 26243. [Abstract] [Full Text] [PDF]