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Metabolic Research Unit (P.W., P.N., J.S., C.A., W.-J.F.,
M.P.N., P.J.K.) University of California School of
Medicine San Francisco, California 94143-0540
Department
of Pathology (D.C., S.-M.H., S.S., M.R.S.) University of Southern
California Los Angeles, California 90033
Department of
Physiology and Biophysics (E.M., B.S.K.) University of Illinois
Urbana, Illinois 61801
Estrogen receptor-
contains two transactivation
functions, a weak constitutive activation function (AF-1) and a
hormone-dependent activation function (AF-2). AF-2 works by recruiting
a large coactivator complex, composed of one or more p160s,
CREB-binding protein (CBP)/p300, and P/CAF (p300 and CBP-associated
factor), via direct contacts with the p160s. We report here that
independent AF-1 activity also requires p160 contacts. Unlike AF-2,
which binds signature NR boxes in the center of the p160 molecule, AF-1
binds to sequences near the p160 C terminus. We propose that the
ability of AF-1 and AF-2 to interact with separate surfaces of the same
coactivator is important for the ability of these transactivation
functions to synergize.
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F. Barletta, C.-W. Wong, C. McNally, B. S. Komm, B. Katzenellenbogen, and B. J. Cheskis Characterization of the Interactions of Estrogen Receptor and MNAR in the Activation of cSrc Mol. Endocrinol., May 1, 2004; 18(5): 1096 - 1108. [Abstract] [Full Text] [PDF] |
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C. L. Smith and B. W. O'Malley Coregulator Function: A Key to Understanding Tissue Specificity of Selective Receptor Modulators Endocr. Rev., February 1, 2004; 25(1): 45 - 71. [Abstract] [Full Text] [PDF] |
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C. K. Cheng, B. K. C. Chow, and P. C. K. Leung An Activator Protein 1-Like Motif Mediates 17{beta}-Estradiol Repression of Gonadotropin-Releasing Hormone Receptor Promoter via an Estrogen Receptor {alpha}-Dependent Mechanism in Ovarian and Breast Cancer Cells Mol. Endocrinol., December 1, 2003; 17(12): 2613 - 2629. [Abstract] [Full Text] [PDF] |
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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] |
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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] |
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S. A. Ghali, B. Gottlieb, R. Lumbroso, L. K. Beitel, Y. Elhaji, J. Wu, L. Pinsky, and M. A. Trifiro The Use of Androgen Receptor Amino/Carboxyl-Terminal Interaction Assays to Investigate Androgen Receptor Gene Mutations in Subjects with Varying Degrees of Androgen Insensitivity J. Clin. Endocrinol. Metab., May 1, 2003; 88(5): 2185 - 2193. [Abstract] [Full Text] [PDF] |
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B. J. Cheskis, N. J. McKenna, C.-W. Wong, J. Wong, B. Komm, C. R. Lyttle, and B. W. O'Malley Hierarchical Affinities and a Bipartite Interaction Model for Estrogen Receptor Isoforms and Full-length Steroid Receptor Coactivator (SRC/p160) Family Members J. Biol. Chem., April 4, 2003; 278(15): 13271 - 13277. [Abstract] [Full Text] [PDF] |
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P. Webb, P. Nguyen, and P. J. Kushner Differential SERM Effects on Corepressor Binding Dictate ERalpha Activity in Vivo J. Biol. Chem., February 21, 2003; 278(9): 6912 - 6920. [Abstract] [Full Text] [PDF] |
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R. Kumar and E. B. Thompson Transactivation Functions of the N-Terminal Domains of Nuclear Hormone Receptors: Protein Folding and Coactivator Interactions Mol. Endocrinol., January 1, 2003; 17(1): 1 - 10. [Abstract] [Full Text] [PDF] |
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Y. He, D. Szapary, and S. S. Simons Jr. Modulation of Induction Properties of Glucocorticoid Receptor-Agonist and -Antagonist Complexes by Coactivators Involves Binding to Receptors but Is Independent of Ability of Coactivators to Augment Transactivation J. Biol. Chem., December 13, 2002; 277(51): 49256 - 49266. [Abstract] [Full Text] [PDF] |
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C. Teyssier, D. Chen, and M. R. Stallcup Requirement for Multiple Domains of the Protein Arginine Methyltransferase CARM1 in Its Transcriptional Coactivator Function J. Biol. Chem., November 22, 2002; 277(48): 46066 - 46072. [Abstract] [Full Text] [PDF] |
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M. E. Torres-Padilla, F. M. Sladek, and M. C. Weiss Developmentally Regulated N-terminal Variants of the Nuclear Receptor Hepatocyte Nuclear Factor 4alpha Mediate Multiple Interactions through Coactivator and Corepressor-Histone Deacetylase Complexes J. Biol. Chem., November 15, 2002; 277(47): 44677 - 44687. [Abstract] [Full Text] [PDF] |
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M. Desclozeaux, I. N. Krylova, F. Horn, R. J. Fletterick, and H. A. Ingraham Phosphorylation and Intramolecular Stabilization of the Ligand Binding Domain in the Nuclear Receptor Steroidogenic Factor 1 Mol. Cell. Biol., October 15, 2002; 22(20): 7193 - 7203. [Abstract] [Full Text] [PDF] |
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L. F. Su, Z. Wang, and M. J. Garabedian Regulation of GRIP1 and CBP Coactivator Activity by Rho GDI Modulates Estrogen Receptor Transcriptional Enhancement J. Biol. Chem., September 27, 2002; 277(40): 37037 - 37044. [Abstract] [Full Text] [PDF] |
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M. Bommer, A. Benecke, H. Gronemeyer, and C. Rochette-Egly TIF2 Mediates the Synergy between RARalpha 1 Activation Functions AF-1 and AF-2 J. Biol. Chem., September 27, 2002; 277(40): 37961 - 37966. [Abstract] [Full Text] [PDF] |
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S. E. Wardell, V. Boonyaratanakornkit, J. S. Adelman, A. Aronheim, and D. P. Edwards Jun Dimerization Protein 2 Functions as a Progesterone Receptor N-Terminal Domain Coactivator Mol. Cell. Biol., August 1, 2002; 22(15): 5451 - 5466. [Abstract] [Full Text] [PDF] |
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P. Yi, S. Bhagat, R. Hilf, R. A. Bambara, and M. Muyan Differences in the Abilities of Estrogen Receptors to Integrate Activation Functions Are Critical for Subtype-Specific Transcriptional Responses Mol. Endocrinol., August 1, 2002; 16(8): 1810 - 1827. [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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A. Vottero, T. Kino, H. Combe, P. Lecomte, and G. P. Chrousos A Novel, C-Terminal Dominant Negative Mutation of the GR Causes Familial Glucocorticoid Resistance through Abnormal Interactions with p160 Steroid Receptor Coactivators J. Clin. Endocrinol. Metab., June 1, 2002; 87(6): 2658 - 2667. [Abstract] [Full Text] [PDF] |
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T. Barkhem, L.-A. Haldosen, J.-A. Gustafsson, and S. Nilsson pS2 Gene Expression in HepG2 cells: Complex Regulation through Crosstalk between the Estrogen Receptor alpha , an Estrogen-Responsive Element, and the Activator Protein 1 Response Element Mol. Pharmacol., June 1, 2002; 61(6): 1273 - 1283. [Abstract] [Full Text] [PDF] |
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D. P. McDonnell and J. D. Norris Connections and Regulation of the Human Estrogen Receptor Science, May 31, 2002; 296(5573): 1642 - 1644. [Abstract] [Full Text] [PDF] |
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P. J. Shughrue, G. R. Askew, T. L. Dellovade, and I. Merchenthaler Estrogen-Binding Sites and Their Functional Capacity in Estrogen Receptor Double Knockout Mouse Brain Endocrinology, May 1, 2002; 143(5): 1643 - 1650. [Abstract] [Full Text] [PDF] |
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D. Kressler, S. N. Schreiber, D. Knutti, and A. Kralli The PGC-1-related Protein PERC Is a Selective Coactivator of Estrogen Receptor alpha J. Biol. Chem., April 12, 2002; 277(16): 13918 - 13925. [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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B. He, J. T. Minges, L. W. Lee, and E. M. Wilson The FXXLF Motif Mediates Androgen Receptor-specific Interactions with Coregulators J. Biol. Chem., March 15, 2002; 277(12): 10226 - 10235. [Abstract] [Full Text] [PDF] |
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J. M. Hall, D. P. McDonnell, and K. S. Korach Allosteric Regulation of Estrogen Receptor Structure, Function, and Coactivator Recruitment by Different Estrogen Response Elements Mol. Endocrinol., March 1, 2002; 16(3): 469 - 486. [Abstract] [Full Text] [PDF] |
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I. T. R. Cavarretta, R. Mukopadhyay, D. M. Lonard, L. M. Cowsert, C. F. Bennett, B. W. O'Malley, and C. L. Smith Reduction of Coactivator Expression by Antisense Oligodeoxynucleotides Inhibits ER{alpha} Transcriptional Activity and MCF-7 Proliferation Mol. Endocrinol., February 1, 2002; 16(2): 253 - 270. [Abstract] [Full Text] [PDF] |
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Z.-x. Zhou, B. He, S. H. Hall, E. M. Wilson, and F. S. French Domain Interactions between Coregulator ARA70 and the Androgen Receptor (AR) Mol. Endocrinol., February 1, 2002; 16(2): 287 - 300. [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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S. Fan, Y. X. Ma, C. Wang, R.-Q. Yuan, Q. Meng, J.-A. Wang, M. Erdos, I. D. Goldberg, P. Webb, P. J. Kushner, et al. p300 Modulates the BRCA1 Inhibition of Estrogen Receptor Activity Cancer Res., January 1, 2002; 62(1): 141 - 151. [Abstract] [Full Text] [PDF] |
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A. Warnmark, A. Wikstrom, A. P. H. Wright, J.-A. Gustafsson, and T. Hard The N-terminal Regions of Estrogen Receptor alpha and beta Are Unstructured in Vitro and Show Different TBP Binding Properties J. Biol. Chem., November 30, 2001; 276(49): 45939 - 45944. [Abstract] [Full Text] [PDF] |
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R. Metivier, G. Penot, G. Flouriot, and F. Pakdel Synergism Between ER{alpha} Transactivation Function 1 (AF-1) and AF-2 Mediated by Steroid Receptor Coactivator Protein-1: Requirement for the AF-1 {alpha}-Helical Core and for a Direct Interaction Between the N- and C-Terminal Domains Mol. Endocrinol., November 1, 2001; 15(11): 1953 - 1970. [Abstract] [Full Text] [PDF] |
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S. Nilsson, S. Makela, E. Treuter, M. Tujague, J. Thomsen, G. Andersson, E. Enmark, K. Pettersson, M. Warner, and J.-A. Gustafsson Mechanisms of Estrogen Action Physiol Rev, October 1, 2001; 81(4): 1535 - 1565. [Abstract] [Full Text] [PDF] |
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M. Maggiolini, D. Bonofiglio, S. Marsico, M. L. Panno, B. Cenni, D. Picard, and S. Ando Estrogen Receptor alpha Mediates the Proliferative but Not the Cytotoxic Dose-Dependent Effects of Two Major Phytoestrogens on Human Breast Cancer Cells Mol. Pharmacol., September 1, 2001; 60(3): 595 - 602. [Abstract] [Full Text] [PDF] |
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Z. Yang and M. L. Privalsky Isoform-Specific Transcriptional Regulation by Thyroid Hormone Receptors: Hormone-Independent Activation Operates through a Steroid Receptor Mode of Coactivator Interaction Mol. Endocrinol., July 1, 2001; 15(7): 1170 - 1185. [Abstract] [Full Text] [PDF] |
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H. Liu, E.-S. Lee, A. D. L. Reyes, J. W. Zapf, and V. C. Jordan Silencing and Reactivation of the Selective Estrogen Receptor Modulator-Estrogen Receptor {{alpha}} Complex Cancer Res., May 1, 2001; 61(9): 3632 - 3639. [Abstract] [Full Text] |
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W. Feng, P. Webb, P. Nguyen, X. Liu, J. Li, M. Karin, and P. J. Kushner Potentiation of Estrogen Receptor Activation Function 1 (AF-1) by Src/JNK through a Serine 118-Independent Pathway Mol. Endocrinol., January 1, 2001; 15(1): 32 - 45. [Abstract] [Full Text] |
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R. M. Tolon, A. I. Castillo, A. M. Jimenez-Lara, and A. Aranda Association with Ets-1 Causes Ligand- and AF2-Independent Activation of Nuclear Receptors Mol. Cell. Biol., December 1, 2000; 20(23): 8793 - 8802. [Abstract] [Full Text] [PDF] |
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F. Schaufele, C.-y. Chang, W. Liu, J. D. Baxter, S. K. Nordeen, Y. Wan, R. N. Day, and D. P. McDonnell Temporally Distinct and Ligand-Specific Recruitment of Nuclear Receptor-Interacting Peptides and Cofactors to Subnuclear Domains Containing the Estrogen Receptor Mol. Endocrinol., December 1, 2000; 14(12): 2024 - 2039. [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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R. Métivier, F. G. Petit, Y. Valotaire, and F. Pakdel Function of N-Terminal Transactivation Domain of the Estrogen Receptor Requires a Potential {alpha}-Helical Structure and Is Negatively Regulated by the A Domain Mol. Endocrinol., November 1, 2000; 14(11): 1849 - 1871. [Abstract] [Full Text] |
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F. Delaunay, K. Pettersson, M. Tujague, and J.-A. Gustafsson Functional Differences between the Amino-Terminal Domains of Estrogen Receptors alpha and beta Mol. Pharmacol., September 1, 2000; 58(3): 584 - 590. [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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J. Font de Mora and M. Brown AIB1 Is a Conduit for Kinase-Mediated Growth Factor Signaling to the Estrogen Receptor Mol. Cell. Biol., July 15, 2000; 20(14): 5041 - 5047. [Abstract] [Full Text] [PDF] |
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H. Fuse, H. Kitagawa, and S. Kato Characterization of Transactivational Property and Coactivator Mediation of Rat Mineralocorticoid Receptor Activation Function-1 (AF-1) Mol. Endocrinol., June 1, 2000; 14(6): 889 - 899. [Abstract] [Full Text] |
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A. Bollig and R. J. Miksicek An Estrogen Receptor-{alpha} Splicing Variant Mediates Both Positive and Negative Effects on Gene Transcription Mol. Endocrinol., May 1, 2000; 14(5): 634 - 649. [Abstract] [Full Text] |
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G. de Haan, S. Chusacultanachai, C. Mao, B. S. Katzenellenbogen, and D. J. Shapiro Estrogen Receptor-KRAB Chimeras Are Potent Ligand-dependent Repressors of Estrogen-regulated Gene Expression J. Biol. Chem., April 28, 2000; 275(18): 13493 - 13501. [Abstract] [Full Text] [PDF] |
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Y. Xu, L. Klein-Hitpass, and M. K. Bagchi E1A-Mediated Repression of Progesterone Receptor-Dependent Transactivation Involves Inhibition of the Assembly of a Multisubunit Coactivation Complex Mol. Cell. Biol., March 15, 2000; 20(6): 2138 - 2146. [Abstract] [Full Text] [PDF] |
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S.-M. Huang and M. R. Stallcup Mouse Zac1, a Transcriptional Coactivator and Repressor for Nuclear Receptors Mol. Cell. Biol., March 1, 2000; 20(5): 1855 - 1867. [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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C. Leo, H. Li, and J. D. Chen Differential Mechanisms of Nuclear Receptor Regulation by Receptor-associated Coactivator 3 J. Biol. Chem., February 25, 2000; 275(8): 5976 - 5982. [Abstract] [Full Text] [PDF] |
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