Ligand-independent activation of the estrogen receptors α and β by mutations of a conserved tyrosine can be abolished by antiestrogens

Cancer Research

Volumn 58, Issue 5, 1998, Pages 877-881

  Tremblay, Gilles B ^a   Tremblay, André ^a   Labrie, Fernand ^c   Giguère, Vincent ^a,b  

^a ROYAL VICTORIA HOSPITAL   (Canada)

^b MCGILL UNIVERSITY   (Canada)

^c UNIVERSITÉ LAVAL   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

4 HYDROXYTAMOXIFEN; ACOLBIFENE; ANTIESTROGEN; ESTRADIOL; ESTROGEN RECEPTOR; FULVESTRANT; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; BREAST CANCER; CELL STRAIN COS1; CONTROLLED STUDY; GENE MUTATION; HELA CELL; HORMONE RESPONSIVE ELEMENT; HUMAN; HUMAN CELL; NONHUMAN; PRIORITY JOURNAL; PROMOTER REGION; TRANSACTIVATION;

ANIMALS; COS CELLS; ESTROGEN ANTAGONISTS; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; HUMANS; LIGANDS; MUTATION; RECEPTORS, ESTROGEN; SIGNAL TRANSDUCTION; TYROSINE;

EID: 0032031082     PISSN: 00085472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (40)

1. Evans, R. M. The steroid and thyroid hormone receptor superfamily. Science (Washington DC), 240: 889-895, 1988.
2. Tora, L., White, J., Brou, C., Tasset, D., Webster, N., Scheer, E., and Chambon, P. The human estrogen receptor has two independent nonacidic transcriptional activation functions. Cell, 59: 477-487, 1989.
3. Lees, J. A., Fawell, S. E., and Parker, M. G. Identification of two transactivation domains in the mouse oestrogen receptor. Nucleic Acids Res., 17: 5477-5488, 1989.
4. Wurtz, J. M., Bourguet, W., Renaud, J. P., Vivat, V., Chambon, P., Moras, D., and Gronemeyer, H. A canonical structure for the ligand-binding domain of nuclear receptors. Nat. Struct. Biol., 3: 87-94, 1996.
5. Brzozowski, A. M., Pike, A. C. W., Dauter, Z., Hubbard, R. E., Bonn, T., Engström, L., Greene, G. L., Gustafsson, J-Å., and Carlquist, M. Molecular basis of agonism and antagonism in the oestrogen receptor. Nature (Lond.), 389: 753-758, 1997.
6. Oñate, S. A., Tsai, S. Y., Tsai, M-J., and O'Malley, B. W. Sequence and characterization of a coactivator for the steroid hormone receptor superfamily. Science (Washington DC), 270: 1354-1357, 1995.
7. Kamei, Y., Xu, L., Heinzel, T., Torchia, J., Kurokawa, R., Gloss, B., Lin, S-C., Heyman, R. A., Rose, D. W., Glass, C. K., and Rosenfeld, M. G. A CBP integrator complex mediates transcriptional activation and AP-1 inhibition by nuclear receptors. Cell, 85: 403-414, 1996.
8. Anzick, S. L., Kononen, J., Walker, R. L., Azorsa, D. O., Tanner, M. M., Guan, X-Y., Sauter, G., Kallioniemi, O-P., Trent, J. M., and Meltzer, P. S. AIB1, a steroid receptor coactivator amplified in breast and ovarian cancer. Science (Washington DC), 277: 965-968, 1997.
9. White, R., Sjöberg, M., Kalkhoven, E., and Parker, M. G. Ligand-independent activation of the estrogen receptor by mutation of a conserved tyrosine. EMBO J., 16: 1427-1435, 1997.
10. Danielian, P. S., White, R., Lees, J. A., and Parker, M. G. Identification of a conserved region required for hormone dependent transcriptional activation by steroid hormone receptors. EMBO J., 11: 1025-1033, 1992.
11. Heery, D. M., Kalkhoven, E., Hoare, S., and Parker, M. G. A signature motif in transcriptional co-activators mediates binding to nuclear receptors. Nature (Lond.), 387: 733-736, 1997.
12. Ignar-Trowbridge, D. M., Teng, C. T., Ross, K. A., Parker, M. G., Korach, K. S., and McLachlan, J. A. Peptide growth factors elicit estrogen receptor-dependent transcriptional activation of an estrogen-responsive element. Mol. Endocrinol., 7: 992-998, 1993.
13. Aronica, S. M., and Katzenellenbogen, B. S. Stimulation of estrogen receptor-mediated transcription and alteration in the phosphorylation state of the rat uterine estrogen receptor by estrogen, cyclic adenosine monophosphate, and insulin-like growth factor-I. Mol. Endocrinol., 7: 743-752, 1993.
14. Bunone, G., Briand, P-A., Miksicek, R. J., and Picard, D. Activation of the unliganded estrogen receptor by EGF involves the MAP kinase pathway and direct phosphorylation. EMBO J., 15: 2174-2183, 1996.
15. Kato, S., Endoh, H., Masuhiro, Y., Kitamoto, T., Uchiyama, S., Sasaki, H., Masushige, S., Gotoh, Y., Nishida, E., Kawashima, H., Metzger, D., and Chambon, P. Activation of the estrogen receptor through phosphorylation by mitogen-activated protein kinase. Science (Washington DC), 270: 1491-1494, 1995.
16. Auricchio, F., Migliaccio, A., Di Domenico, M., and Nola, E. Oestradiol stimulates tyrosine phosphorylation and hormone binding activity of its own receptor in a cell free system. EMBO J., 6: 2923-2929, 1987.
17. Pietras, R. J., Arboleda, J., Reese, D. M., Wongvipat, N., Pegram, M. D., Ramos, L., Gorman, C. M., Parker, M. G., Sliwkowski, M. X., and Slamon, D. J. HER-2 tyrosine kinase pathway targets estrogen receptor and promotes hormone-independent growth in human breast cancer cells. Oncogene, 10: 2435-2446, 1995.
18. Arnold, S. F., Vorojeikkina, D. P., and Notides, A. C. Phosphorylation of tyrosine 537 on the human estrogen receptor is required for binding to an estrogen response element. J. Biol. Chem., 270: 30205-30212, 1995.
19. Arnold, S. F., Obourn, J. D., Jaffe, H., and Notides, A. C. Phosphorylation of the human estrogen receptor on tyrosine-537 in vivo by Src family tyrosine kinases in vitro. Mol. Endocrinol., 9: 24-33, 1995.
20. Weis, K. E., Ekena, K., Thomas, J. A., Lazennec, G., and Katzenellenbogen, B. S. Constitutively active human estrogen receptors containing amino acid substitutions for tyrosine 537 in the receptor protein. Mol. Endocrinol., 10: 1388-1398, 1996.
21. Lazennec, G., Ediger, T. R., Petz, L. N., Nardulli, A. M., and Katzenellenbogen, B. S. Mechanistic aspects of estrogen receptor activation probed with constitutively active estrogen receptors: correlations with DNA and coregulator interactions and receptor conformational changes. Mol. Endocrinol., 11: 1375-1386, 1997.
22. Tremblay, G. B., Tremblay, A., Copeland, N. G., Gilbert, D. J., Jenkins, N. A., Labrie, F., and Giguère, V. Cloning, chromosomal localization and functional analysis of the murine estrogen receptor β. Mol. Endocrinol., 11: 353-365, 1997.
23. Mosselman, S., Polman, J., and Dijkema, R. ERβ: identification and characterization of a novel human estrogen receptor. FEBS Lett., 392: 49-53, 1996.
24. Kuiper, G. G. J. M., Enmark, E., Pelto-Huikko, M., Nilsson, S., and Gustafsson, J-Å. Cloning of a novel estrogen receptor expressed in rat prostate and ovary. Proc. Natl. Acad. Sci. USA, 93: 5925-5930, 1996.
25. Paech, K., Webb, P., Kuiper, G. G. J. M., Nilsson, S., Gustafsson, J-Å., Kushner, P. J., and Scanlan, T. S. Differential ligand activation of estrogen receptors ERα and ERβ at AP1 sites. Science (Washington DC), 277: 1508-1510, 1997.
26. Tremblay, A., Tremblay, G. B., Labrie, C., Labrie, F., and Giguère, V. EM-800, a novel antiestrogen, acts as a pure antagonist of the transcriptional functions of estrogen receptors α and β. Endocrinology, 139: 111-118, 1998.
27. Kuiper, G. G. J. M., Carlsson, B., Grandien, K., Enmark, E., Haggblad, J., Nilsson, S., and Gustafsson, J. A. Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors α and β. Endocrinology, 138: 863-870, 1997.
28. Pettersson, K., Grandien, K., Kuiper, G. G. J. M., and Gustafsson, J-Å. Mouse estrogen receptor β forms estrogen response element-binding heterodimers with estrogen receptor α. Mol. Endocrinol., 11: 1486-1496, 1997.
29. Cowley, S. M., Hoare, S., Mosselman, S., and Parker, M. G. Estrogen receptors α and β form heterodimers on DNA. J. Biol. Chem., 272: 19858-19862, 1997.
30. Pace, P., Taylor, J., Suntharalingam, S., Coombes, R. C., and Ali, S. Human estrogen receptor β binds DNA in a manner similar to and dimerizes with estrogen receptor α. J. Biol. Chem., 272: 25832-25838, 1997.
31. Dotzlaw, H., Leygue, E., Watson, P. H., and Murphy, L. C. Expression of estrogen receptor-β In human breast tumors. J. Clin. Endocrinol. Metab., 82: 2371-2374, 1997.
32. Fuqua, S. A., and Wolf, D. M. Molecular aspects of estrogen receptor variants in breast cancer. Breast Cancer Res. Treat., 35: 233-241, 1995.
33. Zhang, Q. X., Borg, A., Wolf, D. M., Oesterreich, S., and Fuqua, S. A. W. An estrogen receptor mutant with strong hormone-independent activity from a metastatic breast cancer. Cancer Res., 57: 1244-1249, 1997.
34. Gauthier, S., Caron, B., Cloutier, J., Dory, Y. L., Favre, A., Larouche, D., Mailhot, J., Ouellet, C., Schwerdtfeger, A., Leblanc, G., Martel, C., Simard, J., Mérand, Y., Bélanger, A., Labrie, C., and Labrie, F. (S)-(+)[4-[7-2,2-dimethyl-1-oxopropoxy)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy] phenyl]-2H-1-1benzopyran-3-yl]phenyl]-2,2-dimethylpropanoate (EM-800), a highly potent non-steroidal antiestrogen. J. Med. Chem., 40: 2117-2122, 1997.
35. Berry, M., Nunez, A-M., and Chambon, P. Estrogen-responsive element of the human pS2 gene is an imperfectly palindromic sequence. Proc. Natl. Acad. Sci. USA, 86: 1218-1222, 1989.
36. Fuqua, S. A., Chamness, G. C., and McGuire, W. L. Estrogen receptor mutations in breast cancer. J. Cell. Biochem., 51: 135-139, 1993.
37. Madsen, M. W., Reiter, B. E., Larsen, S. S., Briand, P., and Lykkesfeldt, A. E. Estrogen receptor messenger RNA splice variants are not involved in antiestrogen resistance in sublines of MCF-7 human breast cancer cells. Cancer Res., 57: 585-589, 1997.
38. Garcia, T., Sanchez, M., Cox, J. L., Shaw, P. A., Ross, J. B. A., Lehrer, S., and Schachter, B. Identification of a variant form of the human estrogen receptor with an amino acid replacement. Nucleic Acids Res., 17: 8364, 1989.
39. Karnik, P. S., Kullkarni, S., Liu, X. P., Budd, G. T., and Bukowski, R. M. Estrogen receptor mutations in tamoxifen-resistant breast cancer. Cancer Res., 54: 349-353, 1994.
40. Roodi, N , Bailey, L. R., Kao, W-Y., Verrier, C. S., Yee, C. J., Dupont, W. D., and Parl, F. F. Estrogen receptor gene analysis in estrogen receptor-positive and receptor-negative primary breast cancer. J. Natl. Cancer Inst., 87: 446-451, 1995.