Regulation of nuclear receptors by agonists and antagonists

Current Opinion in Endocrinology and Diabetes

Volumn 3, Issue 5, 1996, Pages 397-402

  Stewart, A Francis ^a   Logie, Colin ^a   Nichols, Mark ^a  

^a EUROPEAN MOLECULAR BIOLOGY LABORATORY   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 0008254683     PISSN: 10683097     EISSN: None     Source Type: Journal    
DOI: 10.1097/00060793-199610000-00006     Document Type: Article

References (62)

1. Tonetti DA, Jordan VC: Targeted anti-estrogens to treat and prevent diseases in women. Mol Med Today 1996, 2:218-223.
2. Mangelsdorf DJ, Thummel C, Beato M, Herrlich P, Schutz G, Umesono K, Blumberg B, Kastner P, Mark M, Chambon P, Evans RM: The nuclear receptor superfamily: the second decade. Cell 1995, 83:835-839.
3. Apfel C, Bauer F, Crettaz M, Forni L, Kamber M, Kaufmann F, LeMotte P, Pirson W, Klaus M: A retinoic acid receptor alpha antagonist selectively counteracts retinoic acid effects. Proc Natl Acad U S A Sci 1992, 89:7129-7133.
4. Fanjul A, Dawson MI, Hobbs PD, Jong L, Cameron JF, Harlev E, Graupner G, Lu XP, Pfahl M: A new class of retinoids with selective inhibition of AP-1 inhibits proliferation. Nature 1994, 372:107-111.
5. Chen JY, Penco S, Ostrowski J, Balaguer P, Pons M, Starrett JE, Reczek P, Chambon P, Gronemeyer H: RAR-specffic agonist/antagonists which dissociate transactivation and AP1 transrepression inhibit anchorage-independent cell proliferation. EMBO J 1995, 14:1187-1197.
6. Kuiper GGJM, Emmark E, Pelto-Huikko M, Nilsson S, Gustafsson JA: Cloning of a novel estrogen receptor expressed in rat prostate and ovary. Proc Natl Acad Sci U S A 1996, 93:5925-5930.
7. Fuchs YR, Glasebrook AL, Short LL, Draper MW, Rippy MK, Cole HW, Magee DE, Termine JD, Bryant HU: Raloxifene is a tissue-selective agonist/antagonist that functions through the estrogen receptor. Ann N Y Acad Sci 1995, 761:355-360.
8. Berry M. Metzger D, Chambon P: Role of the two activating domains of the oestrogen receptor in the cell-type and promoter-context dependent agonistic activity of the anti-oestrogen 4-hydroxytamoxifen. EMBO J 1990, 9:2811-2818.
9. Chen JY, Clifford J, Zusi C, Starrett J, Tortolani D, Ostrowski J, Reczek PR, Chambon P, Gronemeyer H: Two distinct events In retinold receptor heterodimer action revealed by ligand synergism. Nature 1996, in press.
10. Bourguet W, Ruff M, Chambon P, Gronemeyer H, Moras D: Crystal structure of the ligand-binding domain of the human nuclear receptor RXR-alpha. Nature 1995, 375:377-382. First determination of a ligand-binding domain structure and recognition of a novel protein fold.
11. Renaud JP, Rochel N, Ruff M, Vivat V, Chambon P, Gronemeyer H, Moras D: Crystal structure of the RAR-gamma ligand-binding domain bound to all-trans retinoic acid. Nature 1995, 378:681-689. This paper identifies the ligand-binding pocket of RAR and, in comparison with the unliganded RXR ligand-binding domain structure, a "mouse trap" model of ligand binding and conformational change was proposed.
12. Wagner RL, Apriletti JW, McGrath ME, West BL, Baxter JD, Fletterick RJ: A structural role for hormone in the thyroid hormone receptor. Nature 1995, 378:690-697. This paper presents the crystal structure of a thyroid hormone ligand-binding domain bound with ligand. Bound ligand is fully buried and integrated into the hydrophobic core of the domain.
13. Wurtz JM, Bourguet W, Renaud JP, Vivat V, Chambon P, Moras D, Gronemeyer H: A canonical structure for the ligand-binding domain of nuclear receptors. Nat Struct Biol 1996, 3:87-94. The first complete definition of the amino acid sequence boundaries and internal alignments of the ligand-binding domain as found throughout the superfamily of nuclear receptors.
14. Gronemeyer H, Laudet V: Transcription factors 3: nuclear receptors. Protein Profile 1995, 2:1173-1308. A comprehensive and remarkable compendium of information on the molecular biology of the nuclear receptor superfamily. Interested readers will find this extremely useful.
15. Allan GF, Leng X, Tsai SY, Weigel NL, Edwards DP, Tsai MJ, O'Malley BW: Hormone and antihormone induce distinct conformational changes which are central to steroid receptor activation. J Biol Chem 1992, 267:19513-19520.
16. Keidel S, LeMotte P, Apfel C: Different agonist- and antagonist-induced conformational changes in retinoic acid receptors analyzed by protease mapping. Mol Cell Biol 1994, 14:287-298.
17. Dalman FC, Sturzenbecker LJ, Levin AA, Lucas DA, Perdew GH, Petkovitch M, Chambon P, Grippo JF, Pratt WB: Retinoic acid receptor belongs to a subclass of nuclear receptors that do not form "docking" complexes with hsp90. Biochemistry 1991, 30:5605-5608.
18. Tuohimaa P, Pekki A, Blauer M, Joensuu T, Vilja P, Ylikomi T: Nuclear progesterone receptor is mainly heat shock protein 90-free in vivo. Proc Natl Acad Sci U S A 1993, 90:5848-5852.
19. Bohen SP, Yamamoto KR: Isolation of Hsp90 mutants by screening for decreased steroid receptor function. Proc Natl Acad Sci U S A 1993, 90:11424-11428.
20. Caplan AJ, Langley E, Wilson EM, Vidal J: Hormone-dependent transactivation by the human androgen receptor is regulated by a dnaJ protein. J Biol Chem 1995, 270:5251-5257.
21. Kimura Y, Yahara I, Lindquist S: Role of the protein chaperone YDJ1 In establishing Hsp90-mediated signal transduction pathways. Science 1995, 268:1362-1365.
22. Nathan DF, Lindquist S: Mutational analysis of Hsp90 function: interactions with a steroid receptor and a protein kinase. Mol Cell Biol 1995, 15:3917-3925.
23. Scherrer LC, Picard D, Massa E, Harmon JM, Simons SJ, Yamamoto KR, Pratt WB: Evidence that the hormone binding domain of steroid receptors confers hormonal control on chimeric proteins by determining their hormone-regulated binding to heat-shock protein 90. Biochemistry 1993, 32:5381-5386.
24. Picard D: Regulation of protein function through expression of chimaeric proteins. Curr Opin Biotechnol 1994, 5:511-515.
25. Logic C, Stewart AF: Ligand-regulated site-specific recombination. Proc Natl Acad Sci U S A 1995, 92:5940-5944.
26. Smith DF, Whitesell L, Nair SC, Chen S, Prapapanich V, Rimerman RA: Progesterone receptor structure and function altered by geldanamycin, an hsp90-binding agent. Mol Cell Biol 1995, 15:6804-6812.
27. Czar MJ, Lyons RH, Welsh MJ, Renoir JM, Pratt WB: Evidence that the FK506-binding immunophilin heat shock protein 56 is required for trafficking of the glucocorticold receptor from the cytoplasm to the nucleus. Mol Endolcrinol 1995, 9:1549-1560.
28. Yang J, DeFranco DB: Assessment of glucocorticoid receptor-heat shock protein 90 interactions in vivo during nucleocytoplasmic trafficking. Mol Endocrinol 1996, 10:3-13.
29. Guiochon MA, Lescop P, Christin MS, Loosfelt, H, Perrot AM, Milgrom E: Nucleocytoplasmic shuttling of the progesterone receptor. EMBO J 1991, 10:3851-3859.
30. Dauvois S, White R, Parker MG: The antiestrogen ICI 182780 disrupts estrogen receptor nucleocytoplasmic shuttling. J Cell Sci 1993, 106:1377-1388.
31. Dauvois S, Danielian PS, White R, Parker MG: Antiestrogen ICI 164,384 reduces cellular estrogen receptor content by increasing its turnover. Proc Natl Acad Sci U S A 1992, 89:4037-4041.
32. Pratt WB, Welsh MJ: Chaperone functions of the heat shock proteins associated with steroid receptors. Semin Cell Biol 1994, 5:83-93.
33. Bunone G, Briand PA, Miksicek RJ, Picard D: Activation of unliganded estrogen receptor by EGF Involves the MAP kinase pathway and direct phosphorylation. EMBO J 1996, 15:2174-2183.
34. Seol W, Choi HS, Moore DD: Isolation of proteins that interact specifically with the retinoid X receptor: two novel orphan receptors. Mol Endocrinol 1995, 9:72-85.
35. Horlein AJ, Naar AM, Heinzel T, Torchia J, Gloss G, Kurokawa R, Ryan A, Kamei Y, Soderstrom M, Glass CK, Rosenfeld MG: Ligand-independent repression by the thyroid hormone receptor mediated by a nuclear receptor co-repressor. Nature 1995, 377:397-404.
36. Chen JD, Evans RM: A transcriptional co-repressor that interacts with nuclear hormone receptors. Nature 1995, 377:454-457.
37. Burris TP, Nawaz Z, Tsai MJ, O'Malley BW: A nuclear hormone receptor-associated protein that inhibits transactivation by the thyroid hormone and retinoic acid receptors. Proc Natl Acad Sci U S A 1995, 92:9525-9529.
38. Reik A, Schutz G, Stewart AF: Glucocorticoids are required for estab-lishment and maintenance of an alteration in chromatin structure: induction leads to reversible disruption of nucleosomes over en enhancer. EMBO J 1991, 10:2569-2576.
39. Thomas HE, Stunnenberg HG, Stewart AF: Heterodimerization of the Drosophila ecdysone receptor with retinold X receptor and ultraspiracle. Nature 1993, 362:471-475.
40. Cheskis B, Freedrnan LP: Ligand modulates the conversion of DNA-bound vitamin D3 receptor (VDR) homodimers into VDR-retinoid X receptor heterodimers. Mol Cell Biol 1994, 14:3329-3338.
41. Au FM, Helmer E, Casanova J, Raaka BM, Samuels HH: The conserved ninth C-terminal heptad In thyroid hormone and retinoic acid receptors mediates diverse responses by affecting heterodimer but not homodimer formation. Mol Cell Biol 1993, 13:5725-5737.
42. Koelle MR: Molecular analysis of the Drosophila ecdysone receptor complex [PhD thesis]. Stanford CA; Stanford University: 1992.
43. Yao TP, Forman BM, Jiang Z, Cherbas L, Chen JD, McKeown M, Cherbas P, Evans RM: Functional ecdysone receptor is the product of EcR and Ultraspiracle genes. Nature 1993, 366:476-479.
44. Kurokawa R, Soderstrom M, Horlein A, Halachmi S, Brown M, Rosenfeld MG, Glass CK: Polarity-specific activities of retinoic acid receptors determined by a co-repressor. Nature 1995, 377:451-454. See editorial comment in same issue.
45. Forman BM, Umesone K, Chen J, Evans RM: Unique response pathways are established by allosteric interactions among nuclear hormone receptors. Cell 1995, 81:541-550.
46. Fawell SE, White R, Hoars S, Sydenham M, Page M, Parker MG: Inhibition of estrogen receptor-DNA binding by the "pure" antiestrogen ICI 164,384 appears to be mediated by Impaired receptor dimerization. Proc Natl Acad Sci U S A 1990, 87:6883-6887.
47. Perez A, Kastner P, Sethi S, Lutz Y, Reibel C, Chambon P: PMLRAR homodimers: distinct DNA binding properties and heteromeric interactions with RXR. EMBO J 1993, 12:3171-3182.
48. Meyer ME, Gronemeyer H, Turcotte B, Bocquel MT, Tasset D, Chambon P: Steroid hormone receptors compete for factors that mediate their enhancer function. Cell 1989, 57:433-442.
49. Barettino D, Vinanco RM, Stunnenberg HG: Characterization of the ligand-dependent transactivation domain of thyroid hormone receptor. EMBO J 1994, 13:3039-3049.
50. Halachmi S, Marden E, Martin G, MacKay H, Abbondanza C, Brown M: Estrogen receptor-associated proteins: possible mediators of hormone-induced transcription. Science 1994, 264:1455-1458.
51. Cavailles V, Dauvois S, L'Horset F, Lopez G, Hoare S, Kushner PJ, Parker MG: Nuclear factor RIP140 modulates transcriptional activation by the estrogen receptor. EMBO J 1995, 14:3741-3751.
52. Lee JW, Choi HS, Gyuris J, Brent R, Moore DD: Two classes of proteins dependent on either the presence or absence of thyroid hormone for Interaction with the thyroid hormone receptor. Mol Endocrinol 1995, 9:243-254.
53. Lee JW, Ryan F, Swaffield JC, Johnston SA, Moore DD: Interaction of thyroid-hormone receptor with a conserved transcriptional mediator. Nature 1995, 374:91-94.
54. LeDouarin B, Zechel C, Garnier JM, Lutz Y, Tora L, Pierrat P, Heery D, Gronemeyer H, Chambon P, Losson R: The N-terminal part of TIF1, 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 1995, 14:2020-2033.
55. Onate SA, Tsai SY, Tsai MJ, O'Malley BW: Sequence and characterization of a coactivator for the steroid hormone receptor superfamily. Science 1995, 270:1354-1357.
56. vom BE, Zechel C, Heery D, Heine MJ, Garnier JM, Vivat V, Le DB, Gronemeyer H, Chambon P, Losson R: Differential ligand-dependent Interactions between the AF-2 activating domain of nuclear receptors and the putative transcriptional intermediary factors mSUG1 and TIF1. EMBO J 1996, 15:110-124.
57. Kamei Y, Xu X, Heinzel T, Torchia J, Kurokawa R, Gloss B, Lin SC, Heyman RA, Rose DW, Glass CK, Rosenfeld MG: A CBP integrator complex mediates transcriptional activation and AP-1 Inhibition by nuclear receptors. Cell 1996, 85:403-414. The identification of a cofactor complex that is likely to be a central player in transcriptional activities mediated by nuclear receptors.
58. Yeh S, Chang C: Cloning and characterisation of a specific coactivator, ARA70, for an androgen receptor in human prostate cells. Proc Natl Acad Sci U S A 1996, 93:5517-5521.
59. Voegel JJ, Heine MJS, Zechel C, Chambon P, Gronemeyer H: TIF2, a 160 kDa transcriptional mediator for the ligand-dependent activation function AF-2 of nuclear receptors. EMBO J 1996, 15:3667-3675.
60. Jonat C, Rahmsdorf HJ, Park KK, Cato AC, Gebel S, Ponta H, Herrlich P: Antitumor promotion and antiinflammation: down-modulation of AP-1 (Fos/Jun) activity by glucocorticoid hormone. Cell 1990, 62:1189-1204.
61. Beato M, Herrlich P, Schutz G: Steroid hormone receptors: many actors in search of a plot. Cell 1995, 83:851-857.
62. Nagpal S, Athanikar J, Chandraratna RA: Separation of transactivation and AP1 antagonism functions of retinoic acid receptor alpha. J Biol Chem 1995, 270:923-927.