Dominant Activity of Activation Function 1 (AF-1) and Differential Stoichiometric Requirements for AF-1 and -2 in the Estrogen Receptor α-β Heterodimeric Complex

REFERENCES

• Ali, S., D. Metzger, J.-M. Bornert, and J. Chambon 1993. Modulation of transcriptional activation by ligand-dependent phosphorylation of the human oestrogen receptor A/B region. EMBO J. 12:1153–1160.
   PubMed Web of Science ®Google Scholar
• Beato, M. 1989. Gene regulation by steroid hormones. Cell 56:335–344.
   PubMed Web of Science ®Google Scholar
• Berry, M., D. Metzger, and J. Chambon 1990. Role of the two activating domains of the oestrogen receptor in the cell-type and promoter-context dependent agonistic activity of the anti-oestrogen 4-hydroxytamoxifen. EMBO J. 9:2811–2818.
   PubMed Web of Science ®Google Scholar
• Berry, M., A.-M. Nunez, and J. Chambon 1989. Estrogen-responsive element of the human pS2 gene is an imperfectly palindromic sequence. Proc. Natl. Acad. Sci. USA 86:1218–1222.
   PubMed Web of Science ®Google Scholar
• Bunone, G., P.-A. Briand, R. J. Miksicek, and J. Picard 1996. Activation of the unliganded estrogen receptor by EGF involves the MAP kinase pathway and direct phosphorylation. EMBO J. 15:2174–2183.
   PubMed Web of Science ®Google Scholar
• Couse, J. F., J. Lindzey, K. Grandien, J. A. Gustafsson, and J. Korach 1997. Tissue distribution and quantitative analysis of estrogen receptor-α (ER-α) and estrogen receptor-β (ER-β) messenger ribonucleic acid in the wild-type and ER-α-knockout mouse. Endocrinology 138:4613–4621.
   PubMed Web of Science ®Google Scholar
• Cowley, S. M., S. Hoare, S. Mosselman, and J. Parker 1997. Estrogen receptors α and β form heterodimers on DNA. J. Biol. Chem. 272:19858–19862.
   PubMed Web of Science ®Google Scholar
• Danielian, P. S., R. White, J. A. Lees, and J. Parker 1992. Identification of a conserved region required for hormone dependent transcriptional activation by steroid hormone receptors. EMBO J. 11:1025–1033.
   PubMed Web of Science ®Google Scholar
• Fawell, S. E., J. A. Lees, R. White, and J. Parker 1990. Characterization and colocalization of steroid binding and dimerization activities in the mouse estrogen receptor. Cell 60:953–962.
   PubMed Web of Science ®Google Scholar
• Forman, B. M., K. Umesono, J. Chen, and J. Evans 1995. Unique response pathways are established by allosteric interactions among nuclear hormone receptors. Cell 81:541–550.
   PubMed Web of Science ®Google Scholar
• Giguère, V., M. Shago, R. Zirngibl, P. Tate, J. Rossant, and J. Varmuza 1990. Identification of a novel isoform of the retinoic acid receptor γ expressed in the mouse embryo. Mol. Cell. Biol. 10:2335–2340.
   PubMed Web of Science ®Google Scholar
• Giguère, V., A. Tremblay, and J. Tremblay 1998. Estrogen receptor β: reevaluation of estrogen and antiestrogen signaling. Steroids 63:335–339.
   PubMed Web of Science ®Google Scholar
• Green, S., P. Walter, V. Kumar, A. Krust, J. M. Bornet, P. Argos, and J. Chambon 1986. Human oestrogen receptor cDNA: sequence, expression and homology to v-erbA. Nature 320:134–139.
   PubMed Web of Science ®Google Scholar
• Greene, G. L., P. Gilna, M. Waterfield, A. Baker, Y. Hort, and J. Shine 1986. Sequence and expression of human estrogen receptor complementary DNA. Science 231:1150–1154.
   PubMed Web of Science ®Google Scholar
• Kalkhoven, E., J. E. Valentine, D. M. Heery, and J. Parker 1998. Isoforms of steroid receptor co-activator 1 differ in their ability to potentiate transcription by the oestrogen receptor. EMBO J. 17:232–243.
   PubMed Web of Science ®Google Scholar
• Kato, S., H. Endoh, Y. Masuhiro, T. Kitamoto, S. Uchiyama, H. Sasaki, S. Masushige, Y. Gotoh, E. Nishida, H. Kawashima, D. Metzger, and J. Chambon 1995. Activation of the estrogen receptor through phosphorylation by mitogen-activated protein kinase. Science 270:1491–1494.
   PubMed Web of Science ®Google Scholar
• Keller, H., C. Dreyer, J. Medin, A. Mahfoudi, K. Ozato, and J. Wahli 1993. Fatty acids and retinoids control lipid metabolism through activation of peroxisome proliferator-activated receptor-retinoid X receptor heterodimers. Proc. Natl. Acad. Sci. USA 90:2160–2164.
   PubMed Web of Science ®Google Scholar
• Kliewer, S. A., K. Umesono, D. J. Noonan, R. A. Heyman, and J. Evans 1992. Convergence of 9-cis retinoic acid and peroxisome proliferator signalling pathways through heterodimer formation of their receptors. Nature 358:771–774.
   PubMed Web of Science ®Google Scholar
• Kuiper, G. G. J. M., E. Enmark, M. Pelto-Huikko, S. Nilsson, and J. Gustafsson 1996. Cloning of a novel estrogen receptor expressed in rat prostate and ovary. Proc. Natl. Acad. Sci. USA 93:5925–5930.
   PubMed Web of Science ®Google Scholar
• Kurokawa, R., J. DiRenzo, M. Boehm, J. Sugarman, B. Gloss, G. M. Rosenfeld, R. A. Heyman, and J. Glass 1994. Regulation of retinoid signalling by receptor polarity and allosteric control of ligand binding. Nature 371:528–531.
   PubMed Web of Science ®Google Scholar
• Leygue, E., H. Dotzlaw, P. H. Watson, and J. Murphy 1998. Altered estrogen receptor α and β messenger RNA expression during human breast tumorigenesis. Cancer Res. 58:3197–3201.
   PubMed Web of Science ®Google Scholar
• Mader, S., V. Kumar, H. de Verneuil, and J. Chambon 1989. Three amino acids of the oestrogen receptor are essential to its ability to distinguish an oestrogen from a glucocorticoid-responsive element. Nature 338:271–274.
   PubMed Web of Science ®Google Scholar
• Mangelsdorf, D. J., and J. Evans 1995. The RXR heterodimers and orphan receptors. Cell 83:841–850.
   PubMed Web of Science ®Google Scholar
• McInerney, E. M., K. E. Weis, J. Sun, S. Mosselman, and J. Katzenellenbogen 1998. Transcription activation by the human estrogen receptor subtype β (ERβ) studied with ERβ and ERα receptor chimeras. Endocrinology 139:4513–4522.
   PubMedGoogle Scholar
• Minucci, S., M. Leid, R. Toyama, J.-P. Saint-Jeannet, V. J. Peterson, V. Horn, J. E. Ishmael, N. Bhattacharyya, A. Dey, I. B. Dawid, and J. Ozato 1997. Retinoid X receptor (RXR) within the RXR-retinoic acid receptor heterodimer binds its ligand and enhances retinoid-dependent gene expression. Mol. Cell. Biol. 17:644–655.
   PubMed Web of Science ®Google Scholar
• Mosselman, S., J. Polman, and J. Dijkema 1996. ERβ: identification and characterization of a novel human estrogen receptor. FEBS Lett. 392:49–53.
   PubMed Web of Science ®Google Scholar
• Nolte, R. T., G. B. Wisely, S. Westin, J. E. Cobb, M. H. Lambert, R. Kurokawa, M. G. Rosenfeld, T. M. Willson, C. K. Glass, and J. Milburn 1998. Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-γ. Nature 395:137–143.
   PubMed Web of Science ®Google Scholar
• Pace, P., J. Taylor, S. Suntharalingam, R. C. Coombes, and J. Ali 1997. Human estrogen receptor β binds DNA in a manner similar to and dimerizes with estrogen receptor α. J. Biol. Chem. 272:25832–25838.
   PubMed Web of Science ®Google Scholar
• Paech, K., P. Webb, G. G. J. M. Kuiper, S. Nilsson, J.-Å. Gustafsson, P. J. Kushner, and J. Scanlan 1997. Differential ligand activation of estrogen receptors ERα and ERβ at AP1 sites. Science 277:1508–1510.
   PubMed Web of Science ®Google Scholar
• Pettersson, K., K. Grandien, G. G. J. M. Kuiper, and J. Gustafsson 1997. Mouse estrogen receptor β forms estrogen response element-binding heterodimers with estrogen receptor α. Mol. Endocrinol. 11:1486–1496.
   PubMed Web of Science ®Google Scholar
• Schulman, I. G., C. Li, J. W. R. Schwabe, and J. Evans 1997. The phantom ligand effect: allosteric control of transcription by the retinoid X receptor. Genes Dev. 11:299–308.
   PubMed Web of Science ®Google Scholar
• Schulman, I. G., G. Shao, and J. Heyman 1998. Transactivation by retinoid X receptor–peroxisome proliferator-activated receptor γ (PPARγ) heterodimers: intermolecular synergy requires only the PPARγ hormone-dependent activation function. Mol. Cell. Biol. 18:3483–3494.
   PubMed Web of Science ®Google Scholar
• Sladek, R., J.-A. Bader, and J. Giguère 1997. The orphan nuclear receptor estrogen-related receptor α is a transcriptional regulator of the human medium-chain acyl coenzyme A dehydrogenase gene. Mol. Cell. Biol. 17:5400–5409.
   PubMed Web of Science ®Google Scholar
• Tremblay, A., G. B. Tremblay, C. Labrie, F. Labrie, and J. Giguère 1998. EM-800, a novel antiestrogen, acts as a pure antagonist of the transcriptional functions of estrogen receptors α and β. Endocrinology 139:111–118.
   PubMed Web of Science ®Google Scholar
• Tremblay, G. B., A. Tremblay, N. G. Copeland, D. J. Gilbert, N. A. Jenkins, F. Labrie, and J. Giguère 1997. Cloning, chromosomal localization and functional analysis of the murine estrogen receptor β. Mol. Endocrinol. 11:353–365.
   PubMed Web of Science ®Google Scholar
• Tremblay, G. B., A. Tremblay, F. Labrie, and J. Giguère 1998. Ligand-independent activation of the estrogen receptors α and β by mutations of a conserved tyrosine can be abolished by antiestrogens. Cancer Res. 58:877–881.
   PubMedGoogle Scholar
• Umesono, K., K. K. Murakami, C. C. Thompson, and J. Evans 1991. Direct repeats as selective response elements for the thyroid hormone, retinoic acid, and vitamin D3 receptors. Cell 65:1255–1266.
   PubMed Web of Science ®Google Scholar
• Watanabe, T., S. Inoue, S. Ogawa, Y. Ishii, H. Hiroi, K. Ikeda, A. Orimo, and J. Muramatsu 1997. Agonistic effect of tamoxifen is dependent on cell type, ERE-promoter context, and estrogen receptor subtype: functional difference between estrogen receptors α and β. Biochem. Biophys. Res. Commun. 236:140–145.
   PubMed Web of Science ®Google Scholar
• Westin, S., R. Kurokawa, R. T. Nolte, G. B. Wisely, E. M. McInerney, D. W. Rose, M. V. Milburn, M. G. Rosenfeld, and J. Glass 1998. Interactions controlling the assembly of nuclear-receptor heterodimers and co-activators. Nature 395:199–202.
   PubMed Web of Science ®Google Scholar
• Wiebel, F. F., and J. Gustafsson 1997. Heterodimeric interaction between retinoid X receptor α and orphan nuclear receptor OR1 reveals dimerization-induced activation as a novel mechanism of nuclear receptor activation. Mol. Cell. Biol. 17:3977–3986.
   PubMedGoogle Scholar
• Willy, P. J., and J. Mangelsdorf 1998. Nuclear orphan receptors: the search for novel ligands and signaling pathways Hormones and signaling In B. W. O’Malley (ed.), 1:307–358 Academic Press, San Diego, Calif.
   Google Scholar
• Willy, P. J., and J. Mangelsdorf 1997. Unique requirements for retinoid-dependent transcriptional activation by the orphan receptor LXR. Genes Dev. 11:289–298.
   PubMedGoogle Scholar