Complex actions of thyroid hormone receptor antagonist NH-3 on gene promoters in different cell lines

Molecular and Cellular Endocrinology

Volumn 296, Issue 1-2, 2008, Pages 69-77

  Shah, Vanya ^a   Nguyen, Phuong ^a   Nguyen, Ngoc Ha ^b   Togashi, Marie ^a,c   Scanlan, Thomas S ^b,d   Baxter, John D ^a,e   Webb, Paul ^a,e  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b UNIVERSITY OF CALIFORNIA   (United States)

^c Primate Center   (Brazil)

^d OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

^e HOUSTON METHODIST RESEARCH INSTITUTE   (United States)

Author keywords

Antagonist; Coactivator; Corepressor; Thyroid hormone; Thyroid hormone receptor

Indexed keywords

HISTONE H4; HORMONE RECEPTOR BLOCKING AGENT; LIGAND; NH 3; REPRESSOR PROTEIN; THYROID HORMONE RECEPTOR; TRANSCRIPTION FACTOR; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ARTICLE; CELL LINE; CONTROLLED STUDY; DRUG MECHANISM; GENE ACTIVATION; HYPOPHYSIS CELL; LIGAND BINDING; LIVER CELL; NONHUMAN; PRIORITY JOURNAL; PROMOTER REGION; PROTEIN BINDING; PROTEIN EXPRESSION; PROTEIN INTERACTION; RAT;

ACETIC ACIDS; ACETYLATION; CELL LINE; GENE EXPRESSION REGULATION; HISTONES; HUMANS; MODELS, BIOLOGICAL; NUCLEAR PROTEINS; PROMOTER REGIONS, GENETIC; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; RECEPTORS, THYROID HORMONE; REPRESSOR PROTEINS; TRANS-ACTIVATORS; TRANSCRIPTION FACTORS; TRANSFECTION;

EID: 56049124540     PISSN: 03037207     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.mce.2008.09.016     Document Type: Article

References (61)

1. Barettino D., Vivanco Ruiz M.M., et al. Characterization of the ligand-dependent transactivation domain of thyroid hormone receptor. EMBO J. 13 13 (1994) 3039-3049
2. Baxter J.D., Dillmann W.H., et al. Selective modulation of thyroid hormone receptor action. J. Steroid Biochem. Mol. Biol. 76 1-5 (2001) 31-42
3. Baxter J.D., Goede P., et al. Structure-based design and synthesis of a thyroid hormone receptor (TR) antagonist. Endocrinology 143 2 (2002) 517-524
4. Blaschke F., Takata Y., et al. A nuclear receptor corepressor-dependent pathway mediates suppression of cytokine-induced C-reactive protein gene expression by liver X receptor. Circ. Res. 99 12 (2006) e88-99
5. In: Braverman L.E., and Utiger R.D. (Eds). Werner's and Ingbar's The Thyroid: A Fundamental and Clinical Text. (2000), Lippincott Williams & Wilkins, Philadelphia
6. Buchholz D.R., Hsia S.C., et al. A dominant-negative thyroid hormone receptor blocks amphibian metamorphosis by retaining corepressors at target genes. Mol. Cell. Biol. 23 19 (2003) 6750-6758
7. Chen C.D., Welsbie D.S., et al. Molecular determinants of resistance to antiandrogen therapy. Nat. Med. 10 1 (2004) 33-39
8. Chiellini G., Apriletti J.W., et al. A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor. Chem. Biol. 5 6 (1998) 299-306
9. Conen D., Melly L., et al. Amiodarone-induced thyrotoxicosis: clinical course and predictors of outcome. J. Am. Coll. Cardiol. 49 24 (2007) 2350-2355
10. Davis P.J., Leonard J.L., et al. Mechanisms of nongenomic actions of thyroid hormone. Front. Neuroendocrinol. 29 2 (2008) 211-218
11. Feng W., Ribeiro R.C., et al. Hormone-dependent coactivator binding to a hydrophobic cleft on nuclear receptors. Science 280 5370 (1998) 1747-1749
12. Ghisletti S., Huang W., et al. Parallel SUMOylation-dependent pathways mediate gene- and signal-specific transrepression by LXRs and PPARgamma. Mol. Cell 25 1 (2007) 57-70
13. Glass C.K., and Rosenfeld M.G. The coregulator exchange in transcriptional functions of nuclear receptors. Genes Dev. 14 2 (2000) 121-141
14. Grover G.J., Dunn C., et al. Pharmacological profile of the thyroid hormone receptor antagonist NH3 in rats. J. Pharmacol. Exp. Ther. 322 1 (2007) 385-390
15. Guan H.P., Ishizuka T., et al. Corepressors selectively control the transcriptional activity of PPARgamma in adipocytes. Genes Dev. 19 4 (2005) 453-461
16. Higgins K.J., Liu S., et al. Vascular endothelial growth factor receptor-2 expression is down-regulated by 17beta-estradiol in MCF-7 breast cancer cells by estrogen receptor alpha/Sp proteins. Mol. Endocrinol. 22 2 (2008) 388-402
17. Hodgson M.C., Astapova I., et al. The androgen receptor recruits nuclear receptor CoRepressor (N-CoR) in the presence of mifepristone via its N and C termini revealing a novel molecular mechanism for androgen receptor antagonists. J. Biol. Chem. 280 8 (2005) 6511-6519
18. Hu X., and Lazar M.A. The CoRNR motif controls the recruitment of corepressors by nuclear hormone receptors. Nature 402 6757 (1999) 93-96
19. Ishizuka T., and Lazar M.A. The N-CoR/histone deacetylase 3 complex is required for repression by thyroid hormone receptor. Mol. Cell. Biol. 23 15 (2003) 5122-5131
20. Jenuwein T., and Allis C.D. Translating the histone code. Science 293 5532 (2001) 1074-1080
21. Jepsen K., Hermanson O., et al. Combinatorial roles of the nuclear receptor corepressor in transcription and development. Cell 102 6 (2000) 753-763
22. Ki S.H., Cho I.J., et al. Glucocorticoid receptor (GR)-associated SMRT binding to C/EBPbeta TAD and Nrf2 Neh4/5: role of SMRT recruited to GR in GSTA2 gene repression. Mol. Cell. Biol. 25 10 (2005) 4150-4165
23. Laudet V., and Gronemeyer H. The Nuclear Receptor Facts Book (2002), Academic Press, London
24. Li J., Lin Q., et al. Specific targeting and constitutive association of histone deacetylase complexes during transcriptional repression. Genes Dev. 16 6 (2002) 687-692
25. Lim W., Nguyen N.H., et al. A thyroid hormone antagonist that inhibits thyroid hormone action in vivo. J. Biol. Chem. 277 38 (2002) 35664-35670
26. Liu Y., Xia X., et al. Thyroid hormone-regulated target genes have distinct patterns of coactivator recruitment and histone acetylation. Mol. Endocrinol. 20 3 (2006) 483-490
27. Loinder K., and Soderstrom M. Functional analyses of an LXXLL motif in nuclear receptor corepressor (N-CoR). J. Steroid Biochem. Mol. Biol. 91 4-5 (2004) 191-196
28. Loinder K., and Soderstrom M. An LXXLL motif in nuclear receptor corepressor mediates ligand-induced repression of the thyroid stimulating hormone-beta gene. J. Steroid Biochem. Mol. Biol. 97 4 (2005) 322-327
29. Lonard D.M., and O'Malley B.W. The expanding cosmos of nuclear receptor coactivators. Cell 125 3 (2006) 411-414
30. Marimuthu A., Feng W., et al. TR surfaces and conformations required to bind nuclear receptor corepressor. Mol. Endocrinol. 16 2 (2002) 271-286
31. Moore J.M., Galicia S.J., et al. Quantitative proteomics of the thyroid hormone receptor-coregulator interactions. J. Biol. Chem. 279 26 (2004) 27584-27590
32. Nagy L., Kao H.Y., et al. Mechanism of corepressor binding and release from nuclear hormone receptors. Genes Dev. 13 24 (1999) 3209-3216
33. Nguyen N.H., Apriletti J.W., et al. Hammett analysis of selective thyroid hormone receptor modulators reveals structural and electronic requirements for hormone antagonists. J. Am. Chem. Soc. 127 13 (2005) 4599-4608
34. Nguyen N.H., Apriletti J.W., et al. Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment. J. Med. Chem. 45 15 (2002) 3310-3320
35. Oberste-Berghaus C., Zanger K., et al. Thyroid hormone-independent interaction between the thyroid hormone receptor beta2 amino terminus and coactivators. J. Biol. Chem. 275 3 (2000) 1787-1792
36. Ogawa S., Lozach J., et al. Molecular determinants of crosstalk between nuclear receptors and toll-like receptors. Cell 122 5 (2005) 707-721
37. Orlando V., Strutt H., et al. Analysis of chromatin structure by in vivo formaldehyde cross-linking. Methods 11 2 (1997) 205-214
38. Ota Y., and Mariash C.N. Paradoxical triiodothyronine suppression of S14 transcription in permanent hepatic cell lines. Thyroid 13 5 (2003) 437-445
39. Pascual G., and Glass C.K. Nuclear receptors versus inflammation: mechanisms of transrepression. Trends Endocrinol. Metab. 17 8 (2006) 321-327
40. Paul B.D., Buchholz D.R., et al. Tissue- and gene-specific recruitment of steroid receptor coactivator-3 by thyroid hormone receptor during development. J. Biol. Chem. 280 29 (2005) 27165-27172
41. Paul B.D., Fu L., et al. Coactivator recruitment is essential for liganded thyroid hormone receptor to initiate amphibian metamorphosis. Mol. Cell. Biol. 25 13 (2005) 5712-5724
42. Rosenfeld M.G., Lunyak V.V., et al. Sensors and signals: a coactivator/corepressor/epigenetic code for integrating signal-dependent programs of transcriptional response. Genes Dev. 20 11 (2006) 1405-1428
43. Scanlan, T.S., Baxter, J.D., et al., 1996. Thyroid hormone receptors and ligands. International Patent. University of California.
44. Sharma D., and Fondell J.D. Ordered recruitment of histone acetyltransferases and the TRAP/Mediator complex to thyroid hormone-responsive promoters in vivo. Proc. Natl. Acad. Sci. U.S.A. 99 12 (2002) 7934-7939
45. Sohn Y.C., Kim S.W., et al. Dynamic inhibition of nuclear receptor activation by corepressor binding. Mol. Endocrinol. 17 3 (2003) 366-372
46. Tian H., Mahajan M.A., et al. The N-terminal A/B domain of the thyroid hormone receptor-{beta}2 isoform influences ligand-dependent recruitment of co-activators to the ligand binding domain. Mol. Endocrinol. (2006)
47. Tomita A., Buchholz D.R., et al. Recruitment of N-CoR/SMRT-TBLR1 corepressor complex by unliganded thyroid hormone receptor for gene repression during frog development. Mol. Cell. Biol. 24 8 (2004) 3337-3346
48. Velasco L.F., Togashi M., et al. Thyroid hormone response element organization dictates the composition of active receptor. J. Biol. Chem. (2007)
49. Wagner R.L., Apriletti J.W., et al. A structural role for hormone in the thyroid hormone receptor. Nature 378 6558 (1995) 690-697
50. Wang D., and Simons Jr. S.S. Corepressor binding to progesterone and glucocorticoid receptors involves the activation function-1 domain and is inhibited by molybdate. Mol. Endocrinol. 19 6 (2005) 1483-1500
51. Webb P., Anderson C.M., et al. The nuclear receptor corepressor (N-CoR) contains three isoleucine motifs (I/LXXII) that serve as receptor interaction domains (IDs). Mol. Endocrinol. 14 12 (2000) 1976-1985
52. Webb P., Nguyen N.H., et al. Design of thyroid hormone receptor antagonists from first principles. J. Steroid Biochem. Mol. Biol. 83 1-5 (2002) 59-73
53. Wilkinson J.R., and Towle H.C. Identification and characterization of the AF-1 transactivation domain of thyroid hormone receptor beta1. J. Biol. Chem. 272 38 (1997) 23824-23832
54. Yang Z., Hong S.H., et al. Transcriptional anti-repression. Thyroid hormone receptor beta-2 recruits SMRT corepressor but interferes with subsequent assembly of a functional corepressor complex. J. Biol. Chem. 274 52 (1999) 37131-37138
55. Yen P.M. Physiological and molecular basis of thyroid hormone action. Physiol. Rev. 81 3 (2001) 1097-1142
56. Yen P.M., Feng X., et al. Effects of ligand and thyroid hormone receptor isoforms on hepatic gene expression profiles of thyroid hormone receptor knockout mice. EMBO Rep. 4 6 (2003) 581-587
57. Yoon H.G., Chan D.W., et al. Purification and functional characterization of the human N-CoR complex: the roles of HDAC3, TBL1 and TBLR1. EMBO J. 22 6 (2003) 1336-1346
58. Yoon H.G., Choi Y., et al. Reading and function of a histone code involved in targeting corepressor complexes for repression. Mol. Cell. Biol. 25 1 (2005) 324-335
59. Yoon H.G., and Wong J. The corepressors silencing mediator of retinoid and thyroid hormone receptor and nuclear receptor corepressor are involved in agonist- and antagonist-regulated transcription by androgen receptor. Mol. Endocrinol. 20 5 (2006) 1048-1060
60. Yoshihara H.A., Apriletti J.W., et al. A designed antagonist of the thyroid hormone receptor. Bioorg. Med. Chem. Lett. 11 21 (2001) 2821-2825
61. Zhang J., and Lazar M.A. The mechanism of action of thyroid hormones. Annu. Rev. Physiol. 62 (2000) 439-466