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Departments of Medicine and Pathology and the Molecular, Biology Program, University of Colorado Health Sciences Center, Denver, Colorado 80262
Steroid receptor antagonists, such as the antiestrogen tamoxifen or the antiprogestin RU486, can have inappropriate agonist-like effects in tissues and tumors. To explain this paradox we postulated that coactivators are inadvertently brought to the promoters of DNA-bound, antagonist-occupied receptors. The human (h) progesterone receptor (PR) hinge-hormone binding domain (H-HBD) was used as bait in a two-hybrid screen of a HeLa cDNA library, in which the yeast cells were treated with RU486. We have isolated and characterized two interesting steroid receptor-interacting proteins that regulate transcription in opposite directions. The first is L7/SPA, a previously described 27-kDa protein containing a basic region leucine zipper domain, having no known nuclear function. When coexpressed with tamoxifen-occupied estrogen receptors (hER) or RU486-occupied hPR or glucocorticoid receptors (hGR), L7/SPA increases the partial agonist activity of the antagonists by 3- to 10-fold, but it has no effect on agonist-mediated transcription. The interaction of L7/SPA with hPR maps to the hinge region, and indeed, the hPR hinge region squelches L7/SPA-dependent induction of antagonist-mediated transcription. Interestingly, pure antagonists that lack partial agonist effects, such as the antiestrogen ICI164,384 or the antiprogestin ZK98299, cannot be up-regulated by L7/SPA. We also isolated, cloned, and sequenced the human homolog (hN-CoR) of the 270-kDa mouse (m) thyroid/retinoic acid receptor corepressor. Binding of hN-CoR maps to the hPR-HBD. mN-CoR, and a related human corepressor, SMRT, suppress RU486 or tamoxifen-mediated partial agonist activity by more than 90%. This suppression is completely squelched by overexpression of the hPR H-HBD. Additionally, both corepressors reverse the antagonist-dependent transcriptional up-regulation produced by L7/SPA. Our data suggest that the direction of transcription by antagonist-occupied steroid receptors can be controlled by the ratio of coactivators to corepressors recruited to the transcription complex by promoter-bound receptors. In normal tissues and in hormone-resistant breast cancers in which the agonist activity of mixed antagonists predominates, steroid receptors may be preferentially bound by coactivators. This suggests a strategy by which such partial agonist activity can be eliminated and by which candidate receptor ligands can be screened for this activity.
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 S. A. Leonhardt and D. P. Edwards Mechanism of Action of Progesterone Antagonists Experimental Biology and Medicine, December 1, 2002; 227(11): 969 - 980. [Abstract] [Full Text]
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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]
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S. Cheng, S. Brzostek, S. R. Lee, A. N. Hollenberg, and S. P. Balk Inhibition of the Dihydrotestosterone-Activated Androgen Receptor by Nuclear Receptor Corepressor Mol. Endocrinol., July 1, 2002; 16(7): 1492 - 1501. [Abstract] [Full Text] [PDF]
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F. Wieser, C. Schneeberger, G. Hudelist, C. Singer, C. Kurz, F. Nagele, C. Gruber, J.C. Huber, and W. Tschugguel Endometrial nuclear receptor co-factors SRC-1 and N-CoR are increased in human endometrium during menstruation Mol. Hum. Reprod., July 1, 2002; 8(7): 644 - 650. [Abstract] [Full Text] [PDF]
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Z. Liu, D. Auboeuf, J. Wong, J. D. Chen, S. Y. Tsai, M.-J. Tsai, and B. W. O'Malley Coactivator/corepressor ratios modulate PR-mediated transcription by the selective receptor modulator RU486 PNAS, June 11, 2002; 99(12): 7940 - 7944. [Abstract] [Full Text] [PDF]
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R. C. Dardes, R. M. O'Regan, C. Gajdos, S. P. Robinson, D. Bentrem, A. De Los Reyes, and V. C. Jordan Effects of a New Clinically Relevant Antiestrogen (GW5638) Related to Tamoxifen on Breast and Endometrial Cancer Growth in Vivo Clin. Cancer Res., June 1, 2002; 8(6): 1995 - 2001. [Abstract] [Full Text] [PDF]
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Z.-Q. Huang, J. Li, and J. Wong AR Possesses an Intrinsic Hormone-Independent Transcriptional Activity Mol. Endocrinol., May 1, 2002; 16(5): 924 - 937. [Abstract] [Full Text] [PDF]
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C. A. Heinlein and C. Chang Androgen Receptor (AR) Coregulators: An Overview Endocr. Rev., April 1, 2002; 23(2): 175 - 200. [Abstract] [Full Text] [PDF]
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C.-Y. Chang and D. P. McDonnell Evaluation of Ligand-Dependent Changes in AR Structure Using Peptide Probes Mol. Endocrinol., April 1, 2002; 16(4): 647 - 660. [Abstract] [Full Text] [PDF]
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H. Dotzlaw, U. Moehren, S. Mink, A. C. B. Cato, J. A. Iniguez Lluhi, and A. Baniahmad The Amino Terminus of the Human AR Is Target for Corepressor Action and Antihormone Agonism Mol. Endocrinol., April 1, 2002; 16(4): 661 - 673. [Abstract] [Full Text] [PDF]
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 Y. Shang and M. Brown Molecular Determinants for the Tissue Specificity of SERMs Science, March 29, 2002; 295(5564): 2465 - 2468. [Abstract] [Full Text] [PDF]
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 K. Jepsen and M. G. Rosenfeld Biological roles and mechanistic actions of co-repressor complexes J. Cell Sci., February 15, 2002; 115(4): 689 - 698. [Abstract] [Full Text] [PDF]
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A. Marimuthu, W. Feng, T. Tagami, H. Nguyen, J. L. Jameson, R. J. Fletterick, J. D. Baxter, and B. L. West TR Surfaces and Conformations Required to Bind Nuclear Receptor Corepressor Mol. Endocrinol., February 1, 2002; 16(2): 271 - 286. [Abstract] [Full Text] [PDF]
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M. Fan, X. Long, J. A. Bailey, C. A. Reed, E. Osborne, E. A. Gize, E. A. Kirk, R. M. Bigsby, and K. P. Nephew The Activating Enzyme of NEDD8 Inhibits Steroid Receptor Function Mol. Endocrinol., February 1, 2002; 16(2): 315 - 330. [Abstract] [Full Text] [PDF]
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S. R. Lee, S. M. Ramos, A. Ko, D. Masiello, K. D. Swanson, M. L. Lu, and S. P. Balk AR and ER Interaction with a p21-Activated Kinase (PAK6) Mol. Endocrinol., January 1, 2002; 16(1): 85 - 99. [Abstract] [Full Text] [PDF]
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V. C. Jordan, J. M. Schafer, A. S. Levenson, H. Liu, K. M. Pease, L. A. Simons, and J. W. Zapf Molecular Classification of Estrogens Cancer Res., September 1, 2001; 61(18): 6619 - 6623. [Abstract] [Full Text] [PDF]
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 S. DJELIDI, A. BEGGAH, N. COURTOIS-COUTRY, M. FAY, F. CLUZEAUD, S. VIENGCHAREUN, J.-P. BONVALET, N. FARMAN, and M. BLOT-CHABAUD Basolateral Translocation by Vasopressin of the Aldosterone-Induced Pool of Latent Na-K-ATPases Is Accompanied by {alpha}1 Subunit Dephosphorylation: Study in a New Aldosterone-Sensitive Rat Cortical Collecting Duct Cell Line J. Am. Soc. Nephrol., September 1, 2001; 12(9): 1805 - 1818. [Abstract] [Full Text] [PDF]
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J. M. Schafer, E.-S. Lee, R. C. Dardes, D. Bentrem, R. M. O'Regan, A. De Los Reyes, and V. C. Jordan Analysis of Cross-Resistance of the Selective Estrogen Receptor Modulators Arzoxifene (LY353381) and LY117018 in Tamoxifen-stimulated Breast Cancer Xenografts Clin. Cancer Res., August 1, 2001; 7(8): 2505 - 2512. [Abstract] [Full Text] [PDF]
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R. N. Cohen, S. Brzostek, B. Kim, M. Chorev, F. E. Wondisford, and A. N. Hollenberg The Specificity of Interactions between Nuclear Hormone Receptors and Corepressors Is Mediated by Distinct Amino Acid Sequences within the Interacting Domains Mol. Endocrinol., July 1, 2001; 15(7): 1049 - 1061. [Abstract] [Full Text] [PDF]
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A. Aranda and A. Pascual Nuclear Hormone Receptors and Gene Expression Physiol Rev, July 1, 2001; 81(3): 1269 - 1304. [Abstract] [Full Text] [PDF]
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 L. J. Havrilesky, C. P. McMahon, E. K. Lobenhofer, R. Whitaker, J. R. Marks, and A. Berchuck Relationship Between Expression of Coactivators and Corepressors of Hormone Receptors and Resistance of Ovarian Cancers to Growth Regulation by Steroid Hormones Reproductive Sciences, April 1, 2001; 8(2): 104 - 113. [Abstract] [PDF]
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R. Clarke, F. Leonessa, J. N. Welch, and T. C. Skaar Cellular and Molecular Pharmacology of Antiestrogen Action and Resistance Pharmacol. Rev., March 1, 2001; 53(1): 25 - 72. [Abstract] [Full Text] [PDF]
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G. Giannoukos, D. Szapary, C. L. Smith, J. E. W. Meeker, and S. S. Simons Jr. New Antiprogestins with Partial Agonist Activity: Potential Selective Progesterone Receptor Modulators (SPRMs) and Probes for Receptor- and Coregulator-Induced Changes in Progesterone Receptor Induction Properties Mol. Endocrinol., February 1, 2001; 15(2): 255 - 270. [Abstract] [Full Text]
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G. Buchanan, M. Yang, J. M. Harris, H. S. Nahm, G. Han, N. Moore, J. M. Bentel, R. J. Matusik, D. J. Horsfall, V. R. Marshall, et al. Mutations at the Boundary of the Hinge and Ligand Binding Domain of the Androgen Receptor Confer Increased Transactivation Function Mol. Endocrinol., January 1, 2001; 15(1): 46 - 56. [Abstract] [Full Text]
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 M. Dutertre and C. L. Smith Molecular Mechanisms of Selective Estrogen Receptor Modulator (SERM) Action J. Pharmacol. Exp. Ther., November 1, 2000; 295(2): 431 - 437. [Abstract] [Full Text]
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H. Kurokawa, A. E. G. Lenferink, J. F. Simpson, P. I. Pisacane, M. X. Sliwkowski, J. T. Forbes, and C. L. Arteaga Inhibition of HER2/neu (erbB-2) and Mitogen-activated Protein Kinases Enhances Tamoxifen Action against HER2-overexpressing, Tamoxifen-resistant Breast Cancer Cells Cancer Res., October 1, 2000; 60(20): 5887 - 5894. [Abstract] [Full Text]
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 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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S. A. W. Fuqua, C. Wiltschke, Q. X. Zhang, A. Borg, C. G. Castles, W. E. Friedrichs, T. Hopp, S. Hilsenbeck, S. Mohsin, P. O’Connell, et al. A Hypersensitive Estrogen Receptor-{{alpha}} Mutation in Premalignant Breast Lesions Cancer Res., August 1, 2000; 60(15): 4026 - 4029. [Abstract] [Full Text]
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K. P. Nephew, S. Ray, M. Hlaing, A. Ahluwalia, S. D. Wu, X. Long, S. M. Hyder, and R. M. Bigsby Expression of Estrogen Receptor Coactivators in the Rat Uterus Biol Reprod, August 1, 2000; 63(2): 361 - 367. [Abstract] [Full Text]
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C. Mao and D. J. Shapiro A Histone Deacetylase Inhibitor Potentiates Estrogen Receptor Activation of a Stably Integrated Vitellogenin Promoter in HepG2 Cells Endocrinology, July 1, 2000; 141(7): 2361 - 2369. [Abstract] [Full Text] [PDF]
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R. N. Cohen, A. Putney, F. E. Wondisford, and A. N. Hollenberg The Nuclear Corepressors Recognize Distinct Nuclear Receptor Complexes Mol. Endocrinol., June 1, 2000; 14(6): 900 - 914. [Abstract] [Full Text]
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 Y. K. Hodges, L. Tung, X.-D. Yan, J. D. Graham, K. B. Horwitz, and L. D. Horwitz Estrogen Receptors {alpha} and {beta} : Prevalence of Estrogen Receptor {beta} mRNA in Human Vascular Smooth Muscle and Transcriptional Effects Circulation, April 18, 2000; 101(15): 1792 - 1798. [Abstract] [Full Text] [PDF]
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D. Robyr, A. P. Wolffe, and W. Wahli Nuclear Hormone Receptor Coregulators In Action: Diversity For Shared Tasks Mol. Endocrinol., March 1, 2000; 14(3): 329 - 347. [Full Text]
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S. Oesterreich, Q. Zhang, T. Hopp, S. A. W. Fuqua, M. Michaelis, H. H. Zhao, J. R. Davie, C. K. Osborne, and A. V. Lee Tamoxifen-Bound Estrogen Receptor (ER) Strongly Interacts with the Nuclear Matrix Protein HET/SAF-B, a Novel Inhibitor of ER-Mediated Transactivation Mol. Endocrinol., March 1, 2000; 14(3): 369 - 381. [Abstract] [Full Text]
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