A systematic analysis of the AF-2 domain of human retinoic acid receptor α reveals amino acids critical for transcriptional activation and conformational integrity

FASEB Journal

Volumn 10, Issue 13, 1996, Pages 1524-1531

  Tate, Bonnie F ^a   Allenby, Gary ^c   Pérez, José R ^b   Levin, Arthur A ^d   Grippo, Joseph F ^a  

^a Hoffman La Roche Department of Metabolic Diseases   (United States)

^b HOFFMANN LA ROCHE INC   (United States)

^c QUEEN MARY UNIVERSITY OF LONDON   (United Kingdom)

^d ISIS PHARMACEUTICALS   (United States)

Author keywords

gel mobility shift assay; plasmid mutants; RARE; retinoic acids; transactivation

Indexed keywords

RETINOIC ACID RECEPTOR;

AMINO ACID METABOLISM; ANALYTIC METHOD; ARTICLE; CONFORMATIONAL TRANSITION; DIMERIZATION; DNA BINDING; GENE MUTATION; GENETIC TRANSCRIPTION; HUMAN; HUMAN CELL; LIGAND BINDING; MUTAGENESIS; PRIORITY JOURNAL; PROTEIN DOMAIN; RECEPTOR GENE; TRANSACTIVATION; TRANSCRIPTION INITIATION;

EID: 0029833187     PISSN: 08926638     EISSN: None     Source Type: Journal    
DOI: 10.1096/fasebj.10.13.8940298     Document Type: Article

References (33)

1. Kastner, P., Chambon, P., and Leid, M. (1994) Role of nuclear retinoic acid receptors in the regulation of gene expression. In Vitamin A in Health and Disease (Blomhoff, R., ed) pp. 189-238, Marcel Dekker, Inc., New York
2. Morriss-Kay, G. (1992) Retinoids in normal development and teratogenesis. Oxford University Press, New York
3. Sporn, M. B., Roberts, A. B., and Goodman, D. S. (1994) The Retinoids: Biology, Chemistry and Medicine. Raven Press, Ltd., New York
4. Evans, R. M. (1988) The steroid and thyroid hormone receptor superfamily. Science 240, 889-395
5. Green, S., and Chambon, P. (1988) Nuclear receptors enhance our understanding of transcription regulation. Trends Genet. 4, 309-314
6. Mangelsdorf, D.J., Umesono, K., and Evans, R. M. (1994) The retinoid receptors. In The Retinoids: Biology, Chemistry and Medicine (Sporn, M. B., Roberts, A. B., Goodman, D. S., ed) 2nd ed, pp. 319-349, Raven Press, Ltd., New York
7. Tate, B. F., Levin, A. A., and Grippo, J. F. (1994) The discovery of 9-cis retinoic acid: a hormone that binds the retinoid-X receptor. Trends Endocrinol. Metab. 5, 189-194
8. Leid, M., Kastner, P., and Chambon, P. (1992) Multiplicity generates diversity in the retinoic acid signalling pathways. Trends Biochem. Sci. 17, 427-433
9. Danielian, P. S., White, R., Lees, J. A., and Parker, M. G. (1992) Identification of a conserved region required for hormone dependent transcriptional activation by steroid hormone receptors. EMBO J. 11, 1025-1033
10. Cavaillès, V., Dauvois, S., Danielian, P. S., and Parker, M. G., (1994) Interaction of proteins with transcriptionally active estrogen receptors. Proc. Natl. Acad. Sci. USA 91, 10009-10013
11. Barettino, D., Vivanco Ruiz, M. d.M., and Stunnenberg, H. G. (1994) Characterization of the ligand-dependenl transactivation domain of thyroid hormone receptor. EMBO J. 13, 3039-3049
12. Leng, X., Blanco, J., Tsai, S. Y., Ozato, K., O'Malley, B. W., and Tsai, M.-J. (1995) Mouse retinoid X receptor contains a sepaable ligand-binding and transactivation domain in its E region. Mol. Cell. Biol. 15, 255-263
13. Durand, B., Saunders, M., Gaudon, C., Roy, B., Losson, R., and Chambon, P. (1994) Activation function 2 (AF-2) of retinoic acid receptor and 9-cis retinoic acid receptor: presence of a conserved autonomous constitutive activating domain and influence of the nature of the response element on AF-2 activity. EMBO J. 13, 5370-5382
14. Nagpal, S., Friant, S., Nakshatri, H., and Chambon, P. (1993) RARs and RXRs: evidence for two autonomous transactivation functions (AF-1 and AF-2) and heterodimerization in vivo. EMBO J. 12, 2349-2360
15. Saatcioglu, F., Bartunek, P., Deng, T., Zenke, M., and Karin, M. (1993) A conserved C-terminal sequence that is deleted in v-ErbA is essential for the biological activities of c-ErbA (the thyroid hormone receptor). Mol. Cell. Biol. 13, 3675-3685
16. Tate, B.F., Allenby, G., Janocha, R.,Kazmer, S., Speck, J., Sturzenbecker, L. J., Abarzúa. P., Levin, A. A., and Grippe, J. F. 1994. Distinct binding determinants for 9-cis retinoic acid are located within AF-2 of relinoic acid receptor α. Mol. Cell Biol. 14, 2323-2330
17. Zenke, M., Muñoz, A., Sap, J., Vennström, B., and Beug, H. (1990) v-erbA oncogene activation entails the loss of hormone-dependent regulator activity of c-erbA. Cell 61, 1035-1049
18. Bourguet, W., Ruff, M., Chambon, P., Cronemeyer, H., and Moras, D. (1995) Crystal structure of the ligand-binding domain of the human nuclear receptor RXR-α. Nature (London) 375, 377-382
19. Halachmi, S., Marden, E.,Martin, G., MacKay, H., Abbondanza, C., and Brown, M. (1994) Estrogen receptor-associated proteins: possible mediators of hormone-induced transcription. Science 264, 1455-1458
20. Le Douarin, B., Zechel, C., Gamier, J.-M., Lutz, Y., Tora, L., Pierrat, B., Heery, D., Gronemeyer, H., Chambon, P., and Losson, R. (1995) The N-terminal part of TIFl, a putative mediator of the ligand-dependent activation function (AF-2) of nuclear receptors, is fused to B-raf in the oncogenic protein T18. EMBO J. 14, 2020-2033
21. Wurtz, J.-M., Bourguet, W.-B., Renaud, J.-P., Vivat, V., Chambon, P., Moras, D., and Gronemeyer, H. (1996) A canonical structure for the ligand-binding domain of nuclear receptors. Nature Struct. Biol. 3, 87-94
22. Green, S., Isseman, I., and Scheer, E. (1988) A versatile in vivo and in vitro eukaryotic expression vector for protein engineering. Nucleic Acids Res. 16, 369
23. de Thé, H., Vivanco-Ruiz, M., Tiollais, P., Stunnenberg, H., and Dejean, A. (1990) Identification of a retinoic acid responsive element in the retinoic acid receptor β gene. Nature (London) 343, 177-180
24. Nervi, C., Grippo, J. F., Sherman, M. I., George, M. D., and Jetten, A. M. (1989) Identification and characterization of nuclear retinoic acid-binding activity in human myeloblastic leukemia HL-60 cells. Proc. Natl. Acad. Sci. USA 86, 5854-5858
25. Costa-Giomi, M. P., Gaub, M.-P., Chambon, P., and Abarzua, P. (1992) Characterization of a retinoic acid responsive element isolated by whole genome PCR. Nucleic Acids Res. 20, 3223-3232
26. Allenby, G., Janocha, R. Kazmer, S., Speck, J., Grippo, J. F., and Levin, A. A. (1994) Binding of 9-cis-retinoic acid and all-trans-retinoic acid to retinoic acid receptors α,β, and γ. J. Biol. Chem. 269, 16689-16695
27. Tate, B. F., and Grippo, J. F. (1995) Mutagenesis of the ligand binding domain of the human retinoic acid receptor a identifies critical residues for 9-cis-retinoic acid binding. J. Biol. Chem. 270, 20258-20263
28. Renaud, J.-P., Rochel, N., Ruff, M., Vivat, V., Chambon, P., Gronemeyer, H., and Moras, D. (1995) Crystal structure of the RAR-γ ligand-binding domain bound to all-trans retinoic acid. Nature (London) 378, 681-689
29. Rosen, E. D., Beninghof, E. G., and Koenig, R. J. 1993. Dimerizalion interfaces of thyroid hormone, retinoic acid, vitamin D, and retinoid X receptors. J. Biol. Chem. 268, 11534-11541
30. Yu, V. C., Delsert, C., Andersen, B., Holloway, J. M., Devary, O. V., Näär, A. M., Kirn, S. Y., Boulin, J.-M., Glass, C. K., and Rosenfeld, M. G. (1991) RXRβ a coregulator that enhances binding of retinoic acid, thyroid hormone, and vitamin D receptors to their cognate response elements. Cell 67, 1251-1266
31. Allan, G. F., Leng, X., Tsai, S. Y., Weigel, N. L., Edwards, D. P., Tsai, M.-J., and O'Malley, B. W. (1992) Hormone and antihormone induce distinct conformational changes which are central to steroid receptor activation. J. Biol. Chem. 267, 19513-19520
32. Keidel, S., LeMotte, P., and Apfel, C. (1994) Different agonist- and antagonist-induced conformational changes in retinoic acid receptors analyzed by protease mapping. Mol. Cell. Biol. 14, 287-298
33. Leng, X., Tsai, S. Y., O'Malley, B. W., and Tsai, M.-J. 1993. Ligand-eiependent conformational changes in thyroid hormone and retinoic acid receptors are potentially enhanced by heterodimerization with retinoic X receptor. J. Steroid Biochem. Mol. Biol. 46, 643-661