Probing the structure and function of the estrogen receptor ligand binding domain by analysis of mutants with altered transactivation characteristics

Molecular and Cellular Biology

Volumn 17, Issue 8, 1997, Pages 4644-4653

  Eng, Frank C S ^a   Lee, Han S ^a   Ferrara, John ^a   Willson, Timothy M ^b   White, John H ^a  

^a MCGILL UNIVERSITY   (Canada)

^b GLAXOSMITHKLINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 METHOXYESTRONE; ANTIESTROGEN; ESTRADIOL; ESTROGEN RECEPTOR; ESTRONE; RETINOIC ACID RECEPTOR;

AMINO ACID SUBSTITUTION; ARTICLE; CONFORMATIONAL TRANSITION; GENETIC SCREENING; HORMONAL REGULATION; HORMONE RECEPTOR INTERACTION; LIGAND BINDING; PRIORITY JOURNAL; PROTEIN DOMAIN; SACCHAROMYCES CEREVISIAE; STRUCTURE ACTIVITY RELATION; TRANSACTIVATION;

SACCHAROMYCES CEREVISIAE;

EID: 0030853941     PISSN: 02707306     EISSN: None     Source Type: Journal    
DOI: 10.1128/MCB.17.8.4644     Document Type: Article

References (61)

1. Beato, M., M. Truss, and S. Chavez. 1996. Control of transcription by steroid hormones. Ann. N.Y. Acad. Sci. 784:93-123.
2. Beekman, J. M., G. F. Allan, S. Y. Tsai, M.-J. Tsai, and B. W. O'Malley. 1993. Transcriptional activation by the estrogen receptor requires a conformational change in the ligand binding domain. Mol. Endocrinol. 7:1266-1274.
3. Bocquel, M. T., V. Kumar, C. Stricker, P. Chamhon, and H. Gronemeyer. 1989. The contribution of tbe N- and C-terminal regions of steroid receptors to activation of transcription is both receptor and cell-specific. Nucleic Acids Res. 17:2581-2595.
4. Bourguet, W., M. Ruff, P. Chambon, H. Gronemeyer, and D. Moras. 1995. Crystal structure of the ligand-binding domain of the human nuclear receptor RXR-alpha. Nature 375:377-382.
5. Chambraud, B., M. Berry, G. Redeuilh, P. Chamhon, and E. E. Baulieu. 1990. Several regions of human estrogen receptor are involved in the formation of receptor-heat shock protein 90 complexes. J. Biol. Chem. 265: 20686-201691.
6. Chen, J. D., and R. M. Evans. 1995. A transcriptional co-repressor that interacts with nuclear hormone receptors. Nature 377:454-457.
7. Danielian, P. S., R. White, J. A. Lees, and M. G. Parker. 1992. Identification of a conserved region required for hormone dependent transcriptional activation by steroid hormone receptors. EMBO J. 3:1025-1033.
8. Evans, R. M., and S. M. Hollenberg. 1988. Zinc fingers: gilt by association. Cell 52:1-3.
9. Forman, B. M., P. Tontonoz, J. Chen, R. P. Brun, B. M. Spiegelman, and R. M. Evans. 1995. 15-Deoxy-delta 12, 14-prostaglandin J2 is a ligand for the adipocyte determination factor PPAR gamma. Cell 83:803-812.
10. Fuxe, K., A. Cintra, L. F. Agnati, A. Harfstrand, A. C. Wikstrom, S. Okret, M. Zoli, L. S. Miller, J. L. Greene, and J. A. Gustafsson. 1987. Studies on the cellular localization and distribution of glucocorticoid receptor and estrogen receptor immunoreactivity in the central nervous system of the rat and their relationship to the monoaminergic and peptidergic neurons of the brain. J. Steroid Biochem, 27:159-170.
11. Green, S., and P. Chambon. 1987. Oestradiol induction of a glucocortieoidresponsive gene by a chimaeric receptor. Nature 325:75-78.
12. Green, S., I. lssemann, and E. Sheer. 1988. A versatile in vivo and in vitro eukaryotic expression vector for protein engineering. Nucleic Acids Res. 16:369.
13. Greene, G. L., and M. F. Press. 1986. Structure and dynamics of the estrogen receptor. J. Steroid Biochem. 24:1-7.
14. Gronemeyer, H. 1991. Transcription activation by estrogen and progesterone receptors. Annu. Rev. Genet. 25:89-123.
15. Hard, T., E. Kellenbach, R. Boelens, B. A. Maler, K. Dahlman, L. P. Freedman, J. Carlstedt-Duke, K. R. Yamamoto, J. A. Gustafsson, and R. Kaptein. 1990. Solution structure of the glucocorticoid receptor DNA-binding domain. Science 249:157-160.
16. Hollenberg, S. M., and R. M. Evans. 1988. Multiple and cooperative transactivation domains of the human glucocorticoid receptor. Cell 55:899-906.
17. Holtje, H. D., and N. Dall. 1993. A molecular modelling study on the hormone binding site of the estrogen receptor. Pharmazie 48:243-249.
18. Horlein, A. J., A. M. Naar, T. Heinzel, J. Torchia, B. Gloss, R. Kurokawa, A. Ryan, Y. Kamei, M. Soderstrom, and C. K. Glass. 1995. Ligand-independent repression by the thyroid hormone receptor mediated by a nuclear receptor co-repressor. Nature 377:397-404.
19. Ince, B. A., Y. Zhuang, C. K. Wrenn, D. J. Shapiro, and B. S. Katzenellenbogen. 1993. Powerful dominant negative mutants of the human estrogen receptor. J. Biol. Chem. 268:14026-14032.
20. Ishibashi, T., Y. Nakabeppu, and M. Sekiguchi. 1994. Artificial control of nuclear translocation of DNA repair methyltransferase. J. Biol. Chem. 269: 7645-7650.
21. Kaiser, C., S. Michaselis, and A. Mitchell. 1994. Methods in yeast genetics. Cold Spring Harbor Laboratory Press, Cold Spring Harbor, N.Y.
22. Katzenellenbogen, B. S., B. Bhardwaj, H. Fang, B. A. Ince, F. Pakdel, J. C. Reese, D. Schodin, and C. K. Wrenn. 1993. Hormone binding and transcription activation by estrogen receptors: analyses using mammalian and yeast systems. J. Steroid Biochem. Mol. Biol. 47:39-48.
23. Kliewer, S. A., J. M. Lenhard, T. M. Willson, I. Patel, D. C. Morris, and J. M. Lehmann. 1995. A prostaglandin J2 metabolite binds peroxisome proliferator-activatcd receplor gamma and promotes adipocyte differentiation. Cell 83:813-819.
24. Korach, K. S. 1944. Insights from the study of animals lacking functional estrogen receptor. Science 266:1524-1527.
25. Knthary, R. S. Clapoff, S. Darling. M. D. Perry, L. A. Moran, and J. Rossant. 1989, Inducible expression of an hsp68-lacZ hybrid gene in transgenic mice. Development 105:707-714.
26. Krust, A., S. Green, P. Argos, V. Kumar, P. Walter, J. M. Bornert, and P. chambon. 1986. The chicken oestrogen receptor sequence: homology with v-erbA and the human oestrogen and clucocorticoid receptors. EMBO J. 5:891-897.
27. Kumar, V., S. Green, G. Stack, M. Berry, J. R. Jin, and P. Chambon. 1987. Functional domains of the human estrogen receptor. Cell 51:941-951.
28. Lee, H. S., J. P. Aumais, and J. H. White, 1996. Hormone-dependent transactivation by estrogen receptor chimeras that do not interact with hsp90: evidence for Transcriptional repressors. J. Biol. Chem. 271:25727-25730.
29. Lubahn, D. B., J. S. Moyer, T. S. Golding, J. F. Couse, K. S. Korach, and O. Smithies. 1993. Alteration of reproductive function hut not prenatal sexual development after insertional disruption of the mouse estrogen receptor gene. Proc. Natl. Acad. Sci. USA 90:11162-11166.
30. Mader, S., P. Chamhon, and J. H. While. 1993. Defining a minimal estrogen receptor DNA binding domain. Nucleic Acids Res. 21:1125-1132.
31. Mangelsdorf, D. J., and R. M. Evans. 1995. The RXR heterodimers and orphan receptors. Cell 83:841-850.
32. Mangelsdorf, D. J., C. Thummel, M. Beato, P. Herrlich, G. Schutz, K. Umesono, B. Blumberg, P. Kastner, M. Mark, P. Chambon, et al. 1995. The nuclear receptor superfamily: the second decade. Cell 83:835-839.
33. Metzger, D., M. Berry, S. Ali, and P. Chambon. 1995. Effect of antagonists on DNA binding properties of the human estrogen receptor in vitro and in vivo. Mol. Endocrinol. 9:579-591.
34. Metzger, D., R. Losson, J. M. Bornert, Y. Lemoine, and P. Chambon. 1992. Promoter specificity of the two transcriptional activation functions of the human oestrogen receptor in yeast. Nucleic Acids Res. 20:2813-2817.
35. Metzger, D., J. H. White, and P. Chambon. 1988. The human oestrogen receptor functions in yeast. Nature 334:31-36.
36. Montano, M. M., E. Ekena, K. D. Krueger, A. L. Keller, and B. S. Katzenellenbogen. 1996. Human estrogen receptor ligand activity inversion mutants: receptors that interpret antiestrogens as estrogens and estrogens as antiestrogens and discriminate among different antiestrogens. Mol. Endocrinol. 10:230-242.
37. Montano, M. M., V. Muller, A. Trobaugh, and B. S. Katzenellenbogen. 1995. The carboxy terminal F domain of the human estrogen receptor: role in transeriptional activity of the receptor and the effectiveness of antiestrogens as estrogen antagonists. Mol. Endocrinol. 9:814-825.
38. Nathan, D. F., and S. Lindquist. 1995. Mutational analysis of Hsp90 function: interactions with a steroid receptor and a protein kinase. Mol. Cell. Biol. 15:3917-3925.
39. Nordeen, S. K. 1988. Luciferase reporter gene vectors for analysis of promoters and enhancers. BioTechniques 6:454-458.
40. Picard, D., B. Khursheed, M. J. Garabedian, M. G. Fortin, S. Lindquist, and K. R. Yamamoto. 1990. Reduced levels of hsp90 compromise steroid receptor action in vivo. Nature 348:166-168.
41. Pierrat, B., D. M. Heery, P. Chambon, and R. Losson. 1994. A highly conserved region in the hormone-binding domain of the human estrogen receptor functions as an efficient transactivation domain in yeast. Gene 143:193-200.
42. Press, M. F., N. A. Nousek-Goebl, M. Bur, and G. L. Greene. 1986. Estrogen receptor localization in the female genital tract. Am. J. Pathol. 123:280-292.
43. Renaud, J. P., N. Rochel, M. Ruff, V. Vivat, P. Chambon, H. Gronemeyer, and D. Moras. 1995. Crystal structure of the RAR-gamma ligand-binding domain hound to all-trans retinoic acid. Nature 378:681-689.
44. Schwabe, J. W., D. Neuhaus, and D. Rhodes. 1990. Solution structure of the DNA-binding domain of the oestrogen receptor. Nature 348:458-461.
45. Segnitz, B., and U. Gehring. 1995. Suhunit structure of the nonactivated human estrogen receptor. Proe. Natl. Acad. Sci. USA 92:2179-2183.
46. Sikorski, R. S., and P. Hieter. 1989. A system of shutlle vectors and yeast host strains designed for efficient manipulation of DNA in Saccharomyces cercvisiae. Genetics 122:19-27.
47. Smith, E. P., J. Boyd, G. R. Frank, H. Takahashi, R. M. Cohen, B. Specker, T. C. Williams, D. B. Lubahn, and K. S. Korach. 1994. Estrogen resistance caused by a mutation in the estrogen-receplor gene in a man. N. Engl. J. Med. 331:1056-1061.
48. Spee, J. H., W. M. de Vos. and O. P. Kuipers. 1993. Efficient random mutagenesis method with adjustable mutation frequency by use of PCR and dITP. Nucleic Acids Res. 21:777-778.
49. Tora, L., H. Gronemeyer, B. Turcotte, M. P. Gauh, and P. Chambon. 1988. The N-terminal region of the chicken progesterone receptor specifies target gene activation. Nature 333:185-188.
50. Tora, L., A. Mullick, D. Metzger, M. Ponglikitmongkol, I. Park, and P. Chambon. 1989. The cloned human oestrogen receptor contains a mutation which alters its hormone binding properties. EMBO J. 8:1981-1986.
51. Tora, L., J. White, C. Brou, D. Tasset, N. Webster, E. Scheer, and P. Chambon. 1989. The human estrogen receptor has two independent nonacidic transcriptional activation functions. Cell 59:4771-487.
52. Tzukerman, M., X. K. Zhang, T. Hermann, K. N. Wills, G. Graupner, and M. Pfahl. 1990. The human estrogen receptor has transcriptional activator and repressor functions in the absence of ligand. New Biol. 2:613-620.
53. Vegeto, E., G. F. Allan, W. T. Schrader, M. J. Tsai, D. P. McDonnell, and B. W. O'Malley. 1992. The mechanism of RU486 antagonism is dependent on the conformation of the carboxy-terminal tail of the human progesterone receptor. Cell 69:703-713.
54. Wagner, R. L., J. W. Apriletti, M. E. McGrath, B. L. West, J. D. Baxter, and R. J. Fletterick. 1995. A structural role for hormone in the thyroid hormone receptor. Nature 378:690-697.
55. Wahli, W., and E. Martinez. 1991. Superfamily of steroid nuclear receptors: positive and negative regulators of gene expression. FASEB J. 5:2243-2249.
56. Webster, N. J., S. Green, J. R. Jin, and P. Chambon. 1988. The hormonebinding domains of the estrogen and glucocorticoid receptors contain an inducible transcription activation function. Cell 54:199-207.
57. Weis, K. E., K. Ekena, J. A. Thomas, G. Lazennec, and B. S. Katzenellenbogen. 1996. Constitutively active human estrogen receptors containing amino acid substitutions for tyrosine 537 in the receptor protein. Mol. Endocrinol. 10:1388-1398.
58. White, J. H., D. Metzger, and P. Chambon. 1988. Expression and function of the human estrogen receptor in yeast. Cold Spring Harbor Symp. Quant. Biol. 53:819-828.
59. Wrenn, C. K., and B. S. Katzenellenbogen. 1993. Structure-function analysis of the hormone binding domain of the human estrogen receptor by region-specific mutagenesis and phenotypic screening in yeast. J. Biol. Chem. 268: 24089-24098.
60. Wurtz, J. M., W. Bourguet, J. P. Renaud, V. Vivat, P. Chambon. D. Moras, and H. Gronemeyer. 1996. A canonical structure for the ligand-hinding domain of nuclear receptors. Nature Struct. Biol. 3:87-94.
61. Zhuang, Y., B. S. Katzenellenbogen, and D. J. Shapiro. 1995. Estrogen receptor mutants which do not bind 17 beta-estradiol dimerize and hind to the estrogen response element in vivo. Mol. Endocrinol. 9:457-466.