Nuclear receptor coregulators as a new paradigm for therapeutic targeting

Advanced Drug Delivery Reviews

Volumn 62, Issue 13, 2010, Pages 1227-1237

  Hsia, Elaine Y ^a,c   Goodson, Michael L ^a   Zou, June X ^b   Privalsky, Martin L ^a   Chen, Hong Wu ^a,c  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b UNIVERSITY OF CALIFORNIA   (United States)

^c UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

ANCCA; Cancer; Diabetes; Histone acetylation; Histone methylation; NCoR; Obesity; P160 SRC; PGC 1; SMRT

Indexed keywords

ANCCA; CANCER; DIABETES; HISTONE ACETYLATION; HISTONE METHYLATION; NCOR; OBESITY; P160/SRC; PGC-1; SMRT;

ALKYLATION; CHROMOSOMES; METHYLATION; NUTRITION; TRANSCRIPTION FACTORS;

ACETYLATION;

AMINE OXIDASE (FLAVIN CONTAINING); ANDROGEN RECEPTOR; ANTIDEPRESSANT AGENT; CELL NUCLEUS RECEPTOR; DIETHYLSTILBESTROL; ESTRADIOL; ESTROGEN RECEPTOR; ESTROGEN RECEPTOR ANTAGONIST; FULVESTRANT; HORMONE RECEPTOR BLOCKING AGENT; JUMONJIC PROTEIN; LYSINE SPECIFIC HISTONE DEMETHYLASE 1; METASTASIS ASSOCIATED PROTEIN; NUCLEAR COREGULATOR CANCER ASSOCIATED PROTEIN; NUCLEAR RECEPTOR COREPRESSOR; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA COACTIVATOR 1ALPHA; PROTEIN AAA; PROTEIN LCOR; PROTEIN P160; PROTEIN TYROSINE KINASE; RALOXIFENE; RECEPTOR INTERACTING PROTEIN 140; REGULATOR PROTEIN; REPRESSOR PROTEIN; RESVERATROL; SELECTIVE ESTROGEN RECEPTOR MODULATOR; SILENCING MEDIATOR OF RETINOID AND THYROID HORMONE RECEPTOR; TAMOXIFEN; TRANSCRIPTION FACTOR; UNCLASSIFIED DRUG; UNINDEXED DRUG;

CHROMATIN ASSEMBLY AND DISASSEMBLY; DEPRESSION; DRUG MECHANISM; ENERGY BALANCE; ENZYME ACTIVITY; EPIGENETICS; GENETIC REGULATION; GENETIC TRANSCRIPTION; HUMAN; HYPERGLYCEMIA; MALIGNANT NEOPLASTIC DISEASE; METABOLIC DISORDER; METABOLIC REGULATION; NONHUMAN; PRIORITY JOURNAL; PROTEIN DEFECT; PROTEIN DOMAIN; PROTEIN EXPRESSION; PROTEIN FAMILY; PROTEIN FUNCTION; PROTEIN MOTIF; PROTEIN PROTEIN INTERACTION; PROTEIN STRUCTURE; PROTEIN TARGETING; REGULATORY MECHANISM; REVIEW; SIGNAL TRANSDUCTION;

CO-REPRESSOR PROTEINS; HEAT-SHOCK PROTEINS; HUMANS; METABOLIC DISEASES; MOLECULAR TARGETED THERAPY; NEOPLASMS; NUCLEAR PROTEINS; NUCLEAR RECEPTOR COACTIVATORS; PROTEIN INTERACTION DOMAINS AND MOTIFS; RECEPTORS, CYTOPLASMIC AND NUCLEAR; SIGNAL TRANSDUCTION; TRANSCRIPTION FACTORS; TRANSCRIPTION, GENETIC;

EID: 78649326873     PISSN: 0169409X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.addr.2010.09.016     Document Type: Review

References (146)

1. Glass C.K., Rosenfeld M.G. The coregulator exchange in transcriptional functions of nuclear receptors. Genes & Development 2000, 14:121-141.
2. Xu J., Li Q. Review of the in vivo functions of the p160 steroid receptor coactivator family. Molecular Endocrinology 2003, 17:1681-1692.
3. Edwards D.P. The role of coactivators and corepressors in the biology and mechanism of action of steroid hormone receptors. Journal of Mammary Gland Biology and Neoplasia 2000, 5:307-324.
4. Shang Y., Hu X., DiRenzo J., Lazar M.A., Brown M. Cofactor dynamics and sufficiency in estrogen receptor-regulated transcription. Cell 2000, 103:843-852.
5. Kushner P.J., et al. Estrogen receptor action through target genes with classical and alternative response elements. Pure and Applied Chemistry 2003, 75:1757-1769.
6. Metivier R., Penot G., Flouriot G., Pakdel F. Synergism between ERa transactivation function 1 (AF-1) and AF-2 mediated by steroid receptor coactivator protein-1: requirement for the AF-1 a-helical core and for a direct interaction between the N- and C-terminal domains. Molecular Endocrinology 2001, 15:1953-1970.
7. McInerney E.M., Rose D.W., Flynn S.E., Westin S., Mullen T.-M., Krones A., Inostroza J., Torchia J., Nolte R.T., Assa-Munt N., Milburn M.V., Glass C.K., Rosenfeld M.G. Determinants of coactivator LXXLL motif specificity in nuclear receptor transcriptional activation. Genes & Development 1998, 12:3357-3368.
8. Darimont B.D., Wagner R.L., Apriletti J.W., Stallcup M.R., Kushner P.J., Baxter J.D., Fletterick R.J., Yamamoto K.R. Structure and specificity of nuclear receptor-coactivator interactions. Genes & Development 1998, 12:3343-3356.
9. M. Doi, J. Hirayama, P. Sassone-Corsi, Circadian Regulator CLOCK Is a Histone Acetyltransferase, Cell 125 (2006) 497-508.
10. Moras D., Gronemeyer H. The nuclear receptor ligand-binding domain: structure and function. Current Opinion in Cell Biology 1998, 10:384-391.
11. Wurtz J.-M., Bourguet W., Renaud J.-P., Vivat V., Chambon P., Moras D., Gronemeyer H. A canonical structure for the ligand-binding domain of nuclear receptors. Nature Structural & Molecular Biology 1996, 3:87-94.
12. Hall J.M., McDonnell D.P., Korach K.S. Allosteric regulation of estrogen receptor structure, function, and coactivator recruitment by different estrogen response elements. Molecular Endocrinology 2002, 16:469-486.
13. Klinge C.M., Jernigan S.C., Smith S.L., Tyulmenkov V.V., Kulakosky P.C. Estrogen response element sequence impacts the conformation and transcriptional activity of estrogen receptor a. Molecular and Cellular Endocrinology 2001, 174:151-166.
14. Hsia E.Y.C., Zou J.X., Chen H.-W. Chapter 8 the roles and action mechanisms of p160/SRC coactivators and the ANCCA coregulator in cancer. Progress in Molecular Biology and Translational Science 2009, 261-298. Elsevier Inc.
15. Harigopal M., Heymann J., Ghosh S., Anagnostou V., Camp R., Rimm D. Estrogen receptor co-activator (AIB1) protein expression by automated quantitative analysis (AQUA) in a breast cancer tissue microarray and association with patient outcome. Breast Cancer Research and Treatment 2009, 115:77-85.
16. Dihge L., Bendahl P.-O., Grabau D., Isola J., Lövgren K., Rydén L., Fernö M. Epidermal growth factor receptor (EGFR) and the estrogen receptor modulator amplified in breast cancer (AIB1) for predicting clinical outcome after adjuvant tamoxifen in breast cancer. Breast Cancer Research and Treatment 2008, 109:255-262.
17. Myers E., Hill A.D.K., Kelly G., McDermott E.W., O'Higgins N.J., Buggy Y., Young L.S. Associations and interactions between Ets-1 and Ets-2 and coregulatory proteins, SRC-1, AIB1, and NCoR in breast cancer. Clinical Cancer Research 2005, 11:2111-2122.
18. Fleming F.J., Myers E., Kelly G., Crotty T.B., McDermott E.W., O'Higgins N.J., Hill A.D.K., Young L.S. Expression of SRC-1, AIB1, and PEA3 in HER2 mediated endocrine resistant breast cancer; a predictive role for SRC-1. Journal of Clinical Pathology 2004, 57:1069-1074.
19. Osborne C.K., Bardou V., Hopp T.A., Chamness G.C., Hilsenbeck S.G., Fuqua S.A.W., Wong J., Allred D.C., Clark G.M., Schiff R. Role of the estrogen receptor coactivator AIB1 (SRC-3) and HER-2/neu in tamoxifen resistance in breast cancer. Journal of the National Cancer Institute 2003, 95:353-361.
20. Gregory C.W., He B., Johnson R.T., Ford O.H., Mohler J.L., French F.S., Wilson E.M. A mechanism for androgen receptor-mediated prostate cancer recurrence after androgen deprivation therapy. Cancer Research 2001, 61:4315-4319.
21. Yan J., Erdem H., Li R., Cai Y., Ayala G., Ittmann M., Yu-Lee L.-Y., Tsai S.Y., Tsai M.-J. Steroid receptor coactivator-3/AIB1 promotes cell migration and invasiveness through focal adhesion turnover and matrix metalloproteinase expression. Cancer Research 2008, 68:5460-5468.
22. Zhou H.-J., Yan J., Luo W., Ayala G., Lin S.-H., Erdem H., Ittmann M., Tsai S.Y., Tsai M.-J. SRC-3 is required for prostate cancer cell proliferation and survival. Cancer Research 2005, 65:7976-7983.
23. Gnanapragasam V.J., Leung H.Y., Pulimood A.S., Neal D.E., Robson C.N. Expression of RAC 3, a steroid hormone receptor co-activator in prostate cancer. British Journal of Cancer 2001, 85:1928-1936.
24. Iwase H., Omoto Y., Toyama T., Yamashita H., Hara Y., Sugiura H., Zhang Z. Clinical significance of AIB1 expression in human breast cancer. Breast Cancer Research and Treatment 2003, 80:339-345.
25. Alkner S., Bendahl P.-O., Grabau D., Lovgren K., Stal O., Ryden L., Ferno M. AIB1 is a predictive factor for tamoxifen response in premenopausal women. Annals of Oncology 2010, 21:238-244. o.b.o.t.S. Swedish, South-East Swedish Breast Cancer Groups.
26. Agoulnik I.U., Vaid A., Nakka M., Alvarado M., Bingman W.E., Erdem H., Frolov A., Smith C.L., Ayala G.E., Ittmann M.M., Weigel N.L. Androgens modulate expression of transcription intermediary Factor 2, an androgen receptor coactivator whose expression level correlates with early biochemical recurrence in prostate cancer. Cancer Research 2006, 66:10594-10602.
27. Louie M.C., Zou J.X., Rabinovich A., Chen H.-W. ACTR/AIB1 functions as an E2F1 coactivator to promote breast cancer cell proliferation and antiestrogen resistance. Molecular and Cellular Biology 2004, 24:5157-5171.
28. Zou J.X., Zhong Z., Shi X.-B., Tepper C.G., White R.W.D., Kung H.-J., Chen H. ACTR/AIB1/SRC-3 and androgen receptor control prostate cancer cell proliferation and tumor growth through direct control of cell cycle genes. The Prostate 2006, 66:1474-1486.
29. Al-azawi D., Ilroy M.M., Kelly G., Redmond A.M., Bane F.T., Cocchiglia S., Hill A.D.K., Young L.S. Ets-2 and p160 proteins collaborate to regulate c-Myc in endocrine resistant breast cancer. Oncogene 2007, 27:3021-3031.
30. Gregory C.W., Fei X., Ponguta L.A., He B., Bill H.M., French F.S., Wilson E.M. Epidermal growth factor increases coactivation of the androgen receptor in recurrent prostate cancer. The Journal of Biological Chemistry 2004, 279:7119-7130.
31. Ueda T., Mawji N.R., Bruchovsky N., Sadar M.D. Ligand-independent activation of the androgen receptor by interleukin-6 and the role of steroid receptor coactivator-1 in prostate cancer cells. The Journal of Biological Chemistry 2002, 277:38087-38094.
32. Feldman B.J., Feldman D. The development of androgen-independent prostate cancer. Nature Reviews Cancer 2001, 1:34-45.
33. Shou J., Massarweh S., Osborne C.K., Wakeling A.E., Ali S., Weiss H., Schiff R. Mechanisms of tamoxifen resistance: increased estrogen receptor-HER2/neu cross-talk in ER/HER2-positive breast cancer. Journal of the National Cancer Institute 2004, 96:926-935.
34. Massarweh S., Osborne C.K., Creighton C.J., Qin L., Tsimelzon A., Huang S., Weiss H., Rimawi M., Schiff R. Tamoxifen resistance in breast tumors is driven by growth factor receptor signaling with repression of classic estrogen receptor genomic function. Cancer Research 2008, 68:826-833.
35. Su Q., Hu S., Gao H., Ma R., Yang Q., Pan Z., Wang T., Li F. Role of AIB1 for tamoxifen resistance in estrogen receptor-positive breast cancer cells. Oncology 2008, 75:159-168.
36. Zhao W., Zhang Q., Kang X., Jin S., Lou C. AIB1 is required for the acquisition of epithelial growth factor receptor-mediated tamoxifen resistance in breast cancer cells. Biochemical and Biophysical Research Communications 2009, 380:699-704.
37. Nettles K.W., Greene G.L. Ligand control of coregulator recruitment to nuclear receptors. Annual Review of Physiology 2005, 67:309-333.
38. Shang Y., Brown M. Molecular determinants for the tissue specificity of SERMs. Science 2002, 295:2465-2468.
39. Shiau A.K., Barstad D., Loria P.M., Cheng L., Kushner P.J., Agard D.A., Greene G.L. The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen. Cell 1998, 95:927-937.
40. Chang C.-Y., Norris J.D., Gron H., Paige L.A., Hamilton P.T., Kenan D.J., Fowlkes D., McDonnell D.P. Dissection of the LXXLL nuclear receptor-coactivator interaction motif using combinatorial peptide libraries: discovery of peptide antagonists of estrogen receptors a and b. Molecular and Cellular Biology 1999, 19:8226-8239.
41. Rodriguez A.L., Tamrazi A., Collins M.L., Katzenellenbogen J.A. Design, synthesis, and in vitro biological evaluation of small molecule inhibitors of estrogen receptor a coactivator binding. Journal of Medicinal Chemistry 2003, 47:600-611.
42. Shao D., Berrodin T.J., Manas E., Hauze D., Powers R., Bapat A., Gonder D., Winneker R.C., Frail D.E. Identification of novel estrogen receptor a antagonists. The Journal of Steroid Biochemistry and Molecular Biology 2004, 88:351-360.
43. Zhou H.-B., Collins M.L., Gunther J.R., Comninos J.S., Katzenellenbogen J.A. Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators. Bioorganic & Medicinal Chemistry Letters 2007, 17:4118-4122.
44. Becerril J., Hamilton Andrew D. Helix mimetics as inhibitors of the interaction of the estrogen receptor with coactivator peptides13. Angewandte Chemie. International Edition 2007, 46:4471-4473.
45. Gunther J.R., Moore T.W., Collins M.L., Katzenellenbogen J.A. Amphipathic benzenes are designed inhibitors of the estrogen receptor α/steroid receptor coactivator interaction. ACS Chemical Biology 2008, 3:282-286.
46. Parent A.A., Gunther J.R., Katzenellenbogen J.A. Blocking estrogen signaling after the hormone: pyrimidine-core inhibitors of estrogen receptor-coactivator binding. Journal of Medicinal Chemistry 2008, 51:6512-6530.
47. LaFrate A.L., Gunther J.R., Carlson K.E., Katzenellenbogen J.A. Synthesis and biological evaluation of guanylhydrazone coactivator binding inhibitors for the estrogen receptor. Bioorganic & Medicinal Chemistry 2008, 16:10075-10084.
48. Wang L.H., Yang X.Y., Zhang X., An P., Kim H.-J., Huang J., Clarke R., Osborne C.K., Inman J.K., Appella E., Farrar W.L. Disruption of estrogen receptor DNA-binding domain and related intramolecular communication restores tamoxifen sensitivity in resistant breast cancer. Cancer Cell 2006, 10:487-499.
49. Redmond A.M., Bane F.T., Stafford A.T., McIlroy M., Dillon M.F., Crotty T.B., Hill A.D., Young L.S. Coassociation of estrogen receptor and p160 proteins predicts resistance to endocrine treatment; SRC-1 is an independent predictor of breast cancer recurrence. Clinical Cancer Research 2009, 15:2098-2106.
50. Arnold L.A., Estebanez-Perpina E., Togashi M., Jouravel N., Shelat A., McReynolds A.C., Mar E., Nguyen P., Baxter J.D., Fletterick R.J., Webb P., Guy R.K. Discovery of small molecule inhibitors of the interaction of the thyroid hormone receptor with transcriptional coregulators. The Journal of Biological Chemistry 2005, 280:43048-43055.
51. Gunther J.R., Parent A.A., Katzenellenbogen J.A. Alternative inhibition of androgen receptor signaling: peptidomimetic pyrimidines as direct androgen receptor/coactivator disruptors. ACS Chemical Biology 2009, 4:435-440.
52. Puigserver P., Adelmant G., Wu Z., Fan M., Xu J., O'Malley B., Spiegelman B.M. Activation of PPAR coactivator-1 through transcription factor docking. Science 1999, 286:1368-1371.
53. Wallberg A.E., Yamamura S., Malik S., Spiegelman B.M., Roeder R.G. Coordination of p300-mediated chromatin remodeling and TRAP/mediator function through coactivator PGC-1a. Molecular Cell 2003, 12:1137-1149.
54. Li S., Liu C., Li N., Hao T., Han T., Hill D.E., Vidal M., Lin J.D. Genome-wide coactivation analysis of PGC-1a identifies BAF60a as a regulator of hepatic lipid metabolism. Cell Metabolism 2008, 8:105-117.
55. Lin J.D. Minireview: the PGC-1 coactivator networks: chromatin-remodeling and mitochondrial energy metabolism. Molecular Endocrinology 2009, 23:2-10.
56. Puigserver P., Wu Z., Park C.W., Graves R., Wright M., Spiegelman B.M. A cold-inducible coactivator of nuclear receptors linked to adaptive thermogenesis. Cell 1998, 92:829-839.
57. Vega R.B., Huss J.M., Kelly D.P. The coactivator PGC-1 cooperates with peroxisome proliferator-activated receptor a in transcriptional control of nuclear genes encoding mitochondrial fatty acid oxidation enzymes. Molecular and Cellular Biology 2000, 20:1868-1876.
58. Huss J.M., Torra I.P., Staels B., Giguere V., Kelly D.P. Estrogen-related receptor a directs peroxisome proliferator-activated receptor a signaling in the transcriptional control of energy metabolism in cardiac and skeletal muscle. Molecular and Cellular Biology 2004, 24:9079-9091.
59. Lin J., Wu H., Tarr P.T., Zhang C.-Y., Wu Z., Boss O., Michael L.F., Puigserver P., Isotani E., Olson E.N., Lowell B.B., Bassel-Duby R., Spiegelman B.M. Transcriptional co-activator PGC-1a drives the formation of slow-twitch muscle fibres. Nature 2002, 418:797-801.
60. Leone T.C., Lehman J.J., Finck B.N., Schaeffer P.J., Wende A.R., Boudina S., Courtois M., Wozniak D.F., Sambandam N., Bernal-Mizrachi C., Chen Z., Holloszy J.O., Medeiros D.M., Schmidt R.E., Saffitz J.E., Abel E.D., Semenkovich C.F., Kelly D.P. PGC-1a deficiency causes multi-system energy metabolic derangements: muscle dysfunction, abnormal weight control and hepatic steatosis. PLoS Biology 2005, 3:e101.
61. Arany Z., Novikov M., Chin S., Ma Y., Rosenzweig A., Spiegelman B.M. Transverse aortic constriction leads to accelerated heart failure in mice lacking PPAR-g coactivator 1a. Proceedings of the National Academy of Sciences 2006, 103:10086-10091.
62. Yoon J.C., Puigserver P., Chen G., Donovan J., Wu Z., Rhee J., Adelmant G., Stafford J., Kahn C.R., Granner D.K., Newgard C.B., Spiegelman B.M. Control of hepatic gluconeogenesis through the transcriptional coactivator PGC-1. Nature 2001, 413:131-138.
63. Michael L.F., Wu Z., Cheatham R.B., Puigserver P., Adelmant G., Lehman J.J., Kelly D.P., Spiegelman B.M. Restoration of insulin-sensitive glucose transporter (GLUT4) gene expression in muscle cells by the transcriptional coactivator PGC-1. Proceedings of the National Academy of Sciences of the United States of America 2001, 98:3820-3825.
64. Patti M.E., Butte A.J., Crunkhorn S., Cusi K., Berria R., Kashyap S., Miyazaki Y., Kohane I., Costello M., Saccone R., Landaker E.J., Goldfine A.B., Mun E., DeFronzo R., Finlayson J., Kahn C.R., Mandarino L.J. Coordinated reduction of genes of oxidative metabolism in humans with insulin resistance and diabetes: potential role of PGC1 and NRF1. Proceedings of the National Academy of Sciences of the United States of America 2003, 100:8466-8471.
65. Hammarstedt A., Jansson P.A., Wesslau C., Yang X., Smith U. Reduced expression of PGC-1 and insulin-signaling molecules in adipose tissue is associated with insulin resistance. Biochemical and Biophysical Research Communications 2003, 301:578-582.
66. Semple R.K., Crowley V.C., Sewter C.P., Laudes M., Christodoulides C., Considine R.V., Vidal-Puig A., O'Rahilly S. Expression of the thermogenic nuclear hormone receptor coactivator PGC-1a is reduced in the adipose tissue of morbidly obese subjects. International Journal of Obesity and Related Metabolic Disorders 2003, 28:176-179.
67. Mootha V.K., Lindgren C.M., Eriksson K.-F., Subramanian A., Sihag S., Lehar J., Puigserver P., Carlsson E., Ridderstrale M., Laurila E., Houstis N., Daly M.J., Patterson N., Mesirov J.P., Golub T.R., Tamayo P., Spiegelman B., Lander E.S., Hirschhorn J.N., Altshuler D., Groop L.C. PGC-1a-responsive genes involved in oxidative phosphorylation are coordinately downregulated in human diabetes. Nature Genetics 2003, 34:267-273.
68. Koo S.-H., Satoh H., Herzig S., Lee C.-H., Hedrick S., Kulkarni R., Evans R.M., Olefsky J., Montminy M. PGC-1 promotes insulin resistance in liver through PPAR-a-dependent induction of TRB-3. Nature Medicine 2004, 10:530-534.
69. Wu Z., Boss O. Targeting PGC-1a to control energy homeostasis. Expert Opinion on Therapeutic Targets 2007, 11:1329-1338.
70. Rodgers J.T., Lerin C., Haas W., Gygi S.P., Spiegelman B.M., Puigserver P. Nutrient control of glucose homeostasis through a complex of PGC-1a and SIRT1. Nature 2005, 434:113-118.
71. Lagouge M., Argmann C., Gerhart-Hines Z., Meziane H., Lerin C., Daussin F., Messadeq N., Milne J., Lambert P., Elliott P., Geny B., Laakso M., Puigserver P., Auwerx J. Resveratrol improves mitochondrial function and protects against metabolic disease by activating SIRT1 and PGC-1a. Cell 2006, 127:1109-1122.
72. Baur J.A., Pearson K.J., Price N.L., Jamieson H.A., Lerin C., Kalra A., Prabhu V.V., Allard J.S., Lopez-Lluch G., Lewis K., Pistell P.J., Poosala S., Becker K.G., Boss O., Gwinn D., Wang M., Ramaswamy S., Fishbein K.W., Spencer R.G., Lakatta E.G., Le Couteur D., Shaw R.J., Navas P., Puigserver P., Ingram D.K., de Cabo R., Sinclair D.A. Resveratrol improves health and survival of mice on a high-calorie diet. Nature 2006, 444:337-342.
73. Beher D., Wu J., Cumine S., Kim K.W., Lu S.-C., Atangan L., Wang M. Resveratrol is not a direct activator of SIRT1 enzyme activity. Chemical Biology & Drug Design 2009, 74:619-624.
74. Palsamy P., Subramanian S. Resveratrol, a natural phytoalexin, normalizes hyperglycemia in streptozotocin-nicotinamide induced experimental diabetic rats. Biomedicine & Pharmacotherapy 2008, 62:598-605.
75. Palsamy P., Subramanian S. Modulatory effects of resveratrol on attenuating the key enzymes activities of carbohydrate metabolism in streptozotocin-nicotinamide-induced diabetic rats. Chemico-Biological Interactions 2009, 179:356-362.
76. Surani M.A., Hayashi K., Hajkova P. Genetic and epigenetic regulators of pluripotency. Cell 2007, 128:747-762.
77. Collado M., Blasco M.A., Serrano M. Cellular senescence in cancer and aging. Cell 2007, 130:223-233.
78. Foster S.L., Medzhitov R. Gene-specific control of the TLR-induced inflammatory response. Clinical Immunology 2009, 130:7-15.
79. Jones P.A., Baylin S.B. The Epigenomics of Cancer. Cell 2007, 128:683-692.
80. Kampranis S.C., Tsichlis P.N., George F.V.W., George K. Chapter 4 histone demethylases and cancer. Advances in Cancer Research 2009, 103-169. Academic Press.
81. Bannister A.J., Schneider R., Kouzarides T. Histone methylation: dynamic or static?. Cell 2002, 109:801-806.
82. Shi Y., Lan F., Matson C., Mulligan P., Whetstine J.R., Cole P.A., Casero R.A., Shi Y. Histone demethylation mediated by the nuclear amine oxidase homolog LSD1. Cell 2004, 119:941-953.
83. Shi Y.-J., Matson C., Lan F., Iwase S., Baba T., Shi Y. Regulation of LSD1 histone demethylase activity by its associated factors. Molecular Cell 2005, 19:857-864.
84. Kouzarides T. Chromatin modifications and their function. Cell 2007, 128:693-705.
85. Shilatifard A. Chromatin modifications by methylation and ubiquitination: implications in the regulation of gene expression. Annual Review of Biochemistry 2006, 75:243-269.
86. Eissenberg J.C., Shilatifard A. Leaving a mark: the many footprints of the elongating RNA polymerase II. Current Opinion in Genetics & Development 2006, 16:184-190.
87. Metzger E., Wissmann M., Yin N., Muller J.M., Schneider R., Peters A.H.F.M., Gunther T., Buettner R., Schule R. LSD1 demethylates repressive histone marks to promote androgen-receptor-dependent transcription. Nature 2005, 437:436-439.
88. Perillo B., Ombra M.N., Bertoni A., Cuozzo C., Sacchetti S., Sasso A., Chiariotti L., Malorni A., Abbondanza C., Avvedimento E.V. DNA oxidation as triggered by H3K9me2 demethylation drives estrogen-induced gene expression. Science 2008, 319:202-206.
89. Huang Y., Greene E., Murray Stewart T., Goodwin A.C., Baylin S.B., Woster P.M., Casero R.A. Inhibition of lysine-specific demethylase 1 by polyamine analogues results in reexpression of aberrantly silenced genes. Proceedings of the National Academy of Sciences 2007, 104:8023-8028.
90. Lee M.G., Wynder C., Schmidt D.M., McCafferty D.G., Shiekhattar R. Histone H3 Lysine 4 demethylation is a target of nonselective antidepressive medications. Chemistry & Biology 2006, 13:563-567.
91. Zhu Q., Liu C., Ge Z., Fang X., Zhang X., Straat K., Bjorkholm M., Xu D. Lysine-specific demethylase 1 (LSD1) is required for the transcriptional repression of the Telomerase Reverse Transcriptase (hTERT) gene. PLoS ONE 2008, 3:e1446.
92. Scoumanne A., Chen X. The lysine-specific demethylase 1 is required for cell proliferation in both p53-dependent and -independent manners. The Journal of Biological Chemistry 2007, 282:15471-15475.
93. Huang J., Sengupta R., Espejo A.B., Lee M.G., Dorsey J.A., Richter M., Opravil S., Shiekhattar R., Bedford M.T., Jenuwein T., Berger S.L. p53 is regulated by the lysine demethylase LSD1. Nature 2007, 449:105-108.
94. Kahl P., Gullotti L., Heukamp L.C., Wolf S., Friedrichs N., Vorreuther R., Solleder G., Bastian P.J., Ellinger J., Metzger E., Schule R., Buettner R. Androgen receptor coactivators lysine-specific histone demethylase 1 and four and a half LIM domain protein 2 predict risk of prostate cancer recurrence. Cancer Research 2006, 66:11341-11347.
95. Wissmann M., Yin N., Muller J.M., Greschik H., Fodor B.D., Jenuwein T., Vogler C., Schneider R., Gunther T., Buettner R., Metzger E., Schule R. Cooperative demethylation by JMJD2C and LSD1 promotes androgen receptor-dependent gene expression. Nature Cell Biology 2007, 9:347-353.
96. Shin S., Janknecht R. Activation of androgen receptor by histone demethylases JMJD2A and JMJD2D. Biochemical and Biophysical Research Communications 2007, 359:742-746.
97. Xiang Y., Zhu Z., Han G., Ye X., Xu B., Peng Z., Ma Y., Yu Y., Lin H., Chen A.P., Chen C.D. JARID1B is a histone H3 lysine 4 demethylase up-regulated in prostate cancer. Proceedings of the National Academy of Sciences 2007, 104:19226-19231.
98. Yamane K., Toumazou C., Tsukada Y.-I., Erdjument-Bromage H., Tempst P., Wong J., Zhang Y. JHDM2A, a JmjC-Containing H3K9 Demethylase, Facilitates Transcription Activation by Androgen Receptor. Cell 2006, 125:483-495.
99. Zou J.X., Revenko A.S., Li L.B., Gemo A.T., Chen H.-W. ANCCA, an estrogen-regulated AAA+ATPase coactivator for ERa, is required for coregulator occupancy and chromatin modification. Proceedings of the National Academy of Sciences 2007, 104:18067-18072.
100. Zou J.X., Guo L., Revenko A.S., Tepper C.G., Gemo A.T., Kung H.-J., Chen H.-W. Androgen-induced coactivator ANCCA mediates specific androgen receptor signaling in prostate cancer. Cancer Research 2009, 69:3339-3346.
101. Ciro M., Prosperini E., Quarto M., Grazini U., Walfridsson J., McBlane F., Nucifero P., Pacchiana G., Capra M., Christensen J., Helin K. ATAD2 is a novel cofactor for MYC, overexpressed and amplified in aggressive tumors. Cancer Research 2009, 69:8491-8498.
102. Hanson P.I., Whiteheart S.W. AAA+proteins: have engine, will work. Nature Reviews Molecular Cell Biology 2005, 6:519-529.
103. Indiani C., O'Donnell M. The replication clamp-loading machine at work in the three domains of life. Nature Reviews Molecular Cell Biology 2006, 7:751-761.
104. Erzberger J.P., Berger J.M. Evolutionary relationships and structural mechanisms of AAA+proteins. Annual Review of Biophysics and Biomolecular Structure 2006, 35:93-114.
105. Burgess S.A., Walker M.L., Sakakibara H., Knight P.J., Oiwa K. Dynein structure and power stroke. Nature 2003, 421:715-718.
106. Siddiqui S.M., Sauer R.T., Baker T.A. Role of the processing pore of the ClpX AAA+ATPase in the recognition and engagement of specific protein substrates. Genes & Development 2004, 18:369-374.
107. Schlieker C., Weibezahn J., Patzelt H., Tessarz P., Strub C., Zeth K., Erbse A., Schneider-Mergener J., Chin J.W., Schultz P.G., Bukau B., Mogk A. Substrate recognition by the AAA+chaperone ClpB. Nature Structural and Molecular Biology 2004, 11:607-615.
108. Martin A., Baker T.A., Sauer R.T. Pore loops of the AAA+ClpX machine grip substrates to drive translocation and unfolding. Nature Structural and Molecular Biology 2008, 15:1147-1151.
109. Hsia E.Y.C., Kalashnikova E.V., Revenko A.S., Zou J.X., Borowsky A.D., Chen H.-W. Deregulated E2F and the AAA+Coregulator ANCCA drive proto-oncogene ACTR/AIB1 overexpression in breast cancer. Molecular Cancer Research 2010, 8:183-193.
110. Wang Y., Klijn J.G.M., Zhang Y., Sieuwerts A.M., Look M.P., Yang F., Talantov D., Timmermans M., Meijer-van Gelder M.E., Yu J., Jatkoe T., Berns E.M.J.J., Atkins D., Foekens J.A. Gene-expression profiles to predict distant metastasis of lymph-node-negative primary breast cancer. Lancet 2005, 365:671-679.
111. Teschendorff A., Naderi A., Barbosa-Morais N., Pinder S., Ellis I., Aparicio S., Brenton J., Caldas C. A consensus prognostic gene expression classifier for ER positive breast cancer. Genome Biology 2006, 7:R101.
112. Ma X.-J., Salunga R., Tuggle J.T., Gaudet J., Enright E., McQuary P., Payette T., Pistone M., Stecker K., Zhang B.M., Zhou Y.-X., Varnholt H., Smith B., Gadd M., Chatfield E., Kessler J., Baer T.M., Erlander M.G., Sgroi D.C. Gene expression profiles of human breast cancer progression. Proceedings of the National Academy of Sciences of the United States of America 2003, 100:5974-5979.
113. van 't Veer L.J., Dai H., van de Vijver M.J., He Y.D., Hart A.A.M., Mao M., Peterse H.L., van der Kooy K., Marton M.J., Witteveen A.T., Schreiber G.J., Kerkhoven R.M., Roberts C., Linsley P.S., Bernards R., Friend S.H. Gene expression profiling predicts clinical outcome of breast cancer. Nature 2002, 415:530-536.
114. Pollack J.R., Sorlie T., Perou C.M., Rees C.A., Jeffrey S.S., Lonning P.E., Tibshirani R., Botstein D., Borresen-Dale A.-L., Brown P.O. Microarray analysis reveals a major direct role of DNA copy number alteration in the transcriptional program of human breast tumors. Proceedings of the National Academy of Sciences of the United States of America 2002, 99:12963-12968.
115. Marmorstein R., Berger S.L. Structure and function of bromodomains in chromatin-regulating complexes. Gene 2001, 272:1-9.
116. Ogura T., Whiteheart S.W., Wilkinson A.J. Conserved arginine residues implicated in ATP hydrolysis, nucleotide-sensing, and inter-subunit interactions in AAA and AAA+ATPases. Journal of Structural Biology 2004, 146:106-112.
117. Privalsky M.L. The role of corepressors in transcriptional regulation by nuclear hormone receptors. Annual Review of Physiology 2004, 66:315-360.
118. Perissi V., Staszewski L.M., McInerney E.M., Kurokawa R., Krones A., Rose D.W., Lambert M.H., Milburn M.V., Glass C.K., Rosenfeld M.G. Molecular determinants of nuclear receptor-corepressor interaction. Genes & Development 1999, 13:3198-3208.
119. Goodson M.L., Jonas B.A., Privalsky M.L. Alternative mRNA splicing of SMRT creates functional diversity by generating corepressor isoforms with different affinities for different nuclear receptors. The Journal of Biological Chemistry 2005, 280:7493-7503.
120. Gurevich I., Flores A.M., Aneskievich B.J. Corepressors of agonist-bound nuclear receptors. Toxicology and Applied Pharmacology 2007, 223:288-298.
121. Heldring N., Pawson T., McDonnell D., Treuter E., Gustafsson J.-Ã.K., Pike A.C.W. Structural insights into corepressor recognition by antagonist-bound estrogen receptors. The Journal of Biological Chemistry 2007, 282:10449-10455.
122. Varlakhanova N., Snyder C., Jose S., Hahm J.B., Privalsky M.L. Estrogen receptors recruit SMRT and N-CoR corepressors through newly recognized contacts between the corepressor N terminus and the receptor DNA binding domain. Molecular and Cellular Biology 2010, 30:1434-1445.
123. Lee C.-H., Chinpaisal C., Wei L.-N. Cloning and characterization of mouse RIP140, a corepressor for nuclear orphan receptor TR2. Molecular and Cellular Biology 1998, 18:6745-6755.
124. Fernandes I., Bastien Y., Wai T., Nygard K., Lin R., Cormier O., Lee H.S., Eng F., Bertos N.R., Pelletier N., Mader S., Han V.K.M., Yang X.-J., White J.H. Ligand-dependent nuclear receptor corepressor LCoR functions by histone deacetylase-dependent and -independent mechanisms. Molecular Cell 2003, 11:139-150.
125. Augereau P., Badia E., Balaguer P., Carascossa S., Castet A., Jalaguier S., Cavaillès V. Negative regulation of hormone signaling by RIP140. The Journal of Steroid Biochemistry and Molecular Biology 2006, 102:51-59.
126. Leonardsson G., Steel J.H., Christian M., Pocock V., Milligan S., Bell J., So P.-W., Medina-Gomez G., Vidal-Puig A., White R., Parker M.G. Nuclear receptor corepressor RIP140 regulates fat accumulation. Proceedings of the National Academy of Sciences of the United States of America 2004, 101:8437-8442.
127. White R., Leonardsson G., Rosewell I., Ann Jacobs M., Milligan S., Parker M. The nuclear receptor co-repressor Nrip1 (RIP140) is essential for female fertility. Nature Medicine 2000, 6:1368-1374.
128. Shi Y., Sawada J.-I., Sui G., Affar E.B., Whetstine J.R., Lan F., Ogawa H., Po-Shan Luke M., Nakatani Y., Shi Y. Coordinated histone modifications mediated by a CtBP co-repressor complex. Nature 2003, 422:735-738.
129. Chinnadurai G. CtBP, an unconventional transcriptional corepressor in development and oncogenesis. Molecular Cell 2002, 9:213-224.
130. Palijan A., Fernandes I., Bastien Y., Tang L., Verway M., Kourelis M., Tavera-Mendoza L.E., Li Z., Bourdeau V., Mader S., Yang X.J., White J.H. Function of histone deacetylase 6 as a cofactor of nuclear receptor coregulator LCoR. The Journal of Biological Chemistry 2009, 284:30264-30274.
131. Palijan A., Fernandes I., Verway M., Kourelis M., Bastien Y., Tavera-Mendoza L.E., Sacheli A., Bourdeau V., Mader S., White J.H. Ligand-dependent corepressor lcor is an attenuator of progesterone-regulated gene expression. The Journal of Biological Chemistry 2009, 284:30275-30287.
132. Lin K.-H., Shieh H.-Y., Chen S.-L., Hsu H.-C. Expression of mutant thyroid hormone nuclear receptors in human hepatocellular carcinoma cells. Molecular Carcinogenesis 1999, 26:53-61.
133. Lin K.-H., Zhu X.-G., Hsu H.-C., Chen S.-L., Shieh H.-Y., Chen S.-T., McPhie P., Cheng S.-Y. Dominant negative activity of mutant thyroid hormone a1 receptors from patients with hepatocellular carcinoma. Endocrinology 1997, 138:5308-5315.
134. Kamiya Y., Puzianowska-Kuznicka M., McPhie P., Nauman J., Cheng S.-Y., Nauman A. Expression of mutant thyroid hormone nuclear receptors is associated with human renal clear cell carcinoma. Carcinogenesis 2002, 23:25-33.
135. Puzianowska-Kuznicka M., Krystyniak A., Madej A., Cheng S.-Y., Nauman J. Functionally impaired TR mutants are present in thyroid papillary cancer. Journal of Clinical Endocrinology & Metabolism 2002, 87:1120-1128.
136. Rosen M.D., Privalsky M.L. Thyroid hormone receptor mutations found in renal clear cell carcinomas alter corepressor release and reveal helix 12 as key determinant of corepressor specificity. Molecular Endocrinology 2009, 23:1183-1192.
137. Thakur M.K., Paramanik V. Role of steroid hormone coregulators in health and disease. Hormone Research in Paediatrics 2009, 71:194-200.
138. Kristensen L.S., Nielsen H.M., Hansen L.L. Epigenetics and cancer treatment. European Journal of Pharmacology 2009, 625:131-142.
139. Lane A.A., Chabner B.A. Histone deacetylase inhibitors in cancer therapy. Journal of Clinical Oncology 2009, 27:5459-5468.
140. Mroz R.M., Noparlik J., Chyczewska E., Braszko J.J., Holownia A. Molecular basis of chronic inflammation in lung diseases: new therapeutic approach. Journal of Physiology and Pharmacology 2007, 58:453-460.
141. Marwick J.A., Ito K., Adcock I.M., Kirkham P.A. Oxidative stress and steroid resistance in asthma and COPD: pharmacological manipulation of HDAC-2 as a therapeutic strategy. Expert Opinion on Therapeutic Targets 2007, 11:745-755.
142. Singh R., Kumar R. MTA family of transcriptional metaregulators in mammary gland morphogenesis and breast cancer. Journal of Mammary Gland Biology and Neoplasia 2007, 12:115-125.
143. Toh Y., Nicolson G. The role of the MTA family and their encoded proteins in human cancers: molecular functions and clinical implications. Clinical & Experimental Metastasis 2009, 26:215-227.
144. Manavathi B., Singh K., Kumar R. MTA family of coregulators in nuclear receptor biology and pathology. Nuclear Receptor Signaling 2007, 5:e010.
145. Kumar R., Wang R.-A., Mazumdar A., Talukder A.H., Mandal M., Yang Z., Bagheri-Yarmand R., Sahin A., Hortobagyi G., Adam L., Barnes C.J., Vadlamudi R.K. A naturally occurring MTA1 variant sequesters oestrogen receptor-a in the cytoplasm. Nature 2002, 418:654-657.
146. Singh R.R., Kaluarachchi K., Chen M., Rayala S.K., Balasenthil S., Ma J., Kumar R. Solution structure and antiestrogenic activity of the unique C-terminal, NR-box motif-containing region of MTA1s. The Journal of Biological Chemistry 2006, 281:25612-25621.