The three-dimensional structures of antagonistic and agonistic forms of the glucocorticoid receptor ligand-binding domain: RU-486 induces a transconformation that leads to active antagonism

Journal of Biological Chemistry

Volumn 278, Issue 25, 2003, Pages 22748-22754

  Kauppi, Björn ^a   Jakob, Clarissa ^b   Färnegårdh, Mathias ^a   Yang, Jie ^b   Ahola, Harri ^a   Alarcon, Maria ^a   Calles, Karin ^a   Engström, Owe ^a   Harlan, John ^b   Muchmore, Steven ^b   Ramqvist, Anna Karin ^a   Thorell, Susanne ^a   Öhman, Lars ^a   Greer, Jonathan ^b   Gustafsson, Jan Åke ^c   Carlstedt Duke, Jan ^c   Carlquist, Mats ^a  

^a Karo Bio   (Sweden)

^b ABBOTT LABORATORIES   (United States)

^c KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

CHEMICAL BONDS; CRYSTAL STRUCTURE; CRYSTALLOGRAPHY; DIMERS; MOLECULAR BIOLOGY;

LIGANDS;

BIOCHEMISTRY;

AMINO ACID; CYSTEINE; DIMER; GLUCOCORTICOID ANTAGONIST; GLUCOCORTICOID RECEPTOR; GLUCOCORTICOID RECEPTOR AGONIST; LIGAND; MIFEPRISTONE; PEPTIDE; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; ARTICLE; CARBOXY TERMINAL SEQUENCE; COVALENT BOND; CRYSTAL STRUCTURE; CRYSTALLOGRAPHY; DISULFIDE BOND; DRUG RECEPTOR BINDING; DRUG STRUCTURE; LIGAND BINDING; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN STRUCTURE; SEQUENCE ANALYSIS; STRUCTURE ANALYSIS;

EID: 0038265311     PISSN: 00219258     EISSN: None     Source Type: Journal    
DOI: 10.1074/jbc.M212711200     Document Type: Article

References (43)

1. Wrange, O., and Gustafsson, J. A. (1978) J. Biol. Chem. 253, 856-865
2. Carlstedt-Duke, J., Okret, S., Wrange, O., and Gustafsson, J. A. (1982) Proc. Natl. Acad. Sci. U. S. A. 79, 4260-4264
3. Payvar, F., Wrange, O., Carlstedt-Duke, J., Okret, S., Gustafsson, J. A., and Yamamoto, K. R. (1981) Proc. Natl. Acad. Sci. U. S. A. 78, 6628-6632
4. Payvar, F., Firestone, G. L., Ross, S. R., Chandler, V. L., Wrange, O., Carlstedt-Duke, J., Gustafsson, J. A., and Yamamoto, K. R. (1982) J. Cell. Biochem. 19, 241-247
5. Miesfeld, R., Okret, S., Wikstrom, A. C., Wrange, O., Gustafsson, J. A., and Yamamoto, K. R. (1984) Nature 312, 779-781
6. Hard, T., Kellenbach, E., Boelens, R., Maler, B. A., Dahlman, K., Freedman, L. P., Carlstedt-Duke, J., Yamamoto, K. R., Gustafsson, J. A., and Kaptein, R. (1990) Science 249, 157-160
7. Hard, T., Kellenbach, E., Boelens, R., Kaptein, R., Dahlman, K., Carlstedt-Duke, J., Freedman, L. P., Maler, B. A., Hyde, E. I., and Gustafsson, J. A. (1990) Biochemistry 29, 9015-9023
8. Williams, S. P., and Sigler, P. B. (1998) Nature 393, 392-396
9. Matias, P. M., Donner, P., Coelho, R., Thomaz, M., Peixoto, C., Macedo, S., Otto, N., Joschko, S., Scholz, P., Wegg, A., Basler, S., Schafer, M., Egner, U., and Carrondo, M. A. (2000) J. Biol. Chem. 275, 26164-26171
10. Bledsoe, R. K., Montana, V. G., Stanley, T. B., Delves, C. J., Apolito, C. J., McKee, D. D., Consler, T. G., Parks, D. J., Stewart, E. L., Willson, T. M., Lambert, M. H., Moore, J. T., Pearce, K. H., and Xu, H. E. (2002) Cell 110, 93-105
11. Wahli, W., and Martinez, E. (1991) Faseb J 5, 2243-2249
12. Myles, K., and Funder, J. W. (1996) Am. J. Physiol. 270, E601-607
13. Funder, J. W. (1997) Annu. Rev. Med. 48, 231-240
14. Fuller, P. J., Lim-Tio, S. S., and Brennan, F. E. (2000) Kidney Int. 57, 1256-1264
15. Simons, S. S., Jr. (1994) Vitam. Horm. 49, 49-130
16. Lind, U., Carlstedt-Duke, J., Gustafsson, J. A., and Wright, A. P. (1996) Mol. Endocrinol. 10, 1358-1370
17. Lind, U., Greenidge, P., Gustafsson, J. A., Wright, A. P., and Carlstedt-Duke, J. (1999) J. Biol. Chem. 274, 18515-18523
18. Lind, U., Greenidge, P., Gillner, M., Koehler, K. F., Wright, A., and Carlstedt-Duke, J. (2000) J. Biol. Chem. 275, 19041-19049
19. Cadepond, F., Ulmann, A., and Baulieu, E. E. (1997) Annu. Rev. Med. 48, 129-156
20. Pandit, S., Geissler, W., Harris, G., and Sitlani, A. (2002) J. Biol. Chem. 277, 1538-1543
21. Gass, E. K., Leonhardt, S. A., Nordeen, S. K., and Edwards, D. P. (1998) Endocrinology 139, 1905-1919
22. Wang, Z., Frederick, J., and Garabedian, M. J. (2002) J. Biol. Chem. 277, 26573-26580
23. Schulz, M., Eggert, M., Baniahmad, A., Dostert, A., Heinzel, T., and Renkawitz, R. (2002) J. Biol. Chem. 277, 26238-26243
24. Rogatsky, I., Hittelman, A. B., Pearce, D., and Garabedian, M. J. (1999) Mol. Cell. Biol. 19, 5036-5049
25. Leonhardt, S. A., and Edwards, D. P. (2002) Exp. Biol. Med. 227, 969-980
26. 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
27. Otwinowski, Z., and Minor, W. (1997) in Methods in Enzymology (Carter, J. C. W., and Sweet, R. M., eds) Vol. 276, pp. 307-326, Academic Press, San Diego, CA
28. Collaborative Computational Project, Number 4 (1994) Acta Crystallogr Sect D Biol. Crystallogr. 50, 760-763
29. Brünger, A. T., Adams, P. D., Clore, G. M., DeLano, W. L., Gros, P., Grosse-Kunstleve, R. W., Jiang, J. S., Kuszewski, J., Nilges, M., Pannu, N. S., Read, R. J., Rice, L. M., Simonson, T., and Warren, G. L. (1998) Acta Crystallogr. Sect. D Biol. Crystallogr. 54, 905-921
30. Garabedian, M. J., and Yamamoto, K. R. (1992) Mol. Biol. Cell 3, 1245-1257
31. Kleywegt, G. J. (1995) CCP4/ESF-EACBM Newsletter on Protein Crystallography, Vol. 31, pp. 45-50, Daresbury Laboratory, Daresbury, UK
32. Jones, T. A., Zou, J. Y., Cowan, S. W., and Kjeldgaard, M. (1991) Acta Crystallogr. Sect. A 47, 110-119
33. Kleywegt, G. J., Zou, J. Y., Kjeldgaard, M., and Jones, T. A. (2001) in International Tables for Crystallography (Rossmann, M. G., and Arnold, E., eds) Vol. F, pp. 353-356, 366-367, Kluwer Academic Publishers, Dordrecht, The Netherlands
34. Kleywegt, G. J., and Jones, T. A. (1996) Structure 4, 1395-1400
35. Kleywegt, G. J. (1996) Acta Crystallogr. Sect. D Biol. Crystallogr. 52, 842-857
36. Ray, D. W., Suen, C. S., Brass, A., Soden, J., and White, A. (1999) Mol. Endocrinol. 13, 1855-1863
37. Tanenbaum, D. M., Wang, Y., Williams, S. P., and Sigler, P. B. (1998) Proc. Natl. Acad. Sci. U. S. A. 95, 5998-6003
38. Carlstedt-Duke, J., Stromstedt, P. E., Persson, B., Cederlund, E., Gustafsson, J. A., and Jornvall, H. (1988) J. Biol. Chem. 263, 6842-6846
39. Chakraborti, P. K., Garabedian, M. J., Yamamoto, K. R., and Simons, S. S., Jr. (1991) J. Biol. Chem. 266, 22075-22078
40. Chakraborti, P. K., Garabedian, M. J., Yamamoto, K. R., and Simons, S. S., Jr. (1992) J. Biol. Chem. 267, 11366-11373
41. 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
42. Savory, J. G., Prefontaine, G. G., Lamprecht, C., Liao, M., Walther, R. F., Lefebvre, Y. A., and Hache, R. J. (2001) Mol. Cell. Biol. 21, 781-793
43. DeLano, W. L. (2001) The PyMol User's Manual, DeLano Scientific, San Carlos, CA