Crystal Structure of a Mutant hERα Ligand-binding Domain Reveals Key Structural Features for the Mechanism of Partial Agonism

Journal of Biological Chemistry

Volumn 276, Issue 18, 2001, Pages 15059-15065

  Gangloff, Monique ^a   Ruff, Marc ^a   Eiler, Sylvia ^a   Duclaud, Sylvie ^a   Wurtz, Jean Marie ^a   Moras, Dino ^a  

^a INSTITUT DE GÉNÉTIQUE ET DE BIOLOGIE MOLÉCULAIRE ET CELLULAIRE   (France)

Author keywords

[No Author keywords available]

Indexed keywords

CONFORMATIONS; CRYSTAL STRUCTURE; MUTAGENESIS; PROTEINS;

LIGAND BINDING DOMAIN;

BIOCHEMISTRY;

4 HYDROXYTAMOXIFEN; ESTRADIOL; ESTROGEN RECEPTOR ALPHA; MUTANT PROTEIN; PARTIAL AGONIST; RALOXIFENE; ANTIESTROGEN; ESTROGEN RECEPTOR; LIGAND;

ANIMAL CELL; ARTICLE; CELL STRAIN COS1; CRYSTAL STRUCTURE; HORMONE RECEPTOR INTERACTION; LIGAND BINDING; MOLECULAR STABILITY; NONHUMAN; PRIORITY JOURNAL; PROTEIN DOMAIN; STRUCTURE ACTIVITY RELATION; CHEMICAL STRUCTURE; CHEMISTRY; DRUG POTENTIATION; GENETICS; HUMAN; HYDROGEN BOND; METABOLISM; MOLECULAR CLONING; PROTEIN CONFORMATION; SITE DIRECTED MUTAGENESIS; X RAY CRYSTALLOGRAPHY;

ANIMALIA;

CLONING, MOLECULAR; CRYSTALLOGRAPHY, X-RAY; ESTROGEN ANTAGONISTS; ESTROGEN RECEPTOR ALPHA; HUMANS; HYDROGEN BONDING; LIGANDS; MODELS, MOLECULAR; MUTAGENESIS, SITE-DIRECTED; PROTEIN CONFORMATION; RECEPTORS, ESTROGEN;

EID: 0035805514     PISSN: 00219258     EISSN: None     Source Type: Journal    
DOI: 10.1074/jbc.M009870200     Document Type: Article

References (39)

1. Mangelsdorf, D. J., and Evans, R. M. (1995) Cell 83, 841-850
2. Katzenellenbogen, J. A., and Katzenellenbogen, B. S. (1996) Chem. Biol. 3, 529-536
3. McKenna, N. J., Lanz, R. B., and O'Malley, B. W. (1999) Endocr. Rev. 20, 321-344
4. Ruff, M., Gangloff, M., Wurtz, J. M., and Moras, D. (2000) Breast Cancer Res. 2, 353-359
5. Moras, D., and Gronemeyer, H. (1998) Curr. Opin. Cell Biol. 10, 384-391
6. Bourguet, W., Ruff, M., Chambon, P., Gronemeyer, H., and Moras, D. (1995) Nature 375, 377-382
7. Egea, P. F., Mitschler, A., Rochel, N., Ruff, M., Chambon, P., and Moras, D. (2000) EMBO J. 19, 2592-2601
8. Renaud, J. P., Rochel, N., Ruff, M., Vivat, V., Chambon, P., Gronemeyer, H., and Moras, D. (1995) Nature 378, 681-689
9. Darimont, B. D., Wagner, R. L., Apriletti, J. W., Stallcup, M. R., Kushner, P. J., Baxter, J. D., Fletterick, R. J., and Yamamoto, K. R. (1998) Genes Dev. 12, 3343-3356
10. Gampe, R. T., Jr., Montana, V. G., Lambert, M. H., Miller, A. B., Bledsoe, R. K., Milburn, M. V., Kliewer, S. A., Willson, T. M., and Xu, H. E. (2000) Mol. Cell 5, 545-555
11. Nolte, R. T., Wisely, G. B., Westin, S., Cobb, J. E., Lambert, M. H., Kurokawa, R., Rosenfeld, M. G., Willson, T. M., Glass, C. K., and Milburn, M. V. (1998) Nature 395, 137-143
12. Shiau, A. K., Barstad, D., Loria, P. M., Cheng, L., Kushner, P. J., Agard, D. A., and Greene, G. L. (1998) Cell 95, 927-937
13. Brzozowski, A. M., Pike, A. C., Dauter, Z., Hubbard, R. E., Bonn, T., Engstrom, O., Ohman, L., Greene, G. L., Gustafsson, J. A., and Carlquist, M. (1997) Nature 389, 753-758
14. Tanenbaum, D. M., Wang, Y., Williams, S. P., and Sigler, P. B. (1998) Proc. Natl. Acad. Sci. U. S. A. 95, 5998-6003
15. Pike, A. C., Brzozowski, A. M., Hubbard, R. E., Bonn, T., Thorsell, A. G., Engstrom, O., Ljunggren, J., Gustafsson, J. A., and Carlquist, M. (1999) EMBO J. 18, 4608-4618
16. Eiler, S., Gangloff, M., Duclaud, S., Moras, D., and Ruff, M. (2001) Protein Expression Purif., in press
17. MacGregor, J. I., and Jordan, V. C. (1998) Pharmacol. Rev. 50, 151-196
18. Katzenellenbogen, B. S., and Katzenellenbogen, J. A. (2000) Breast Cancer Res. 2, 335-344
19. Barkhem, T., Carlsson, B., Nilsson, Y., Enmark, E., Gustafsson, J., and Nilsson, S. (1998) Mol. Pharmacol. 54, 105-112
20. McInerney, E. M., Weis, K. E., Sun, J., Mosselman, S., and Katzenellenbogen, B. S. (1998) Endocrinology 139, 4513-4522
21. Otwinoswski, Z., and Minor, W. (1997) Methods Enzymol. 276, 307-326
22. Collaborative Computational Project No. 4 (1994) Acta Crystallogr. Sect. D Biol. Crystallogr. 50, 760-763
23. de la Fortelle, E., and Bricogne, G. (1997) Methods Enzymol. 276, 472-494
24. Brüger, A. T., Adams, P. D., Clore, G. M., Delano, W. L., Gros, P., Grosse-Kuntstleve, R. W., Jiang, J. S., Kuszewski, J., Nilges, M., Pannu, N. S., Read, R. J., Rice, M. L., Simonson, T., and Warren, G. L. (1998) Acta Crystallogr. Sect. D Biol. Crystallogr. 54, 905-921
25. Nichols, A., and Honig, B. (1991) J. Comp. Chem. 12, 435-445
26. Tora, L., Mullick, A., Metzger, D., Ponglikitmongkol, M., Park, I., and Chambon, P. (1989) EMBO J. 8, 1981-1986
27. Brou, C., Chaudhary, S., Davidson, I., Lutz, Y., Wu, J., Egly, J. M., Tora, L., and Chambon, P. (1993) EMBO J. 12, 489-499
28. Klein-Hitpass, L., Schorpp, M., Wagner, U., and Ryffel, G. U. (1986) Cell 46, 1053-1061
29. Chen, J. D., and Evans, R. M. (1995) Nature 377, 454-457
30. Rafestin-Oblin, M. E., Couette, B., Radanyi, C., Lombes, M., and Baulieu, E. E. (1989) J. Biol. Chem. 264, 9304-9309
31. Claire, M., Rafestin-Oblin, M. E., Michaud, A., Corvol, P., Venot, A., Roth-Meyer, C., Boisvieux, J. F., and Mallet, A. (1978) FEBS Lett. 88, 295-299
32. Dauvois, S., White, R., and Parker, M. G. (1993) J. Cell Sci. 106, 1377-1388
33. Devin-Leclerc, J., Meng, X., Delahaye, F., Leclerc, P., Baulieu, E. E., and Catelli, M. G. (1998) Mol. Endocrinol. 12, 842-854
34. Bourguet, W., Vivat, V., Wurtz, J. M., Chambon, P., Gronemeyer, H., and Moras, D. (2000) Mol. Cell 5, 289-298
35. Oberfield, J. L., Collins, J. L., Holmes, C. P., Goreham, D. M., Cooper, J. P., Cobb, J. E., Lenhard, J. M., Hull-Ryde, E. A., Mohr, C. P., Blanchard, S. G., Parks, D. J., Moore, L. B., Lehmann, J. M., Plunket, K., Miller, A. B., Milburn, M. V., Kliewer, S. A., and Willson, T. M. (1999) Proc. Natl. Acad. Sci. U. S. A. 96, 6102-6106
36. Hayashi, S., Hajiro-Nakanishi, K., Makino, Y., Eguchi, H., Yodoi, J., and Tanaka, H. (1997) Nucleic Acids Res. 25, 4035-4040
37. Okamoto, K., Tanaka, H., Ogawa, H., Makino, Y., Eguchi, H., Hayashi, S., Yoshikawa, N., Poellinger, L., Umesono, K., and Makino, I. (1999) J. Biol. Chem. 274, 10363-10371
38. Makino, Y., Tanaka, H., Dahlman-Wright, K., and Makino, I. (1996) Mol. Pharmacol. 49, 612-620
39. Morel, Y., and Barouki, R. (2000) Biochem. J. 348, 235-240