Histone lysine methylation and demethylation pathways in cancer

Biochimica et Biophysica Acta - Reviews on Cancer

Volumn 1815, Issue 1, 2011, Pages 75-89

  Varier, Radhika A ^a   Timmers, H T Marc ^a  

^a UNIVERSITY MEDICAL CENTER UTRECHT   (Netherlands)

Author keywords

Cancer; Chromatin; Epidrugs; Epigenetics; Histone methylation; Menin

Indexed keywords

AZACITIDINE; CHETOCIN; DNA METHYLTRANSFERASE INHIBITOR; ENZYME INHIBITOR; EPIGALLOCATECHIN GALLATE; HISTONE DEACETYLASE INHIBITOR; HISTONE DEMETHYLASE; HISTONE LYSINE DEMETHYLASE; HISTONE LYSINE METHYLTRANSFERASE; HISTONE METHYLTRANSFERASE; HISTONE METHYLTRANSFERASE INHIBITOR; PROTEIN; PROTEIN KDM1; PROTEIN KDM2B; PROTEIN KDM4C; PROTEIN KDM5B; PROTEIN KDM6A; PROTEIN KDM6B; PROTEIN KMT1A; PROTEIN KMT1C; PROTEIN KMT2A; PROTEIN KMT3B; PROTEIN KMT6; PROTEIN KMT8; RETINOBLASTOMA BINDING PROTEIN 2; SINEFUNGIN; TRANSCRIPTION FACTOR EZH2; UNCLASSIFIED DRUG; UNINDEXED DRUG; VORINOSTAT; ZEBULARINE;

CANCER GROWTH; CARCINOGENESIS; CHROMATIN STRUCTURE; DEMETHYLATION; DRUG DESIGN; EPIGENETICS; GENE EXPRESSION; GENOMIC INSTABILITY; HISTONE LYSINE METHYLATION; HISTONE MODIFICATION; HUMAN; MYELODYSPLASTIC SYNDROME; NEOPLASM; NONHUMAN; PRIORITY JOURNAL; PROTEIN METHYLATION; PROTEIN PROCESSING; REVIEW; SKIN LYMPHOMA; T CELL LYMPHOMA;

ANIMALS; EPIGENESIS, GENETIC; HISTONE DEMETHYLASES; HISTONE-LYSINE N-METHYLTRANSFERASE; HISTONES; HUMANS; NEOPLASMS;

EID: 78650582970     PISSN: 0304419X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bbcan.2010.10.002     Document Type: Review

References (230)

1. Berger S.L., Kouzarides T., Shiekhattar R., Shilatifard A. An operational definition of epigenetics. Genes Dev. 2009, 23:781-783.
2. Illingworth R.S., Bird A.P. CpG islands-"a rough guide". FEBS Lett. 2009, 583:1713-1720.
3. Sandelin A., Carninci P., Lenhard B., Ponjavic J., Hayashizaki Y., Hume D.A. Mammalian RNA polymerase II core promoters: insights from genome-wide studies. Nat. Rev. Genet. 2007, 8:424-436.
4. Berger S.L. The complex language of chromatin regulation during transcription. Nature 2007, 447:407-412.
5. Schuettengruber B., Chourrout D., Vervoort M., Leblanc B., Cavalli G. Genome regulation by polycomb and trithorax proteins. Cell 2007, 128:735-745.
6. Bernstein B.E., Mikkelsen T.S., Xie X., Kamal M., Huebert D.J., Cuff J., Fry B., Meissner A., Wernig M., Plath K., Jaenisch R., Wagschal A., Feil R., Schreiber S.L., Lander E.S. A bivalent chromatin structure marks key developmental genes in embryonic stem cells. Cell 2006, 125:315-326.
7. Creyghton M.P., Markoulaki S., Levine S.S., Hanna J., Lodato M.A., Sha K., Young R.A., Jaenisch R., Boyer L.A. H2AZ is enriched at polycomb complex target genes in ES cells and is necessary for lineage commitment. Cell 2008, 135:649-661.
8. Baker L.A., Allis C.D., Wang G.G. PHD fingers in human diseases: disorders arising from misinterpreting epigenetic marks. Mutat. Res. 2008, 647:3-12.
9. Taverna S.D., Li H., Ruthenburg A.J., Allis C.D., Patel D.J. How chromatin-binding modules interpret histone modifications: lessons from professional pocket pickers. Nat. Struct. Mol. Biol. 2007, 14:1025-1040.
10. Peterlin B.M., Price D.H. Controlling the elongation phase of transcription with P-TEFb. Mol. Cell 2006, 23:297-305.
11. Wu C.H., Yamaguchi Y., Benjamin L.R., Horvat-Gordon M., Washinsky J., Enerly E., Larsson J., Lambertsson A., Handa H., Gilmour D. NELF and DSIF cause promoter proximal pausing on the hsp70 promoter in Drosophila. Genes Dev. 2003, 17:1402-1414.
12. Barski A., Cuddapah S., Cui K., Roh T.Y., Schones D.E., Wang Z., Wei G., Chepelev I., Zhao K. High-resolution profiling of histone methylations in the human genome. Cell 2007, 129:823-837.
13. Mosammaparast N., Shi Y. Reversal of histone methylation: biochemical and molecular mechanisms of histone demethylases. Annu. Rev. Biochem. 2010, 79:155-179.
14. Campos E.I., Reinberg D. Histones: annotating chromatin. Annu. Rev. Genet. 2009, 43:559-599.
15. Rando O.J., Chang H.Y. Genome-wide views of chromatin structure. Annu. Rev. Biochem. 2009, 78:245-271.
16. Ruthenburg A.J., Li H., Patel D.J., Allis C.D. Multivalent engagement of chromatin modifications by linked binding modules. Nat. Rev. Mol. Cell Biol. 2007, 8:983-994.
17. Chi P., Allis C.D., Wang G.G. Covalent histone modifications-miswritten, misinterpreted and mis-erased in human cancers. Nat. Rev. Cancer 2010, 10:457-469.
18. Seligson D.B., Horvath S., McBrian M.A., Mah V., Yu H., Tze S., Wang Q., Chia D., Goodglick L., Kurdistani S.K. Global levels of histone modifications predict prognosis in different cancers. Am. J. Pathol. 2009, 174:1619-1628.
19. Barlesi F., Giaccone G., Gallegos-Ruiz M.I., Loundou A., Span S.W., Lefesvre P., Kruyt F.A., Rodriguez J.A. Global histone modifications predict prognosis of resected non small-cell lung cancer. J. Clin. Oncol. 2007, 25:4358-4364.
20. Magerl C., Ellinger J., Braunschweig T., Kremmer E., Koch L.K., Holler T., Buttner R., Luscher B., Gutgemann I. H3K4 dimethylation in hepatocellular carcinoma is rare compared with other hepatobiliary and gastrointestinal carcinomas and correlates with expression of the methylase Ash2 and the demethylase LSD1. Hum. Pathol. 2010, 41:181-189.
21. Elsheikh S.E., Green A.R., Rakha E.A., Powe D.G., Ahmed R.A., Collins H.M., Soria D., Garibaldi J.M., Paish C.E., Ammar A.A., Grainge M.J., Ball G.R., Abdelghany M.K., Martinez-Pomares L., Heery D.M., Ellis I.O. Global histone modifications in breast cancer correlate with tumor phenotypes, prognostic factors, and patient outcome. Cancer Res. 2009, 69:3802-3809.
22. Hess J.L. MLL: a histone methyltransferase disrupted in leukemia. Trends Mol. Med. 2004, 10:500-507.
23. Krivtsov A.V., Armstrong S.A. MLL translocations, histone modifications and leukaemia stem-cell development. Nat. Rev. Cancer 2007, 7:823-833.
24. Muntean A.G., Hess J.L. Epigenetic dysregulation in cancer. Am. J. Pathol. 2009, 175:1353-1361.
25. Yu B.D., Hess J.L., Horning S.E., Brown G.A., Korsmeyer S.J. Altered Hox expression and segmental identity in Mll-mutant mice. Nature 1995, 378:505-508.
26. Shah N., Sukumar S. The Hox genes and their roles in oncogenesis. Nat. Rev. Cancer 2010, 10:361-371.
27. Ayton P.M., Cleary M.L. Transformation of myeloid progenitors by MLL oncoproteins is dependent on Hoxa7 and Hoxa9. Genes Dev. 2003, 17:2298-2307.
28. Mueller D., Bach C., Zeisig D., Garcia-Cuellar M.P., Monroe S., Sreekumar A., Zhou R., Nesvizhskii A., Chinnaiyan A., Hess J.L., Slany R.K. A role for the MLL fusion partner ENL in transcriptional elongation and chromatin modification. Blood 2007, 110:4445-4454.
29. Feng Q., Wang H., Ng H.H., Erdjument-Bromage H., Tempst P., Struhl K., Zhang Y. Methylation of H3-lysine 79 is mediated by a new family of HMTases without a SET domain. Curr. Biol. 2002, 12:1052-1058.
30. van Leeuwen F., Gafken P.R., Gottschling D.E. Dot1p modulates silencing in yeast by methylation of the nucleosome core. Cell 2002, 109:745-756.
31. Mohan M., Herz H.M., Takahashi Y.H., Lin C., Lai K.C., Zhang Y., Washburn M.P., Florens L., Shilatifard A. Linking H3K79 trimethylation to Wnt signaling through a novel Dot1-containing complex. Genes Dev. 2010, 24:574-589.
32. Mohan M., Lin C., Guest E., Shilatifard A. Licensed to elongate: a molecular mechanism for MLL-based leukaemogenesis. Nat. Rev. Cancer 2010, 10:721-728.
33. Okada Y., Feng Q., Lin Y., Jiang Q., Li Y., Coffield V.M., Su L., Xu G., Zhang Y. hDOT1L links histone methylation to leukemogenesis. Cell 2005, 121:167-178.
34. Thiel A.T., Blessington P., Zou T., Feather D., Wu X., Yan J., Zhang H., Liu Z., Ernst P., Koretzky G.A., Hua X. MLL-AF9-induced leukemogenesis requires coexpression of the wild-type Mll allele. Cancer Cell 2010, 17:148-159.
35. Lin C., Smith E.R., Takahashi H., Lai K.C., Martin-Brown S., Florens L., Washburn M.P., Conaway J.W., Conaway R.C., Shilatifard A. AFF4, a component of the ELL/P-TEFb elongation complex and a shared subunit of MLL chimeras, can link transcription elongation to leukemia. Mol. Cell 2010, 37:429-437.
36. Miremadi A., Oestergaard M.Z., Pharoah P.D., Caldas C. Cancer genetics of epigenetic genes. Hum. Mol. Genet. 2007, 16(Spec No 1):R28-R49.
37. Balakrishnan A., Bleeker F.E., Lamba S., Rodolfo M., Daniotti M., Scarpa A., van Tilborg A.A., Leenstra S., Zanon C., Bardelli A. Novel somatic and germline mutations in cancer candidate genes in glioblastoma, melanoma, and pancreatic carcinoma. Cancer Res. 2007, 67:3545-3550.
38. Huntsman D.G., Chin S.F., Muleris M., Batley S.J., Collins V.P., Wiedemann L.M., Aparicio S., Caldas C. MLL2, the second human homolog of the Drosophila trithorax gene, maps to 19q13.1 and is amplified in solid tumor cell lines. Oncogene 1999, 18:7975-7984.
39. Prasad R., Zhadanov A.B., Sedkov Y., Bullrich F., Druck T., Rallapalli R., Yano T., Alder H., Croce C.M., Huebner K., Mazo A., Canaani E. Structure and expression pattern of human ALR, a novel gene with strong homology to ALL-1 involved in acute leukemia and to Drosophila trithorax. Oncogene 1997, 15:549-560.
40. Ruault M., Brun M.E., Ventura M., Roizes G., De Sario A. MLL3, a new human member of the TRX/MLL gene family, maps to 7q36, a chromosome region frequently deleted in myeloid leukaemia. Gene 2002, 284:73-81.
41. Heuser M., Yap D.B., Leung M., de Algara T.R., Tafech A., McKinney S., Dixon J., Thresher R., Colledge B., Carlton M., Humphries R.K., Aparicio S.A. Loss of MLL5 results in pleiotropic hematopoietic defects, reduced neutrophil immune function, and extreme sensitivity to DNA demethylation. Blood 2009, 113:1432-1443.
42. Madan V., Madan B., Brykczynska U., Zilbermann F., Hogeveen K., Dohner K., Dohner H., Weber O., Blum C., Rodewald H.R., Sassone-Corsi P., Peters A.H., Fehling H.J. Impaired function of primitive hematopoietic cells in mice lacking the Mixed-Lineage-Leukemia homolog MLL5. Blood 2009, 113:1444-1454.
43. Sebastian S., Sreenivas P., Sambasivan R., Cheedipudi S., Kandalla P., Pavlath G.K., Dhawan J. MLL5, a trithorax homolog, indirectly regulates H3K4 methylation, represses cyclin A2 expression, and promotes myogenic differentiation. Proc. Natl Acad. Sci. USA 2009, 106:4719-4724.
44. Zhang Y., Wong J., Klinger M., Tran M.T., Shannon K.M., Killeen N. MLL5 contributes to hematopoietic stem cell fitness and homeostasis. Blood 2009, 113:1455-1463.
45. Marx S.J., Stratakis C.A. Multiple endocrine neoplasia-introduction. J. Intern. Med. 2005, 257:2-5.
46. Chandrasekharappa S.C., Guru S.C., Manickam P., Olufemi S.E., Collins F.S., Emmert-Buck M.R., Debelenko L.V., Zhuang Z., Lubensky I.A., Liotta L.A., Crabtree J.S., Wang Y., Roe B.A., Weisemann J., Boguski M.S., Agarwal S.K., Kester M.B., Kim Y.S., Heppner C., Dong Q., Spiegel A.M., Burns A.L., Marx S.J. Positional cloning of the gene for multiple endocrine neoplasia-type 1. Science 1997, 276:404-407.
47. Guru S.C., Goldsmith P.K., Burns A.L., Marx S.J., Spiegel A.M., Collins F.S., Chandrasekharappa S.C. Menin, the product of the MEN1 gene, is a nuclear protein. Proc. Natl Acad. Sci. USA 1998, 95:1630-1634.
48. Hughes C.M., Rozenblatt-Rosen O., Milne T.A., Copeland T.D., Levine S.S., Lee J.C., Hayes D.N., Shanmugam K.S., Bhattacharjee A., Biondi C.A., Kay G.F., Hayward N.K., Hess J.L., Meyerson M. Menin associates with a trithorax family histone methyltransferase complex and with the hoxc8 locus. Mol. Cell 2004, 13:587-597.
49. Yokoyama A., Wang Z., Wysocka J., Sanyal M., Aufiero D.J., Kitabayashi I., Herr W., Cleary M.L. Leukemia proto-oncoprotein MLL forms a SET1-like histone methyltransferase complex with menin to regulate Hox gene expression. Mol. Cell. Biol. 2004, 24:5639-5649.
50. Bertolino P., Radovanovic I., Casse H., Aguzzi A., Wang Z.Q., Zhang C.X. Genetic ablation of the tumor suppressor menin causes lethality at mid-gestation with defects in multiple organs. Mech. Dev. 2003, 120:549-560.
51. Bertolino P., Tong W.M., Galendo D., Wang Z.Q., Zhang C.X. Heterozygous Men1 mutant mice develop a range of endocrine tumors mimicking multiple endocrine neoplasia type 1. Mol. Endocrinol. 2003, 17:1880-1892.
52. Bai F., Pei X.H., Nishikawa T., Smith M.D., Xiong Y. p18Ink4c, but not p27Kip1, collaborates with Men1 to suppress neuroendocrine organ tumors. Mol. Cell. Biol. 2007, 27:1495-1504.
53. Karnik S.K., Hughes C.M., Gu X., Rozenblatt-Rosen O., McLean G.W., Xiong Y., Meyerson M., Kim S.K. Menin regulates pancreatic islet growth by promoting histone methylation and expression of genes encoding p27Kip1 and p18INK4c. Proc. Natl Acad. Sci. USA 2005, 102:14659-14664.
54. Pei X.H., Bai F., Smith M.D., Xiong Y. p18Ink4c collaborates with Men1 to constrain lung stem cell expansion and suppress non-small-cell lung cancers. Cancer Res. 2007, 67:3162-3170.
55. Jager R., List B., Knabbe C., Souttou B., Raulais D., Zeiler T., Wellstein A., Aigner A., Neubauer A., Zugmaier G. Serum levels of the angiogenic factor pleiotrophin in relation to disease stage in lung cancer patients. Br. J. Cancer 2002, 86:858-863.
56. La P., Schnepp R.W., D.P.C, C.S.A, Hua X. Tumor suppressor menin regulates expression of insulin-like growth factor binding protein 2. Endocrinology 2004, 145:3443-3450.
57. Perez-Pinera P., Chang Y., Deuel T.F. Pleiotrophin, a multifunctional tumor promoter through induction of tumor angiogenesis, remodeling of the tumor microenvironment, and activation of stromal fibroblasts. Cell Cycle 2007, 6:2877-2883.
58. Gao S.B., Feng Z.J., Xu B., Wu Y., Yin P., Yang Y., Hua X., Jin G.H. Suppression of lung adenocarcinoma through menin and polycomb gene-mediated repression of growth factor pleiotrophin. Oncogene 2009, 28:4095-4104.
59. Perez-Pinera P., Chang Y., Astudillo A., Mortimer J., Deuel T.F. Anaplastic lymphoma kinase is expressed in different subtypes of human breast cancer. Biochem. Biophys. Res. Commun. 2007, 358:399-403.
60. Dreijerink K.M., Mulder K.W., Winkler G.S., Hoppener J.W., Lips C.J., Timmers H.T. Menin links estrogen receptor activation to histone H3K4 trimethylation. Cancer Res. 2006, 66:4929-4935.
61. Imachi H., Murao K., Dobashi H., Bhuyan M.M., Cao X., Kontani K., Niki S., Murazawa C., Nakajima H., Kohno N., Yamashita H., Iwase H., Hayashi S.I., Ishida T., Yamauchi A. Menin, a product of the MENI gene, binds to estrogen receptor to enhance its activity in breast cancer cells: possibility of a novel predictive factor for tamoxifen resistance. Breast Cancer Res. Treat. 2009, 122:395-407.
62. Chen Y.X., Yan J., Keeshan K., Tubbs A.T., Wang H., Silva A., Brown E.J., Hess J.L., Pear W.S., Hua X. The tumor suppressor menin regulates hematopoiesis and myeloid transformation by influencing Hox gene expression. Proc. Natl Acad. Sci. USA 2006, 103:1018-1023.
63. Yokoyama A., Somervaille T.C., Smith K.S., Rozenblatt-Rosen O., Meyerson M., Cleary M.L. The menin tumor suppressor protein is an essential oncogenic cofactor for MLL-associated leukemogenesis. Cell 2005, 123:207-218.
64. Karnik S.K., Chen H., McLean G.W., Heit J.J., Gu X., Zhang A.Y., Fontaine M., Yen M.H., Kim S.K. Menin controls growth of pancreatic beta-cells in pregnant mice and promotes gestational diabetes mellitus. Science 2007, 318:806-809.
65. Paris P.L., Andaya A., Fridlyand J., Jain A.N., Weinberg V., Kowbel D., Brebner J.H., Simko J., Watson J.E., Volik S., Albertson D.G., Pinkel D., Alers J.C., van der Kwast T.H., Vissers K.J., Schroder F.H., Wildhagen M.F., Febbo P.G., Chinnaiyan A.M., Pienta K.J., Carroll P.R., Rubin M.A., Collins C., van Dekken H. Whole genome scanning identifies genotypes associated with recurrence and metastasis in prostate tumors. Hum. Mol. Genet. 2004, 13:1303-1313.
66. Lapointe J., Li C., Higgins J.P., van de Rijn M., Bair E., Montgomery K., Ferrari M., Egevad L., Rayford W., Bergerheim U., Ekman P., DeMarzo A.M., Tibshirani R., Botstein D., Brown P.O., Brooks J.D., Pollack J.R. Gene expression profiling identifies clinically relevant subtypes of prostate cancer. Proc. Natl Acad. Sci. USA 2004, 101:811-816.
67. Paris P.L., Sridharan S., Hittelman A.B., Kobayashi Y., Perner S., Huang G., Simko J., Carroll P., Rubin M.A., Collins C. An oncogenic role for the multiple endocrine neoplasia type 1 gene in prostate cancer. Prostate Cancer Prostatic Dis. 2009, 12:184-191.
68. Dreijerink K.M., Varier R.A., van Beekum O., Jeninga E.H., Hoppener J.W., Lips C.J., Kummer J.A., Kalkhoven E., Timmers H.T. The multiple endocrine neoplasia type 1 (MEN1) tumor suppressor regulates peroxisome proliferator-activated receptor gamma-dependent adipocyte differentiation. Mol. Cell. Biol. 2009, 29:5060-5069.
69. Dreijerink K.M., Varier R.A., van Nuland R., Broekhuizen R., Valk G.D., van der Wal J.E., Lips C.J., Kummer J.A., Timmers H.T. Regulation of vitamin D receptor function in MEN1-related parathyroid adenomas. Mol. Cell. Endocrinol. 2009, 313:1-8.
70. Mo R., Rao S.M., Zhu Y.J. Identification of the MLL2 complex as a coactivator for estrogen receptor alpha. J. Biol. Chem. 2006, 281:15714-15720.
71. Yokoyama A., Cleary M.L. Menin critically links MLL proteins with LEDGF on cancer-associated target genes. Cancer Cell 2008, 14:36-46.
72. Xu S., Powers M.A. Nuclear pore proteins and cancer. Semin. Cell Dev. Biol. 2009, 20:620-630.
73. Wu X., Hua X. Menin, histone h3 methyltransferases, and regulation of cell proliferation: current knowledge and perspective. Curr. Mol. Med. 2008, 8:805-815.
74. Gracanin A., Dreijerink K.M., van der Luijt R.B., Lips C.J., Hoppener J.W. Tissue selectivity in multiple endocrine neoplasia type 1-associated tumorigenesis. Cancer Res. 2009, 69:6371-6374.
75. Dou Y., Milne T.A., Ruthenburg A.J., Lee S., Lee J.W., Verdine G.L., Allis C.D., Roeder R.G. Regulation of MLL1 H3K4 methyltransferase activity by its core components. Nat. Struct. Mol. Biol. 2006, 13:713-719.
76. Luscher-Firzlaff J., Gawlista I., Vervoorts J., Kapelle K., Braunschweig T., Walsemann G., Rodgarkia-Schamberger C., Schuchlautz H., Dreschers S., Kremmer E., Lilischkis R., Cerni C., Wellmann A., Luscher B. The human trithorax protein hASH2 functions as an oncoprotein. Cancer Res. 2008, 68:749-758.
77. Hamamoto R., Furukawa Y., Morita M., Iimura Y., Silva F.P., Li M., Yagyu R., Nakamura Y. SMYD3 encodes a histone methyltransferase involved in the proliferation of cancer cells. Nat. Cell Biol. 2004, 6:731-740.
78. Hamamoto R., Silva F.P., Tsuge M., Nishidate T., Katagiri T., Nakamura Y., Furukawa Y. Enhanced SMYD3 expression is essential for the growth of breast cancer cells. Cancer Sci. 2006, 97:113-118.
79. Kim H., Heo K., Kim J.H., Kim K., Choi J., An W. Requirement of histone methyltransferase SMYD3 for estrogen receptor-mediated transcription. J. Biol. Chem. 2009, 284:19867-19877.
80. Silva F.P., Hamamoto R., Kunizaki M., Tsuge M., Nakamura Y., Furukawa Y. Enhanced methyltransferase activity of SMYD3 by the cleavage of its N-terminal region in human cancer cells. Oncogene 2008, 27:2686-2692.
81. Kirmizis A., Bartley S.M., Kuzmichev A., Margueron R., Reinberg D., Green R., Farnham P.J. Silencing of human polycomb target genes is associated with methylation of histone H3 Lys 27. Genes Dev. 2004, 18:1592-1605.
82. Li G., Margueron R., Ku M., Chambon P., Bernstein B.E., Reinberg D. Jarid2 and PRC2, partners in regulating gene expression. Genes Dev. 2010, 24:368-380.
83. Pasini D., Cloos P.A., Walfridsson J., Olsson L., Bukowski J.P., Johansen J.V., Bak M., Tommerup N., Rappsilber J., Helin K. JARID2 regulates binding of the Polycomb repressive complex 2 to target genes in ES cells. Nature 2010, 464:306-310.
84. Varambally S., Dhanasekaran S.M., Zhou M., Barrette T.R., Kumar-Sinha C., Sanda M.G., Ghosh D., Pienta K.J., Sewalt R.G., Otte A.P., Rubin M.A., Chinnaiyan A.M. The polycomb group protein EZH2 is involved in progression of prostate cancer. Nature 2002, 419:624-629.
85. Rhodes D.R., Sanda M.G., Otte A.P., Chinnaiyan A.M., Rubin M.A. Multiplex biomarker approach for determining risk of prostate-specific antigen-defined recurrence of prostate cancer. J. Natl Cancer Inst. 2003, 95:661-668.
86. Saramaki O.R., Tammela T.L., Martikainen P.M., Vessella R.L., Visakorpi T. The gene for polycomb group protein enhancer of zeste homolog 2 (EZH2) is amplified in late-stage prostate cancer. Genes Chromosom. Cancer 2006, 45:639-645.
87. Kleer C.G., Cao Q., Varambally S., Shen R., Ota I., Tomlins S.A., Ghosh D., Sewalt R.G., Otte A.P., Hayes D.F., Sabel M.S., Livant D., Weiss S.J., Rubin M.A., Chinnaiyan A.M. EZH2 is a marker of aggressive breast cancer and promotes neoplastic transformation of breast epithelial cells. Proc. Natl Acad. Sci. USA 2003, 100:11606-11611.
88. Yu J., Yu J., Rhodes D.R., Tomlins S.A., Cao X., Chen G., Mehra R., Wang X., Ghosh D., Shah R.B., Varambally S., Pienta K.J., Chinnaiyan A.M. A polycomb repression signature in metastatic prostate cancer predicts cancer outcome. Cancer Res. 2007, 67:10657-10663.
89. Steele J.C., Torr E.E., Noakes K.L., Kalk E., Moss P.A., Reynolds G.M., Hubscher S.G., van Lohuizen M., Adams D.H., Young L.S. The polycomb group proteins, BMI-1 and EZH2, are tumour-associated antigens. Br. J. Cancer 2006, 95:1202-1211.
90. Morin R.D., Johnson N.A., Severson T.M., Mungall A.J., An J., Goya R., Paul J.E., Boyle M., Woolcock B.W., Kuchenbauer F., Yap D., Humphries R.K., Griffith O.L., Shah S., Zhu H., Kimbara M., Shashkin P., Charlot J.F., Tcherpakov M., Corbett R., Tam A., Varhol R., Smailus D., Moksa M., Zhao Y., Delaney A., Qian H., Birol I., Schein J., Moore R., Holt R., Horsman D.E., Connors J.M., Jones S., Aparicio S., Hirst M., Gascoyne R.D., Marra M.A. Somatic mutations altering EZH2 (Tyr641) in follicular and diffuse large B-cell lymphomas of germinal-center origin. Nat. Genet. 2010, 42:181-185.
91. Rea S., Eisenhaber F., O'Carroll D., Strahl B.D., Sun Z.W., Schmid M., Opravil S., Mechtler K., Ponting C.P., Allis C.D., Jenuwein T. Regulation of chromatin structure by site-specific histone H3 methyltransferases. Nature 2000, 406:593-599.
92. O'Carroll D., Scherthan H., Peters A.H., Opravil S., Haynes A.R., Laible G., Rea S., Schmid M., Lebersorger A., Jerratsch M., Sattler L., Mattei M.G., Denny P., Brown S.D., Schweizer D., Jenuwein T. Isolation and characterization of Suv39h2, a second histone H3 methyltransferase gene that displays testis-specific expression. Mol. Cell. Biol. 2000, 20:9423-9433.
93. Rice J.C., Briggs S.D., Ueberheide B., Barber C.M., Shabanowitz J., Hunt D.F., Shinkai Y., Allis C.D. Histone methyltransferases direct different degrees of methylation to define distinct chromatin domains. Mol. Cell 2003, 12:1591-1598.
94. Peters A.H., O'Carroll D., Scherthan H., Mechtler K., Sauer S., Schofer C., Weipoltshammer K., Pagani M., Lachner M., Kohlmaier A., Opravil S., Doyle M., Sibilia M., Jenuwein T. Loss of the Suv39h histone methyltransferases impairs mammalian heterochromatin and genome stability. Cell 2001, 107:323-337.
95. Nielsen S.J., Schneider R., Bauer U.M., Bannister A.J., Morrison A., O'Carroll D., Firestein R., Cleary M., Jenuwein T., Herrera R.E., Kouzarides T. Rb targets histone H3 methylation and HP1 to promoters. Nature 2001, 412:561-565.
96. Ozdag H., Teschendorff A.E., Ahmed A.A., Hyland S.J., Blenkiron C., Bobrow L., Veerakumarasivam A., Burtt G., Subkhankulova T., Arends M.J., Collins V.P., Bowtell D., Kouzarides T., Brenton J.D., Caldas C. Differential expression of selected histone modifier genes in human solid cancers. BMC Genomics 2006, 7:90.
97. Tachibana M., Sugimoto K., Fukushima T., Shinkai Y. Set domain-containing protein, G9a, is a novel lysine-preferring mammalian histone methyltransferase with hyperactivity and specific selectivity to lysines 9 and 27 of histone H3. J. Biol. Chem. 2001, 276:25309-25317.
98. Tachibana M., Sugimoto K., Nozaki M., Ueda J., Ohta T., Ohki M., Fukuda M., Takeda N., Niida H., Kato H., Shinkai Y. G9a histone methyltransferase plays a dominant role in euchromatic histone H3 lysine 9 methylation and is essential for early embryogenesis. Genes Dev. 2002, 16:1779-1791.
99. Tachibana M., Ueda J., Fukuda M., Takeda N., Ohta T., Iwanari H., Sakihama T., Kodama T., Hamakubo T., Shinkai Y. Histone methyltransferases G9a and GLP form heteromeric complexes and are both crucial for methylation of euchromatin at H3-K9. Genes Dev. 2005, 19:815-826.
100. Kondo Y., Shen L., Suzuki S., Kurokawa T., Masuko K., Tanaka Y., Kato H., Mizuno Y., Yokoe M., Sugauchi F., Hirashima N., Orito E., Osada H., Ueda R., Guo Y., Chen X., Issa J.P., Sekido Y. Alterations of DNA methylation and histone modifications contribute to gene silencing in hepatocellular carcinomas. Hepatol. Res. 2007, 37:974-983.
101. Lee S.H., Kim J., Kim W.H., Lee Y.M. Hypoxic silencing of tumor suppressor RUNX3 by histone modification in gastric cancer cells. Oncogene 2009, 28:184-194.
102. Kim K.C., Geng L., Huang S. Inactivation of a histone methyltransferase by mutations in human cancers. Cancer Res. 2003, 63:7619-7623.
103. Buyse I.M., Shao G., Huang S. The retinoblastoma protein binds to RIZ, a zinc-finger protein that shares an epitope with the adenovirus E1A protein. Proc. Natl Acad. Sci. USA 1995, 92:4467-4471.
104. Steele-Perkins G., Fang W., Yang X.H., Van Gele M., Carling T., Gu J., Buyse I.M., Fletcher J.A., Liu J., Bronson R., Chadwick R.B., de la Chapelle A., Zhang X., Speleman F., Huang S. Tumor formation and inactivation of RIZ1, an Rb-binding member of a nuclear protein-methyltransferase superfamily. Genes Dev. 2001, 15:2250-2262.
105. Du Y., Carling T., Fang W., Piao Z., Sheu J.C., Huang S. Hypermethylation in human cancers of the RIZ1 tumor suppressor gene, a member of a histone/protein methyltransferase superfamily. Cancer Res. 2001, 61:8094-8099.
106. Tokumaru Y., Nomoto S., Jeronimo C., Henrique R., Harden S., Trink B., Sidransky D. Biallelic inactivation of the RIZ1 gene in human gastric cancer. Oncogene 2003, 22:6954-6958.
107. Rayasam G.V., Wendling O., Angrand P.O., Mark M., Niederreither K., Song L., Lerouge T., Hager G.L., Chambon P., Losson R. NSD1 is essential for early post-implantation development and has a catalytically active SET domain. EMBO J. 2003, 22:3153-3163.
108. Wang G.G., Cai L., Pasillas M.P., Kamps M.P. NUP98-NSD1 links H3K36 methylation to Hox-A gene activation and leukaemogenesis. Nat. Cell Biol. 2007, 9:804-812.
109. Jaju R.J., Fidler C., Haas O.A., Strickson A.J., Watkins F., Clark K., Cross N.C., Cheng J.F., Aplan P.D., Kearney L., Boultwood J., Wainscoat J.S. A novel gene, NSD1, is fused to NUP98 in the t(5;11)(q35;p15.5) in de novo childhood acute myeloid leukemia. Blood 2001, 98:1264-1267.
110. Tatton-Brown K., Douglas J., Coleman K., Baujat G., Cole T.R., Das S., Horn D., Hughes H.E., Temple I.K., Faravelli F., Waggoner D., Turkmen S., Cormier-Daire V., Irrthum A., Rahman N. Genotype-phenotype associations in Sotos syndrome: an analysis of 266 individuals with NSD1 aberrations. Am. J. Hum. Genet. 2005, 77:193-204.
111. Hersh J.H., Cole T.R., Bloom A.S., Bertolone S.J., Hughes H.E. Risk of malignancy in Sotos syndrome. J. Pediatr. 1992, 120:572-574.
112. Berdasco M., Ropero S., Setien F., Fraga M.F., Lapunzina P., Losson R., Alaminos M., Cheung N.K., Rahman N., Esteller M. Epigenetic inactivation of the Sotos overgrowth syndrome gene histone methyltransferase NSD1 in human neuroblastoma and glioma. Proc. Natl Acad. Sci. USA 2009, 106:21830-21835.
113. Chesi M., Nardini E., Lim R.S., Smith K.D., Kuehl W.M., Bergsagel P.L. The t(4;14) translocation in myeloma dysregulates both FGFR3 and a novel gene, MMSET, resulting in IgH/MMSET hybrid transcripts. Blood 1998, 92:3025-3034.
114. Keats J.J., Reiman T., Maxwell C.A., Taylor B.J., Larratt L.M., Mant M.J., Belch A.R., Pilarski L.M. In multiple myeloma, t(4;14)(p16;q32) is an adverse prognostic factor irrespective of FGFR3 expression. Blood 2003, 101:1520-1529.
115. Marango J., Shimoyama M., Nishio H., Meyer J.A., Min D.J., Sirulnik A., Martinez-Martinez Y., Chesi M., Bergsagel P.L., Zhou M.M., Waxman S., Leibovitch B.A., Walsh M.J., Licht J.D. The MMSET protein is a histone methyltransferase with characteristics of a transcriptional corepressor. Blood 2008, 111:3145-3154.
116. Li Y., Trojer P., Xu C.F., Cheung P., Kuo A., Drury W.J., Qiao Q., Neubert T.A., Xu R.M., Gozani O., Reinberg D. The target of the NSD family of histone lysine methyltransferases depends on the nature of the substrate. J. Biol. Chem. 2009, 284:34283-34295.
117. Nimura K., Ura K., Shiratori H., Ikawa M., Okabe M., Schwartz R.J., Kaneda Y. A histone H3 lysine 36 trimethyltransferase links Nkx2-5 to Wolf-Hirschhorn syndrome. Nature 2009, 460:287-291.
118. Li J., Yin C., Okamoto H., Mushlin H., Balgley B.M., Lee C.S., Yuan K., Ikejiri B., Glasker S., Vortmeyer A.O., Oldfield E.H., Weil R.J., Zhuang Z. Identification of a novel proliferation-related protein, WHSC1 4a, in human gliomas. Neurooncol. 2008, 10:45-51.
119. Kassambara A., Klein B., Moreaux J. MMSET is overexpressed in cancers: link with tumor aggressiveness. Biochem. Biophys. Res. Commun. 2009, 379:840-845.
120. Angrand P.O., Apiou F., Stewart A.F., Dutrillaux B., Losson R., Chambon P. NSD3, a new SET domain-containing gene, maps to 8p12 and is amplified in human breast cancer cell lines. Genomics 2001, 74:79-88.
121. Rosati R., La Starza R., Veronese A., Aventin A., Schwienbacher C., Vallespi T., Negrini M., Martelli M.F., Mecucci C. NUP98 is fused to the NSD3 gene in acute myeloid leukemia associated with t(8;11)(p11.2;p15). Blood 2002, 99:3857-3860.
122. Kim S.M., Kee H.J., Eom G.H., Choe N.W., Kim J.Y., Kim Y.S., Kim S.K., Kook H., Kook H., Seo S.B. Characterization of a novel WHSC1-associated SET domain protein with H3K4 and H3K27 methyltransferase activity. Biochem. Biophys. Res. Commun. 2006, 345:318-323.
123. 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.
124. Metzger E., Wissmann M., Yin N., Muller J.M., Schneider R., Peters A.H., Gunther T., Buettner R., Schule R. LSD1 demethylates repressive histone marks to promote androgen-receptor-dependent transcription. Nature 2005, 437:436-439.
125. 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. Nat. Cell Biol. 2007, 9:347-353.
126. 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 Res. 2006, 66:11341-11347.
127. Schulte J.H., Lim S., Schramm A., Friedrichs N., Koster J., Versteeg R., Ora I., Pajtler K., Klein-Hitpass L., Kuhfittig-Kulle S., Metzger E., Schule R., Eggert A., Buettner R., Kirfel J. Lysine-specific demethylase 1 is strongly expressed in poorly differentiated neuroblastoma: implications for therapy. Cancer Res. 2009, 69:2065-2071.
128. Lim S., Janzer A., Becker A., Zimmer A., Schule R., Buettner R., Kirfel J. Lysine-specific demethylase 1 (LSD1) is highly expressed in ER-negative breast cancers and a biomarker predicting aggressive biology. Carcinogenesis 2010, 31:512-520.
129. Frescas D., Guardavaccaro D., Bassermann F., Koyama-Nasu R., Pagano M. JHDM1B/FBXL10 is a nucleolar protein that represses transcription of ribosomal RNA genes. Nature 2007, 450:309-313.
130. He J., Kallin E.M., Tsukada Y., Zhang Y. The H3K36 demethylase Jhdm1b/Kdm2b regulates cell proliferation and senescence through p15(Ink4b). Nat. Struct. Mol. Biol. 2008, 15:1169-1175.
131. Cloos P.A., Christensen J., Agger K., Helin K. Erasing the methyl mark: histone demethylases at the center of cellular differentiation and disease. Genes Dev. 2008, 22:1115-1140.
132. Suzuki T., Minehata K., Akagi K., Jenkins N.A., Copeland N.G. Tumor suppressor gene identification using retroviral insertional mutagenesis in Blm-deficient mice. EMBO J. 2006, 25:3422-3431.
133. Bredel M., Bredel C., Juric D., Harsh G.R., Vogel H., Recht L.D., Sikic B.I. Functional network analysis reveals extended gliomagenesis pathway maps and three novel MYC-interacting genes in human gliomas. Cancer Res. 2005, 65:8679-8689.
134. Freije W.A., Castro-Vargas F.E., Fang Z., Horvath S., Cloughesy T., Liau L.M., Mischel P.S., Nelson S.F. Gene expression profiling of gliomas strongly predicts survival. Cancer Res. 2004, 64:6503-6510.
135. Cloos P.A., Christensen J., Agger K., Maiolica A., Rappsilber J., Antal T., Hansen K.H., Helin K. The putative oncogene GASC1 demethylates tri- and dimethylated lysine 9 on histone H3. Nature 2006, 442:307-311.
136. Liu G., Bollig-Fischer A., Kreike B., van de Vijver M.J., Abrams J., Ethier S.P., Yang Z.Q. Genomic amplification and oncogenic properties of the GASC1 histone demethylase gene in breast cancer. Oncogene 2009, 28:4491-4500.
137. Ehrbrecht A., Muller U., Wolter M., Hoischen A., Koch A., Radlwimmer B., Actor B., Mincheva A., Pietsch T., Lichter P., Reifenberger G., Weber R.G. Comprehensive genomic analysis of desmoplastic medulloblastomas: identification of novel amplified genes and separate evaluation of the different histological components. J. Pathol. 2006, 208:554-563.
138. Italiano A., Attias R., Aurias A., Perot G., Burel-Vandenbos F., Otto J., Venissac N., Pedeutour F. Molecular cytogenetic characterization of a metastatic lung sarcomatoid carcinoma: 9p23 neocentromere and 9p23-p24 amplification including JAK2 and JMJD2C. Cancer Genet. Cytogenet. 2006, 167:122-130.
139. Vinatzer U., Gollinger M., Mullauer L., Raderer M., Chott A., Streubel B. Mucosa-associated lymphoid tissue lymphoma: novel translocations including rearrangements of ODZ2, JMJD2C, and CNN3. Clin. Cancer Res. 2008, 14:6426-6431.
140. Yang Z.Q., Imoto I., Fukuda Y., Pimkhaokham A., Shimada Y., Imamura M., Sugano S., Nakamura Y., Inazawa J. Identification of a novel gene, GASC1, within an amplicon at 9p23-24 frequently detected in esophageal cancer cell lines. Cancer Res. 2000, 60:4735-4739.
141. Christensen J., Agger K., Cloos P.A., Pasini D., Rose S., Sennels L., Rappsilber J., Hansen K.H., Salcini A.E., Helin K. RBP2 belongs to a family of demethylases, specific for tri-and dimethylated lysine 4 on histone 3. Cell 2007, 128:1063-1076.
142. Klose R.J., Yan Q., Tothova Z., Yamane K., Erdjument-Bromage H., Tempst P., Gilliland D.G., Zhang Y., Kaelin W.G. The retinoblastoma binding protein RBP2 is an H3K4 demethylase. Cell 2007, 128:889-900.
143. Zeng J., Ge Z., Wang L., Li Q., Wang N., Bjorkholm M., Jia J., Xu D. The histone demethylase RBP2 Is overexpressed in gastric cancer and its inhibition triggers senescence of cancer cells. Gastroenterology 2010, 138:981-992.
144. Sharma S.V., Lee D.Y., Li B., Quinlan M.P., Takahashi F., Maheswaran S., McDermott U., Azizian N., Zou L., Fischbach M.A., Wong K.K., Brandstetter K., Wittner B., Ramaswamy S., Classon M., Settleman J. A chromatin-mediated reversible drug-tolerant state in cancer cell subpopulations. Cell 2010, 141:69-80.
145. 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. Proc. Natl Acad. Sci. USA 2007, 104:19226-19231.
146. Lu P.J., Sundquist K., Baeckstrom D., Poulsom R., Hanby A., Meier-Ewert S., Jones T., Mitchell M., Pitha-Rowe P., Freemont P., Taylor-Papadimitriou J. A novel gene (PLU-1) containing highly conserved putative DNA/chromatin binding motifs is specifically up-regulated in breast cancer. J. Biol. Chem. 1999, 274:15633-15645.
147. Barrett A., Madsen B., Copier J., Lu P.J., Cooper L., Scibetta A.G., Burchell J., Taylor-Papadimitriou J. PLU-1 nuclear protein, which is upregulated in breast cancer, shows restricted expression in normal human adult tissues: a new cancer/testis antigen?. Int. J. Cancer 2002, 101:581-588.
148. Yamane K., Tateishi K., Klose R.J., Fang J., Fabrizio L.A., Erdjument-Bromage H., Taylor-Papadimitriou J., Tempst P., Zhang Y. PLU-1 is an H3K4 demethylase involved in transcriptional repression and breast cancer cell proliferation. Mol. Cell 2007, 25:801-812.
149. Chen Y.T., Old L.J. Cancer-testis antigens: targets for cancer immunotherapy. Cancer J. Sci. Am. 1999, 5:16-17.
150. Tahiliani M., Mei P., Fang R., Leonor T., Rutenberg M., Shimizu F., Li J., Rao A., Shi Y. The histone H3K4 demethylase SMCX links REST target genes to X-linked mental retardation. Nature 2007, 447:601-605.
151. Smith J.A., White E.A., Sowa M.E., Powell M.L., Ottinger M., Harper J.W., Howley P.M. Genome-wide siRNA screen identifies SMCX, EP400, and Brd4 as E2-dependent regulators of human papillomavirus oncogene expression. Proc. Natl Acad. Sci. USA 2010, 107:3752-3757.
152. Agger K., Cloos P.A., Christensen J., Pasini D., Rose S., Rappsilber J., Issaeva I., Canaani E., Salcini A.E., Helin K. UTX and JMJD3 are histone H3K27 demethylases involved in HOX gene regulation and development. Nature 2007, 449:731-734.
153. Hong S., Cho Y.W., Yu L.R., Yu H., Veenstra T.D., Ge K. Identification of JmjC domain-containing UTX and JMJD3 as histone H3 lysine 27 demethylases. Proc. Natl Acad. Sci. USA 2007, 104:18439-18444.
154. Lan F., Bayliss P.E., Rinn J.L., Whetstine J.R., Wang J.K., Chen S., Iwase S., Alpatov R., Issaeva I., Canaani E., Roberts T.M., Chang H.Y., Shi Y. A histone H3 lysine 27 demethylase regulates animal posterior development. Nature 2007, 449:689-694.
155. Lee M.G., Villa R., Trojer P., Norman J., Yan K.P., Reinberg D., Di Croce L., Shiekhattar R. Demethylation of H3K27 regulates polycomb recruitment and H2A ubiquitination. Science 2007, 318:447-450.
156. Issaeva I., Zonis Y., Rozovskaia T., Orlovsky K., Croce C.M., Nakamura T., Mazo A., Eisenbach L., Canaani E. Knockdown of ALR (MLL2) reveals ALR target genes and leads to alterations in cell adhesion and growth. Mol. Cell. Biol. 2007, 27:1889-1903.
157. van Haaften G., Dalgliesh G.L., Davies H., Chen L., Bignell G., Greenman C., Edkins S., Hardy C., O'Meara S., Teague J., Butler A., Hinton J., Latimer C., Andrews J., Barthorpe S., Beare D., Buck G., Campbell P.J., Cole J., Forbes S., Jia M., Jones D., Kok C.Y., Leroy C., Lin M.L., McBride D.J., Maddison M., Maquire S., McLay K., Menzies A., Mironenko T., Mulderrig L., Mudie L., Pleasance E., Shepherd R., Smith R., Stebbings L., Stephens P., Tang G., Tarpey P.S., Turner R., Turrell K., Varian J., West S., Widaa S., Wray P., Collins V.P., Ichimura K., Law S., Wong J., Yuen S.T., Leung S.Y., Tonon G., DePinho R.A., Tai Y.T., Anderson K.C., Kahnoski R.J., Massie A., Khoo S.K., Teh B.T., Stratton M.R., Futreal P.A. Somatic mutations of the histone H3K27 demethylase gene UTX in human cancer. Nat. Genet. 2009, 41:521-523.
158. Dalgliesh G.L., Furge K., Greenman C., Chen L., Bignell G., Butler A., Davies H., Edkins S., Hardy C., Latimer C., Teague J., Andrews J., Barthorpe S., Beare D., Buck G., Campbell P.J., Forbes S., Jia M., Jones D., Knott H., Kok C.Y., Lau K.W., Leroy C., Lin M.L., McBride D.J., Maddison M., Maguire S., McLay K., Menzies A., Mironenko T., Mulderrig L., Mudie L., O'Meara S., Pleasance E., Rajasingham A., Shepherd R., Smith R., Stebbings L., Stephens P., Tang G., Tarpey P.S., Turrell K., Dykema K.J., Khoo S.K., Petillo D., Wondergem B., Anema J., Kahnoski R.J., Teh B.T., Stratton M.R., Futreal P.A. Systematic sequencing of renal carcinoma reveals inactivation of histone modifying genes. Nature 2010, 463:360-363.
159. Hinz S., Weikert S., Magheli A., Hoffmann M., Engers R., Miller K., Kempkensteffen C. Expression profile of the polycomb group protein enhancer of Zeste homologue 2 and its prognostic relevance in renal cell carcinoma. J. Urol. 2009, 182:2920-2925.
160. Wang J.K., Tsai M.C., Poulin G., Adler A.S., Chen S., Liu H., Shi Y., Chang H.Y. The histone demethylase UTX enables RB-dependent cell fate control. Genes Dev. 2010, 24:327-332.
161. De Santa F., Totaro M.G., Prosperini E., Notarbartolo S., Testa G., Natoli G. The histone H3 lysine-27 demethylase Jmjd3 links inflammation to inhibition of polycomb-mediated gene silencing. Cell 2007, 130:1083-1094.
162. Xiang Y., Zhu Z., Han G., Lin H., Xu L., Chen C.D. JMJD3 is a histone H3K27 demethylase. Cell Res. 2007, 17:850-857.
163. Fei T., Xia K., Li Z., Zhou B., Zhu S., Chen H., Zhang J., Chen Z., Xiao H., Han J.D., Chen Y.G. Genome-wide mapping of SMAD target genes reveals the role of BMP signaling in embryonic stem cell fate determination. Genome Res. 2010, 20:36-44.
164. Pena P.V., Davrazou F., Shi X., Walter K.L., Verkhusha V.V., Gozani O., Zhao R., Kutateladze T.G. Molecular mechanism of histone H3K4me3 recognition by plant homeodomain of ING2. Nature 2006, 442:100-103.
165. Shi X., Hong T., Walter K.L., Ewalt M., Michishita E., Hung T., Carney D., Pena P., Lan F., Kaadige M.R., Lacoste N., Cayrou C., Davrazou F., Saha A., Cairns B.R., Ayer D.E., Kutateladze T.G., Shi Y., Cote J., Chua K.F., Gozani O. ING2 PHD domain links histone H3 lysine 4 methylation to active gene repression. Nature 2006, 442:96-99.
166. Coles A.H., Jones S.N. The ING gene family in the regulation of cell growth and tumorigenesis. J. Cell. Physiol. 2009, 218:45-57.
167. Ythier D., Larrieu D., Brambilla C., Brambilla E., Pedeux R. The new tumor suppressor genes ING: genomic structure and status in cancer. Int. J. Cancer 2008, 123:1483-1490.
168. Shi X., Gozani O. The fellowships of the INGs. J. Cell. Biochem. 2005, 96:1127-1136.
169. Tokunaga E., Maehara Y., Oki E., Kitamura K., Kakeji Y., Ohno S., Sugimachi K. Diminished expression of ING1 mRNA and the correlation with p53 expression in breast cancers. Cancer Lett. 2000, 152:15-22.
170. Toyama T., Iwase H., Watson P., Muzik H., Saettler E., Magliocco A., DiFrancesco L., Forsyth P., Garkavtsev I., Kobayashi S., Riabowol K. Suppression of ING1 expression in sporadic breast cancer. Oncogene 1999, 18:5187-5193.
171. Gunduz M., Ouchida M., Fukushima K., Hanafusa H., Etani T., Nishioka S., Nishizaki K., Shimizu K. Genomic structure of the human ING1 gene and tumor-specific mutations detected in head and neck squamous cell carcinomas. Cancer Res. 2000, 60:3143-3146.
172. Shen D.H., Chan K.Y., Khoo U.S., Ngan H.Y., Xue W.C., Chiu P.M., Ip P., Cheung A.N. Epigenetic and genetic alterations of p33ING1b in ovarian cancer. Carcinogenesis 2005, 26:855-863.
173. Wang G.G., Song J., Wang Z., Dormann H.L., Casadio F., Li H., Luo J.L., Patel D.J., Allis C.D. Haematopoietic malignancies caused by dysregulation of a chromatin-binding PHD finger. Nature 2009, 459:847-851.
174. Grewal S.I., Jia S. Heterochromatin revisited. Nat. Rev. Genet. 2007, 8:35-46.
175. Jacobs S.A., Khorasanizadeh S. Structure of HP1 chromodomain bound to a lysine 9-methylated histone H3 tail. Science 2002, 295:2080-2083.
176. Williams L., Grafi G. The retinoblastoma protein - a bridge to heterochromatin. Trends Plant Sci. 2000, 5:239-240.
177. De Koning L., Savignoni A., Boumendil C., Rehman H., Asselain B., Sastre-Garau X., Almouzni G. Heterochromatin protein 1alpha: a hallmark of cell proliferation relevant to clinical oncology. EMBO Mol. Med. 2009, 1:178-191.
178. Kirschmann D.A., Lininger R.A., Gardner L.M., Seftor E.A., Odero V.A., Ainsztein A.M., Earnshaw W.C., Wallrath L.L., Hendrix M.J. Down-regulation of HP1Hsalpha expression is associated with the metastatic phenotype in breast cancer. Cancer Res. 2000, 60:3359-3363.
179. Norwood L.E., Moss T.J., Margaryan N.V., Cook S.L., Wright L., Seftor E.A., Hendrix M.J., Kirschmann D.A., Wallrath L.L. A requirement for dimerization of HP1Hsalpha in suppression of breast cancer invasion. J. Biol. Chem. 2006, 281:18668-18676.
180. Pomeroy S.L., Tamayo P., Gaasenbeek M., Sturla L.M., Angelo M., McLaughlin M.E., Kim J.Y., Goumnerova L.C., Black P.M., Lau C., Allen J.C., Zagzag D., Olson J.M., Curran T., Wetmore C., Biegel J.A., Poggio T., Mukherjee S., Rifkin R., Califano A., Stolovitzky G., Louis D.N., Mesirov J.P., Lander E.S., Golub T.R. Prediction of central nervous system embryonal tumour outcome based on gene expression. Nature 2002, 415:436-442.
181. Wasenius V.M., Hemmer S., Kettunen E., Knuutila S., Franssila K., Joensuu H. Hepatocyte growth factor receptor, matrix metalloproteinase-11, tissue inhibitor of metalloproteinase-1, and fibronectin are up-regulated in papillary thyroid carcinoma: a cDNA and tissue microarray study. Clin. Cancer Res. 2003, 9:68-75.
182. Dialynas G.K., Terjung S., Brown J.P., Aucott R.L., Baron-Luhr B., Singh P.B., Georgatos S.D. Plasticity of HP1 proteins in mammalian cells. J. Cell Sci. 2007, 120:3415-3424.
183. Dialynas G.K., Vitalini M.W., Wallrath L.L. Linking Heterochromatin Protein 1 (HP1) to cancer progression. Mutat. Res. 2008, 647:13-20.
184. Lukasova E., Koristek Z., Falk M., Kozubek S., Grigoryev S., Kozubek M., Ondrej V., Kroupova I. Methylation of histones in myeloid leukemias as a potential marker of granulocyte abnormalities. J. Leukoc. Biol. 2005, 77:100-111.
185. Popova E.Y., Claxton D.F., Lukasova E., Bird P.I., Grigoryev S.A. Epigenetic heterochromatin markers distinguish terminally differentiated leukocytes from incompletely differentiated leukemia cells in human blood. Exp. Hematol. 2006, 34:453-462.
186. Fuks F. DNA methylation and histone modifications: teaming up to silence genes. Curr. Opin. Genet. Dev. 2005, 15:490-495.
187. Wu J., Wang S.H., Potter D., Liu J.C., Smith L.T., Wu Y.Z., Huang T.H., Plass C. Diverse histone modifications on histone 3 lysine 9 and their relation to DNA methylation in specifying gene silencing. BMC Genomics 2007, 8:131.
188. Cedar H., Bergman Y. Linking DNA methylation and histone modification: patterns and paradigms. Nat. Rev. Genet. 2009, 10:295-304.
189. Hernandez-Munoz I., Taghavi P., Kuijl C., Neefjes J., van Lohuizen M. Association of BMI1 with polycomb bodies is dynamic and requires PRC2/EZH2 and the maintenance DNA methyltransferase DNMT1. Mol. Cell. Biol. 2005, 25:11047-11058.
190. Vire E., Brenner C., Deplus R., Blanchon L., Fraga M., Didelot C., Morey L., Van Eynde A., Bernard D., Vanderwinden J.M., Bollen M., Esteller M., Di Croce L., de Launoit Y., Fuks F. The Polycomb group protein EZH2 directly controls DNA methylation. Nature 2006, 439:871-874.
191. Li H., Rauch T., Chen Z.X., Szabo P.E., Riggs A.D., Pfeifer G.P. The histone methyltransferase SETDB1 and the DNA methyltransferase DNMT3A interact directly and localize to promoters silenced in cancer cells. J. Biol. Chem. 2006, 281:19489-19500.
192. Smallwood A., Esteve P.O., Pradhan S., Carey M. Functional cooperation between HP1 and DNMT1 mediates gene silencing. Genes Dev. 2007, 21:1169-1178.
193. Meng C.F., Zhu X.J., Peng G., Dai D.Q. Role of histone modifications and DNA methylation in the regulation of O6-methylguanine-DNA methyltransferase gene expression in human stomach cancer cells. Cancer Invest. 2010, 28:331-339.
194. Sakuraba K., Yasuda T., Sakata M., Kitamura Y.H., Shirahata A., Goto T., Mizukami H., Saito M., Ishibashi K., Kigawa G., Nemoto H., Sanada Y., Hibi K. Down-regulation of Tip60 gene as a potential marker for the malignancy of colorectal cancer. Anticancer Res. 2009, 29:3953-3955.
195. Gorrini C., Squatrito M., Luise C., Syed N., Perna D., Wark L., Martinato F., Sardella D., Verrecchia A., Bennett S., Confalonieri S., Cesaroni M., Marchesi F., Gasco M., Scanziani E., Capra M., Mai S., Nuciforo P., Crook T., Lough J., Amati B. Tip60 is a haplo-insufficient tumour suppressor required for an oncogene-induced DNA damage response. Nature 2007, 448:1063-1067.
196. Halkidou K., Gnanapragasam V.J., Mehta P.B., Logan I.R., Brady M.E., Cook S., Leung H.Y., Neal D.E., Robson C.N. Expression of Tip60, an androgen receptor coactivator, and its role in prostate cancer development. Oncogene 2003, 22:2466-2477.
197. ME L.L., Vidal F., Gallardo D., Diaz-Fuertes M., Rojo F., Cuatrecasas M., Lopez-Vicente L., Kondoh H., Blanco C., Carnero A., Ramon y Cajal S. New p53 related genes in human tumors: significant downregulation in colon and lung carcinomas. Oncol. Rep. 2006, 16:603-608.
198. Sun Y., Jiang X., Xu Y., Ayrapetov M.K., Moreau L.A., Whetstine J.R., Price B.D. Histone H3 methylation links DNA damage detection to activation of the tumour suppressor Tip60. Nat. Cell Biol. 2009, 11:1376-1382.
199. Spannhoff A., Hauser A.T., Heinke R., Sippl W., Jung M. The emerging therapeutic potential of histone methyltransferase and demethylase inhibitors. ChemMedChem 2009, 4:1568-1582.
200. Greiner D., Bonaldi T., Eskeland R., Roemer E., Imhof A. Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9. Nat. Chem. Biol. 2005, 1:143-145.
201. Iwasa E., Hamashima Y., Fujishiro S., Higuchi E., Ito A., Yoshida M., Sodeoka M. Total synthesis of (+)-chaetocin and its analogues: their histone methyltransferase G9a inhibitory activity. J. Am. Chem. Soc. 2010, 132:4078-4079.
202. Isham C.R., Tibodeau J.D., Jin W., Xu R., Timm M.M., Bible K.C. Chaetocin: a promising new antimyeloma agent with in vitro and in vivo activity mediated via imposition of oxidative stress. Blood 2007, 109:2579-2588.
203. Lakshmikuttyamma A., Scott S.A., DeCoteau J.F., Geyer C.R. Reexpression of epigenetically silenced AML tumor suppressor genes by SUV39H1 inhibition. Oncogene 2010, 29:576-588.
204. Tan J., Yang X., Zhuang L., Jiang X., Chen W., Lee P.L., Karuturi R.K., Tan P.B., Liu E.T., Yu Q. Pharmacologic disruption of Polycomb-repressive complex 2-mediated gene repression selectively induces apoptosis in cancer cells. Genes Dev. 2007, 21:1050-1063.
205. Fiskus W., Wang Y., Sreekumar A., Buckley K.M., Shi H., Jillella A., Ustun C., Rao R., Fernandez P., Chen J., Balusu R., Koul S., Atadja P., Marquez V.E., Bhalla K.N. Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor panobinostat against human AML cells. Blood 2009, 114:2733-2743.
206. Miranda T.B., Cortez C.C., Yoo C.B., Liang G., Abe M., Kelly T.K., Marquez V.E., Jones P.A. DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation. Mol. Cancer Ther. 2009, 8:1579-1588.
207. Kubicek S., O'Sullivan R.J., August E.M., Hickey E.R., Zhang Q., Teodoro M.L., Rea S., Mechtler K., Kowalski J.A., Homon C.A., Kelly T.A., Jenuwein T. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol. Cell 2007, 25:473-481.
208. Chang Y., Zhang X., Horton J.R., Upadhyay A.K., Spannhoff A., Liu J., Snyder J.P., Bedford M.T., Cheng X. Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Nat. Struct. Mol. Biol. 2009, 16:312-317.
209. Chang Y., Ganesh T., Horton J.R., Spannhoff A., Liu J., Sun A., Zhang X., Bedford M.T., Shinkai Y., Snyder J.P., Cheng X. Adding a Lysine Mimic in the Design of Potent Inhibitors of Histone Lysine Methyltransferases. J. Mol. Biol. 2010, 400:1-7.
210. Balasubramanian S., Eckert R.L. Green tea polyphenol and curcumin inversely regulate human involucrin promoter activity via opposing effects on CCAAT/enhancer-binding protein function. J. Biol. Chem. 2004, 279:24007-24014.
211. Balasubramanian S., Efimova T., Eckert R.L. Green tea polyphenol stimulates a Ras, MEKK1, MEK3, and p38 cascade to increase activator protein 1 factor-dependent involucrin gene expression in normal human keratinocytes. J. Biol. Chem. 2002, 277:1828-1836.
212. Balasubramanian S., Lee K., Adhikary G., Gopalakrishnan R., Rorke E.A., Eckert R.L. The Bmi-1 polycomb group gene in skin cancer: regulation of function by (-)-epigallocatechin-3-gallate. Nutr. Rev. 2008, 66(Suppl 1):S65-S68.
213. Balasubramanian S., Adhikary G., Eckert R.L. The Bmi-1 polycomb protein antagonizes the (-)-epigallocatechin-3-gallate-dependent suppression of skin cancer cell survival. Carcinogenesis 2010, 31:496-503.
214. Luo X.G., Zou J.N., Wang S.Z., Zhang T.C., Xi T. Novobiocin decreases SMYD3 expression and inhibits the migration of MDA-MB-231 human breast cancer cells. IUBMB Life 2010, 62:194-199.
215. Edmondson D.E., Binda C., Mattevi A. Structural insights into the mechanism of amine oxidation by monoamine oxidases A and B. Arch. Biochem. Biophys. 2007, 464:269-276.
216. Schmidt D.M., McCafferty D.G. trans-2-Phenylcyclopropylamine is a mechanism-based inactivator of the histone demethylase LSD1. Biochemistry 2007, 46:4408-4416.
217. Culhane J.C., Szewczuk L.M., Liu X., Da G., Marmorstein R., Cole P.A. A mechanism-based inactivator for histone demethylase LSD1. J. Am. Chem. Soc. 2006, 128:4536-4537.
218. Szewczuk L.M., Culhane J.C., Yang M., Majumdar A., Yu H., Cole P.A. Mechanistic analysis of a suicide inactivator of histone demethylase LSD1. Biochemistry 2007, 46:6892-6902.
219. Yang M., Culhane J.C., Szewczuk L.M., Gocke C.B., Brautigam C.A., Tomchick D.R., Machius M., Cole P.A., Yu H. Structural basis of histone demethylation by LSD1 revealed by suicide inactivation. Nat. Struct. Mol. Biol. 2007, 14:535-539.
220. 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. Proc. Natl Acad. Sci. USA 2007, 104:8023-8028.
221. Huang Y., Marton L.J., Woster P.M., Casero R.A. Polyamine analogues targeting epigenetic gene regulation. Essays Biochem. 2009, 46:95-110.
222. Huang Y., Stewart T.M., Wu Y., Baylin S.B., Marton L.J., Perkins B., Jones R.J., Woster P.M., Casero R.A. Novel oligoamine analogues inhibit lysine-specific demethylase 1 and induce reexpression of epigenetically silenced genes. Clin. Cancer Res. 2009, 15:7217-7228.
223. Chen Z., Zang J., Kappler J., Hong X., Crawford F., Wang Q., Lan F., Jiang C., Whetstine J., Dai S., Hansen K., Shi Y., Zhang G. Structural basis of the recognition of a methylated histone tail by JMJD2A. Proc. Natl Acad. Sci. USA 2007, 104:10818-10823.
224. Sekirnik R., Rose N.R., Thalhammer A., Seden P.T., Mecinovic J., Schofield C.J. Inhibition of the histone lysine demethylase JMJD2A by ejection of structural Zn(II). Chem. Commun. (Camb) 2009, 6376-6378.
225. Rose N.R., Woon E.C., Kingham G.L., King O.N., Mecinovic J., Clifton I.J., Ng S.S., Talib-Hardy J., Oppermann U., McDonough M.A., Schofield C.J. Selective inhibitors of the JMJD2 histone demethylases: combined nondenaturing mass spectrometric screening and crystallographic approaches. J. Med. Chem. 2010, 53:1810-1818.
226. Manuyakorn A., Paulus R., Farrell J., Dawson N.A., Tze S., Cheung-Lau G., Hines O.J., Reber H., Seligson D.B., Horvath S., Kurdistani S.K., Guha C., Dawson D.W. Cellular histone modification patterns predict prognosis and treatment response in resectable pancreatic adenocarcinoma: results from RTOG 9704. J. Clin. Oncol. 2010, 28:1358-1365.
227. Seligson D.B., Horvath S., Shi T., Yu H., Tze S., Grunstein M., Kurdistani S.K. Global histone modification patterns predict risk of prostate cancer recurrence. Nature 2005, 435:1262-1266.
228. Park Y.S., Jin M.Y., Kim Y.J., Yook J.H., Kim B.S., Jang S.J. The global histone modification pattern correlates with cancer recurrence and overall survival in gastric adenocarcinoma. Ann. Surg. Oncol. 2008, 15:1968-1976.
229. Wei Y., Xia W., Zhang Z., Liu J., Wang H., Adsay N.V., Albarracin C., Yu D., Abbruzzese J.L., Mills G.B., Bast R.C., Hortobagyi G.N., Hung M.C. Loss of trimethylation at lysine 27 of histone H3 is a predictor of poor outcome in breast, ovarian, and pancreatic cancers. Mol. Carcinog. 2008, 47:701-706.
230. Baysal B.E., Ferrell R.E., Willett-Brozick J.E., Lawrence E.C., Myssiorek D., Bosch A., van der Mey A., Taschner P.E., Rubinstein W.S., Myers E.N., Richard C.W., Cornelisse C.J., Devilee P., Devlin B. Mutations in SDHD, a mitochondrial complex II gene, in hereditary paraganglioma. Science 2000, 287:848-851.