Epi-drugs and epi-mirs: Moving beyond current cancer therapies

Current Cancer Drug Targets

Volumn 16, Issue 9, 2016, Pages 773-788

  Salarinia, Reza ^a,b   Sahebkar, Amirhossein ^a   Peyvandi, Mostafa ^a,c   Mirzaei, Hamid Reza ^d   Jaafari, Mahmoud Reza ^e   Riahi, Maryam Matbou ^a   Ebrahimnejad, Hamed ^f   Nahand, Javid Sadri ^a   Hadjati, Jamshid ^a   Asrami, Mobina Ostadi ^g   Fadaei, Sara ^h   Salehi, Rasoul ⁱ   Mirzaei, Hamed ^a  

^a MASHHAD UNIVERSITY OF MEDICAL SCIENCES   (Iran)

^b NORTH KHORASAN UNIVERSITY OF MEDICAL SCIENCES   (Iran)

^c BIRJAND UNIVERSITY OF MEDICAL SCIENCES   (Iran)

^d TEHRAN UNIVERSITY OF MEDICAL SCIENCES   (Iran)

^e MASHHAD UNIVERSITY OF MEDICAL SCIENCES   (Iran)

^f MASHHAD UNIVERSITY OF MEDICAL SCIENCES   (Iran)

^g ISLAMIC AZAD UNIVERSITY   (Iran)

^h KASHAN UNIVERSITY OF MEDICAL SCIENCES   (Iran)

ⁱ ISFAHAN UNIVERSITY OF MEDICAL SCIENCES   (Iran)

Author keywords

Cancer epigenetics; DNA methyltransferase inhibitor; Epi drugs; Epi miRs; Histone deacetylase inhibitor

Indexed keywords

AURORA B KINASE; BELINOSTAT; BET PROTEIN; DECITABINE; DNA METHYLTRANSFERASE; DNA METHYLTRANSFERASE INHIBITOR; DOT1L PROTEIN; EPIGALLOCATECHIN GALLATE; HISTONE DEACETYLASE; HISTONE DEACETYLASE INHIBITOR; HYDRALAZINE; ISOCITRATE DEHYDROGENASE 1; ISOCITRATE DEHYDROGENASE 2; MICRORNA; MICRORNA 127; MICRORNA 137; MICRORNA 224; MICRORNA 34; MICRORNA 449; MICRORNA 512; MICRORNA 9; PROCAINAMIDE; PROCAINE; PROTEIN S 100; PROTEIN SWI; TRANSCRIPTION FACTOR EZH2; TRANSCRIPTION FACTOR SNF; TRICHOSTATIN A; UNCLASSIFIED DRUG; UNINDEXED DRUG; ZEBULARINE; ANTINEOPLASTIC AGENT;

CANCER THERAPY; CPG ISLAND; DNA METHYLATION; EPIGENETICS; GENE EXPRESSION; GENE SILENCING; GENOTYPE; HISTONE MODIFICATION; HUMAN; INTRACELLULAR SIGNALING; MITOSIS; MOLECULAR PATHOLOGY; ONCOGENE; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PHENOTYPE; REVIEW; TUMOR SUPPRESSOR GENE; ANTAGONISTS AND INHIBITORS; DRUG EFFECTS; GENETIC EPIGENESIS; GENETICS; METABOLISM; NEOPLASMS;

ANTINEOPLASTIC AGENTS; DNA METHYLATION; DNA MODIFICATION METHYLASES; EPIGENESIS, GENETIC; HISTONE DEACETYLASE INHIBITORS; HUMANS; MICRORNAS; NEOPLASMS;

EID: 84995543375     PISSN: 15680096     EISSN: 18735576     Source Type: Journal    
DOI: 10.2174/1568009616666151207110143     Document Type: Review

References (248)

1. Suzuki, M. M.; Bird, A. DNA methylation landscapes: provocative insights from epigenomics. Nat. Rev. Genet., 2008, 9 (6), 465-476.
2. Dai, E.; Yu, X.; Zhang, Y.; Meng, F.; Wang, S.; Liu, X.; Liu, D.; Wang, J.; Li, X.; Jiang, W. EpimiR: a database of curated mutual regulation between miRNAs and epigenetic modifications. Database., 2014, 28; 2014: bau02.
3. Zhou, V.W.; Goren, A.; Bernstein, B.E. Charting histone modifications and the functional organization of mammalian genomes. Nat. Rev. Genet., 2011, 12 (1), 7-18.
4. Bueno, M. J.; de Castro, I. P.; de Cedron, M. G.; Santos, J.; Calin, G. A.; Cigudosa, J. C.; Croce, C. M. Fernandez-Piqueras, J.; Malumbres, M., Genetic and epigenetic silencing of microRNA-203 enhances ABL1 and BCR-ABL1 oncogene expression. Cancer cell., 2008, 13 (6), 496-506.
5. Yang, D.; Sun, Y.; Hu, L.; Zheng, H.; Ji, P.; Pecot, C. V.; Zhao, Y.; Reynolds, S.; Cheng, H.; Rupaimoole, R. Integrated analyses identify a master microRNA regulatory network for the mesenchymal subtype in serous ovarian cancer. Cancer cell., 2013, 23 (2), 186-199
6. Lujambio, A.; Calin, G. A.; Villanueva, A.; Ropero, S.; Sanchez-Cespedes, M.; Blanco, D.; Montuenga, L. M.; Rossi, S.; Nicoloso, M. S.; Faller, W. J. A microRNA DNA methylation signature for human cancer metastasis. Proc. Natl. Acad. Sci., 2008, 105 (36), 13556-13561.
7. Suzuki, H.; Takatsuka, S.; Akashi, H.; Yamamoto, E.; Nojima, M.; Maruyama, R.; Kai, M.; Yamano, H.-o.; Sasaki, Y.; Tokino, T. Genome-wide profiling of chromatin signatures reveals epigenetic regulation of MicroRNA genes in colorectal cancer. Cancer. Res., 2011, 71 (17), 5646-5658.
8. Vrba, L.; Garbe, J. C.; Stampfer, M. R.; Futscher, B. W. Epigenetic regulation of normal human mammary cell type–specific miRNAs. Genome. Res., 2011, 21 (12), 2026-2037.
9. Kitagawa, N.; Ojima, H.; Shirakihara, T.; Shimizu, H.; Kokubu, A.; Urushidate, T.; Totoki, Y.; Kosuge, T.; Miyagawa, S.; Shibata, T. Downregulation of the microRNA biogenesis components and its association with poor prognosis in hepatocellular carcinoma. Cancer. Sci., 2013, 104 (5), 543-551.
10. Kelly, T. K.; De Carvalho, D. D.; Jones, P. A. Epigenetic modifications as therapeutic targets. _Nat. Biotechnol., 2010, 28 (10), 1069-1078.
11. Saito, Y.; Jones, P. M. Epigenetic activation of tumor suppressor microRNAs in human cancer cells. Cell Cycle., 2006, 5 (19), 2220-2222.
12. Scott, G. K.; Mattie, M. D.; Berger, C. E.; Benz, S. C.; Benz, C. C., Rapid alteration of microRNA levels by histone deacetylase inhibition. Cancer Res., 2006, 66 (3), 1277-1281.
13. Wen, Y.; Grandis, J.R. Emerging drugs for head and neck cancer. Expert. Opin. Emerg. Drugs., 2015, 1-17.
14. Feinberg, A. P.; Tycko, B. The history of cancer epigenetics. Nat. Rev. Cancer., 2004, 4 (2), 143-153.
15. Horsburgh, S.; Robson-Ansley, P.; Adams, R.; Smith, C. Exercise and inflammation-related epigenetic modifications: focus on DNA methylation. Exerc. Immunol. Rev., 2015, 21, 26-41.
16. Nephew, K P.; Balch, C.; Zhang, S.; Huang, T.H., Epigenetics and ovarian cancer. Springer., 2010; pp. 131-146.
17. Liu, L.; Jin, G.; Zhou, X. Modeling the relationship of epigenetic modifications to transcription factor binding. Nucleic. Acids. Res., 2015, 43 (8), 3873-85.
18. Dhar, A. O7.4Targeting BET bromo domain and other epigenetic modifiers for treatment of cancer. Ann.Oncol., 2015, 26 (2), ii10.
19. Allfrey, V.; Faulkner, R.; Mirsky, A. Acetylation and methylation of histones and their possible role in the regulation of RNA synthesis. Proc. Natl. Acad. Sci. U.S.A., 1964, 51 (5), 786.
20. Gronbak, K.; Hother, C.; Jones, P. A. Epigenetic changes in cancer. Apmis., 2007, 115 (10), 1039-1059.
21. Feinberg, A. P.; Vogelstein, B. Hypomethylation distinguishes genes of some human cancers from their normal counterparts. Nature., 1983, 301 (5895), 89-92.
22. Gama-Sosa, M. A.; Slagel, V. A.; Trewyn, R. W.; Oxenhandler, R.; Kuo, K. C.; Gehrke, C. W.; Ehrlich, M. The 5-methylcytosine content of DNA from human tumors. Nucleic. Acids. Res., 1983, 11 (19), 6883-6894.
23. Feinberg, A. P.; Ohlsson, R.; Henikoff, S. The epigenetic progenitor origin of human cancer. Nat. Rev. Genet., 2006, 7 (1), 21-33.
24. Baylin, S. B.; Ohm, J. E. Epigenetic gene silencing in cancer–a mechanism for early oncogenic pathway addiction? Nat. Rev. Cancer., 2006, 6 (2), 107-116.
25. Vaiopoulos, A. G.; Athanasoula, K. C.; Papavassiliou, A. G. Epignetic modifications in colorectal cancer: molecular insights and therapeutic challenges. BBA-MOL. Basis. Dis., 2014, 1842 (7), 971-980.
26. Matzke, M. A.; Mosher, R. A. RNA-directed DNA methylation: an epigenetic pathway of increasing complexity. Nat. Rev. Genet., 2014, 15 (6), 394-408.
27. Sharma, A.; Heuck, C. J.; Fazzari, M. J.; Mehta, J.; Singhal, S.; Greally, J. M.; Verma, A. DNA methylation alterations in multiple myeloma as a model for epigenetic changes in cancer. Wiley. Interdiscip. Rev. Syst. Biol. Med., 2010, 2 (6), 654-669.
28. Bird, A. P. CpG-rich islands and the function of DNA methylation. Nature., 1985, 321 (6067), 209-213.
29. Li, E.; Beard, C.; Jaenisch, R. Role for DNA methylation in genomic imprinting. Nature., 1993, 366 (6453), 362-365.
30. Mirzaei H.Y F., Salehi R, Mirzaei HR. SiRNA and epigenetic aberrations in ovarian cancer. J. Can. Res. Ther., 2015.
31. Fazzari, M. J.; Greally, J. M. Epigenomics: beyond CpG islands. Nat. Rev.Genet., 2004, 5 (6), 446-455.
32. Jones, P. A.; Baylin, S. B. The epigenomics of cancer. Cell., 2007, 128 (4), 683-692.
33. Li, E.; Bestor, T. H.; Jaenisch, R. Targeted mutation of the DNA methyltransferase gene results in embryonic lethality. Cell., 1992, 69 (6), 915-926.
34. Wang, K.; Yuen, S. T.; Xu, J.; Lee, S. P.; Yan, H. H.; Shi, S. T.; Siu, H. C.; Deng, S.; Chu, K. M.; Law, S. Whole-genome sequencing and comprehensive molecular profiling identify new driver mutations in gastric cancer. Nat. Genet., 2014, 46 (6), 573-582.
35. Baylin, S. B. DNA methylation and gene silencing in cancer. Nat. Rev. Clin. Oncol., 2005, 2, S4-S11.
36. Razin, A.; Cedar, H. DNA methylation and gene expression. Microbiol. Rev., 1991, 55 (3), 451-458.
37. Melki, J. R.; Vincent, P. C.; Clark, S. J. Concurrent DNA hypermethylation of multiple genes in acute myeloid leukemia. Cancer. Res., 1999, 59 (15), 3730-3740.
38. Lee, W.-H.; Morton, R. A.; Epstein, J. I.; Brooks, J. D.; Campbell, P. A.; Bova, G. S.; Hsieh, W.-S.; Isaacs, W. B.; Nelson, W. G. Cytidine methylation of regulatory sequences near the pi-class glutathione S-transferase gene accompanies human prostatic carcinogenesis. Proc. Natl. Acad. Sci., 1994, 91 (24), 11733-11737.
39. Hinoue, T.; Weisenberger, D. J.; Lange, C. P.; Shen, H.; Byun, H.-M.; Van Den Berg, D.; Malik, S.; Pan, F.; Noushmehr, H; van Dijk, C. M. Genome-scale analysis of aberrant DNA methylation in colorectal cancer. Genome Res., 2012, 22 (2), 271-282.
40. Szyf, M.; Pakneshan, P.; Rabbani, S. A. DNA methylation and breast cancer. Biochem. Pharmacol., 2004, 68 (6), 1187-1197.
41. Catteau, A.; Morris, J. R. In BRCA1 methylation: a significant role in tumour development. Sem. Cancer Biol., 2002; 359-371.
42. Rodriguez, J.; Frigola, J.; Vendrell, E.; Risques, R.-A.; Fraga, M. F.; Morales, C.; Moreno, V.; Esteller, M.; Capella, G.; Ribas, M. Chromosomal instability correlates with genome-wide DNA demethylation in human primary colorectal cancers. Cancer Res., 2006, 66 (17), 8462-9468.
43. Jones, P. A.; Baylin, S. B. The fundamental role of epigenetic events in cancer. Nat. Rev. Genet., 2002, 3 (6), 415-428.
44. Eden, A.; Gaudet, F.; Waghmare, A.; Jaenisch, R. Chromosomal instability and tumors promoted by DNA hypomethylation. Science., 2003, 300 (5618), 455-455.
45. Howard, G.; Eiges, R.; Gaudet, F.; Jaenisch, R.; Eden, A. Activation and transposition of endogenous retroviral elements in hypomethylation induced tumors in mice. Oncogene., 2008, 27 (3), 404-408.
46. Ehrlich, M. The ICF syndrome, a DNA methyltransferase 3B deficiency and immunodeficiency disease. Clin. Immunol., 2003, 109 (1), 17-28.
47. Wilson, A. S.; Power, B. E.; Molloy, P.L. DNA hypomethylation and human diseases. BBA-REV. Cancer., 2007, 1775 (1), 138-162.
48. Rainier, S.; Johnson, L. A.; Dobry, C. J.; Ping, A. J.; Grundy, P. E.; Feinberg, A. P. Relaxation of imprinted genes in human cancer. Nature., 1993, 22, 362 (6422), 747-9.
49. Ogawa, O.; Eccles, M. R.; Szeto, J.; McNoe, L. A.; Yun, K.; Maw, M. A.; Smith, P. J.; Reeve, A. E.Relaxation of insulin-like growth factor II gene imprinting implicated in Wilms' tumour. Nature., 1993, 362 (6422), 749-751.
50. Cui, H.; Cruz-Correa, M.; Giardiello, F. M.; Hutcheon, D. F.; Kafonek, D. R.; Brandenburg, S.; Wu, Y.; He, X.; Powe, N. R.; Feinberg, A. P. Loss of IGF2 imprinting: a potential marker of colorectal cancer risk. Science., 2003, 299 (5613), 1753-1755.
51. Campbell, M. J.; Turner, B. M. Altered histone modifications in cancer. In Epigenetic Alterations in Oncogenesis, Springer: 2013; 81-107.
52. Waldmann, T.; Schneider, R. Targeting histone modifications— Epigenetics in cancer. Curr. Opin. Chem. Biol., 2013, 25 (2), 184-189.
53. Zhang, K.; Dent, S. Y. Histone modifying enzymes and cancer: going beyond histones. _J. Cell. Biochem., 2005, 96 (6), 1137-1148.
54. Santos-Rosa, H.; Caldas, C. Chromatin modifier enzymes, the histone code and cancer. Eur. J. Cancer., 2005, 41 (16), 2381-2402.
55. LaVoie, H. A. Epigenetic control of ovarian function: the emerging role of histone modifications. Mol. Cell. Endocrinol., 2005, 243 (1), 12-18.
56. Kala, R.; Peek, G. W.; Hardy, T. M.; Tollefsbol, T. O. MicroRNAs: an emerging science in cancer epigenetics. J. Clin. Bioinform., 2013, 3, 6.
57. Jimenez-Wences, H.; Peralta-Zaragoza, O.; Fernandez-Tilapa, G. Human papilloma virus, DNA methylation and microRNA expression in cervical cancer (Review). Oncol. Rep., 2014, 31 (6), 2467-2476.
58. Saito, Y.; Saito, H.; Liang, G.; Friedman, J. M. Epigenetic alterations and microRNA misexpression in cancer and autoimmune diseases: a critical review. Clin. Rev. Allergy. Immunol., 2014, 47 (2), 128-135.
59. Ferracin, M.; Lupini, L. MicroRNA Expression Profiling and Its Clinical Impact in Breast Cancer. In MicroRNAs: Key Regulators of Oncogenesis, Springer: 2014; pp. 355-367.
60. Tavallaie, R.; De Almeida, S. R.; Gooding, J. J.Toward biosensors for the detection of circulating microRNA as a cancer biomarker: an overview of the challenges and successes. Wiley. Interdiscip. Rev. Nanomed. Nanobiotechnol., 2015, 7 (4), 580-92.
61. Saito, Y.; Liang, G.; Egger, G.; Friedman, J. M.; Chuang, J. C.; Coetzee, G. A.; Jones, P. A. Specific activation of microRNA-127 with downregulation of the proto-oncogene BCL6 by chromatinmodifying drugs in human cancer cells. Cancer cell., 2006, 9 (6), 435-443.
62. Kita, Y.; Vincent, K.; Natsugoe, S.; Berindan-Neagoe, I.; Calin, G. A. Epigenetically regulated microRNAs and their prospect in cancer diagnosis. Expert. Rev. Mol. Diagn., 2014, 14 (6), 673-683.
63. Rusek, A. M.; Abba, M.; Eljaszewicz, A.; Moniuszko, M.; Niklinski, J.; Allgayer, H. MicroRNA modulators of epigenetic regulation, the tumor microenvironment and the immune system in lung cancer. Mol. Cancer., 2015, 14 (1), 34.
64. McKee, T. C.; Tricoli, J. V. Epigenetics of Prostate Cancer. In Cancer Epigenetics, Springer: 2015; pp. 217-234.
65. Baer, C.; Claus, R.; Plass, C. Genome-wide epigenetic regulation of miRNAs in cancer. Cancer. Res., 2013, 73 (2), 473-477.
66. Plongthongkum, N.; Diep, D. H.; Zhang, K. Advances in the profiling of DNA modifications: cytosine methylation and beyond. Nat. Rev. Genet., 2014, 15 (10), 647-661.
67. Hirata, H.; Hinoda, Y.; Shahryari, V.; Deng, G.; Tanaka, Y.; Tabatabai, Z.; Dahiya, R. Genistein downregulates onco-miR-1260b and upregulates sFRP1 and Smad4 via demethylation and histone modification in prostate cancer cells. Br. J. Cancer., 2014, 110 (6), 1645-1654.
68. Di Leva, G.; Garofalo, M.; Croce, C. M. MicroRNAs in cancer. Annu. Rev. Pathol., 2014, 9, 287.
69. Robertson, K. D. DNA methylation and human disease. Nat. Rev. Genet., 2005, 6 (8), 597-610.
70. Kareta, M. S.; Botello, Z. M.; Ennis, J. J.; Chou, C.; Chedin, F. Reconstitution and mechanism of the stimulation of de novo methylation by human DNMT3L. J. Biol. Chem., 2006, 281 (36), 25893-25902.
71. Yoder, J. A.; Walsh, C. P.; Bestor, T. H. Cytosine methylation and the ecology of intragenomic parasites. TIG., 1997, 13 (8), 335-340.
72. Barneda-Zahonero, B.; Parra, M. Histone deacetylases and cancer. Mol. oncol., 2012, 6 (6), 579-589
73. Falkenberg, K. J.; Johnstone, R. W. Histone deacetylases and their inhibitors in cancer, neurological diseases and imune disorders. Nat. Rev. Drug. Discov., 2015, 14 (3), 219-219.
74. Polo, S. E.; Almouzni, G. Histone metabolic pathways and chromatin assembly factors as proliferation markers. Cancer. Lett., 2005, 220 (1), 1-9.
75. Vidanes, G. M.; Bonilla, C. Y.; Toczyski, D. P. Complicated tails: histone modifications and the DNA damage response. Cell., 2005, 121 (7), 973-976.
76. Johnstone, R. W. Histone-deacetylase inhibitors: novel drugs for the treatment of cancer. Nat. Rev. Drug. Discov., 2002, 1 (4), 287-299.
77. Iizuka, M.; Smith, M. M. Functional consequences of histone modifications. Curr. Opin. Genet. Dev., 2003, 13 (2), 154-160.
78. Lin, H. Y.; Chen, C. S.; Lin, S. P.; Weng, J. R.; Chen, C. S. Targeting histone deacetylase in cancer therapy. Med. Res. Rev., 2006, 26 (4), 397-413.
79. Giannini, G.; Cabri, W.; Fattorusso, C.; Rodriquez, M. Histone deacetylase inhibitors in the treatment of cancer: overview and perspectives. Future. Med. Chem., 2012, 4 (11), 1439-1460.
80. Lubbert, M.; Jones, P. A. Epigenetic Therapy of Cancer. 2014.
81. Ali, M.; Hanif, M.; Farooqi, A. A. Epigenetic therapy for cancer. Pak. J. Pharm. Sci., 2015, 28 (3), 1023-1032.
82. Copeland, R. A.; Olhava, E. J.; Scott, M. P. Targeting epigenetic enzymes for drug discovery. Curr. Opin. Chem. Biol., 2010, 14 (4), 505-510.
83. Zheng, Y. G.; Wu, J.; Chen, Z.; Goodman, M. Chemical regulation of epigenetic modifications: opportunities for new cancer therapy. Med. Res. Rev., 2008, 28 (5), 645-687.
84. Hamm, C. A.; Costa, F. F. The impact of epigenomics on future drug design and new therapies. Drug Discov. Today., 2011, 16 (13), 626-635
85. Copeland, R. A.; Solomon, M. E.; Richon, V. M. Protein methyltransferases as a target class for drug discovery. Nat. Rev. Drug. Discov., 2009, 8 (9), 724-732.
86. Grunau, C.; Renault, E.; Rosenthal, A.; Roizes, G. MethDB—a public database for DNA methylation data. Nucleic Acids. Res., 2001, 29 (1), 270-274.
87. Barrett, T.; Troup, D. B.; Wilhite, S. E.; Ledoux, P.; Evangelista, C.; Kim, I. F.; Tomashevsky, M.; Marshall, K. A.; Phillippy, K. H.; Sherman, P. M. NCBI GEO: archive for functional genomics data sets—10 years on. Nucleic. Acids. Res., 2011, 39 (suppl 1), D1005-D1010.
88. Zhang, Y.; Lv, J.; Liu, H.; Zhu, J.; Su, J.; Wu, Q.; Qi, Y.; Wang, F.; Li, X. HHMD: the human histone modification database. Nucleic. Acids. Res., 2010, 38 (suppl 1), D149-D154.
89. Sullivan, S.; Sink, D. W.; Trout, K. L.; Makalowska, I.; Taylor, P. M.; Baxevanis, A. D.; Landsman, D. The histone database. Nucleic. Acids. Res., 2002, 30 (1), 341-342.
90. Shipra, A.; Chetan, K.; Rao, M. CREMOFAC—a database of chromatin remodeling factors. Bioinformatics., 2006, 22 (23), 2940-2944.
91. Turinsky, A. L.; Turner, B.; Borja, R. C.; Gleeson, J. A.; Heath, M.; Pu, S.; Switzer, T.; Dong, D.; Gong, Y.; On, T. DAnCER: disease-annotated chromatin epigenetics resource. Nucleic. Acids. Res., 2011, 39 (suppl 1), D889-D894.
92. He, X.; Chang, S.; Zhang, J.; Zhao, Q.; Xiang, H.; Kusonmano, K.; Yang, L.; Sun, Z. S.; Yang, H.; Wang, J. MethyCancer: the database of human DNA methylation and cancer. Nucleic. Acids. Res., 2008, 36 (suppl 1), D836-D841.
93. Ongenaert, M.; Van Neste, L.; De Meyer, T.; Menschaert, G.; Bekaert, S.; Van Criekinge, W. PubMeth: a cancer methylation database combining text-mining and expert annotation. Nucleic Acids Res., 2008, 36 (suppl 1), D842-D846.
94. Shen, J.; Wang, S.; Siegel, A. B.; Remotti, H.; Wang, Q.; Sirosh, I.; Santella, R. M. Integrative analyses of genome-wide expression of miRNAs and DNA methylation patterns in hepatocellular carcinoma to improve functional biomarker identification. Cancer Res., 2014, 74 (19 Supplement), 285-285.
95. Pinto, R.; De Summa, S.; Pilato, B.; Tommasi, S. DNA Methylation and miRNAs Regulation in Hereditary Breast Cancer: Epigenetic Changes, Players in Transcriptional and Post-Transcriptional Regulation in Hereditary Breast Cancer. Curr. Mol. Med., 2014, 14 (1), 45-57.
96. Niskakoski, A.; Kaur, S.; Staff, S.; Renkonen-Sinisalo, L.; Lassus, H.; Jarvinen, H. J.; Mecklin, J.-P.; Butzow, R.; Peltomaki, P. Epigenetic analysis of sporadic and Lynch-associated ovarian cancers reveals histology-specific patterns of DNA methylation. Epigenetics., 2014, 9 (12), 1577-1587.
97. Lapenna, S.; Giordano, A. Cell cycle kinases as therapeutic targets for cancer. Nat. Rev. Drug. Discov., 2009, 8 (7), 547-566.
98. de Carcer, G.; Perez de Castro, I.; Malumbres, M. Targeting cell cycle kinases for cancer therapy. Curr. Med. Chem., 2007, 14 (9), 969-985.
99. Bischoff, J. R.; Anderson, L.; Zhu, Y.; Mossie, K.; Ng, L.; Souza, B.; Schryver, B.; Flanagan, P.; Clairvoyant, F.; Ginther, C. A homologue of Drosophila aurora kinase is oncogenic and amplified in human colorectal cancers. EMBO. J., 1998, 17 (11), 3052-3065.
100. Lens, S. M.; Voest, E. E.; Medema, R. H. Shared and separate functions of polo-like kinases and aurora kinases in cancer. Nat. Rev. Cancer., 2010, 10 (12), 825-841.
101. Shannon, K. B.; Salmon, E. Chromosome dynamics: new light on Aurora B kinase function. _Curr. Biol., 2002, 12 (13), R458-R460.
102. Ruchaud, S.; Carmena, M.; Earnshaw, W. C. Chromosomal passengers: conducting cell division. Nat. Rev. Mol. Cell. Biol., 2007, 8 (10), 798-812.
103. Meulenbeld, H. J.; Bleuse, J. P.; Vinci, E. M.; Raymond, E.; Vitali, G.; Santoro, A.; Dogliotti, L.; Berardi, R.; Cappuzzo, F.; Tagawa, S. T. Randomized phase II study of danusertib in patients with metastatic castration_resistant prostate cancer after docetaxel failure. BJU Int., 2013, 111 (1), 44-52.
104. Lowenberg, B.; Muus, P.; Ossenkoppele, G.; Rousselot, P.; Cahn, J.-Y.; Ifrah, N.; Martinelli, G.; Amadori, S.; Berman, E.; Sonneveld, P. Phase 1/2 study to assess the safety, efficacy, and pharmacokinetics of barasertib (AZD1152) in patients with advanced acute myeloid leukemia. Blood., 2011, 118 (23), 6030-6036.
105. Traynor, A. M.; Hewitt, M.; Liu, G.; Flaherty, K. T.; Clark, J.; Freedman, S. J.; Scott, B. B.; Leighton, A. M.; Watson, P. A.; Zhao, B. Phase I dose escalation study of MK-0457, a novel Aurora kinase inhibitor, in adult patients with advanced solid tumors. Cancer Chemother. Pharmacol., 2011, 67 (2), 305-314.
106. Rubin, E.; Shapiro, G.; Stein, M.; Watson, P.; Bergstrom, D.; Xiao, A.; Clark, J.; Freedman, S.; Eder, J. A phase I clinical and pharmacokinetic (PK) trial of the aurora kinase (AK) inhibitor MK-0457 in cancer patients. J. Clin. Oncol., 2006, 24 (18S), 3009.
107. Seymour, J. F.; Kim, D. W.; Rubin, E.; Haregewoin, A.; Clark, J.; Watson, P.; Hughes, T.; Dufva, I.; Jimenez, J. L.; Mahon, F. X.; Rousselot, P.; Cortes, J.; Martinelli, G.; Papayannidis, C.; Nagler, A.; Giles, F. J. A phase 2 study of MK-0457 in patients with BCRABL T315I mutant chronic myelogenous leukemia and philadelphia chromosome-positive acute lymphoblastic leukemia. Blood. Cancer J., 2014, 4, e238.
108. Foran, J.; Ravandi, F.; O’brien, S.; Borthakur, G.; Rios, M.; Boone, P.; Worrell, J.; Mallett, K.; Squires, M.; Fazal, L. Phase I and pharmacodynamic trial of AT9283, an aurora kinase inhibitor, in patients with refractory leukemia. J. Clin. Oncol., 2008, 26 (15 Suppl), 2518.
109. Arkenau, H.-T.; Plummer, R.; Molife, L.; Olmos, D.; Yap, T.; Squires, M.; Lewis, S.; Lock, V.; Yule, M.; Lyons, J. A phase I dose escalation study of AT9283, a small molecule inhibitor of aurora kinases, in patients with advanced solid malignancies. Ann. Oncol., 2012, 23 (5), 1307-1313.
110. Robert, F.; Verschraegen, C.; Hurwitz, H.; Uronis, H.; Advani, R.; Chen, A.; Taverna, P.; Havrilla, N.; Evanchik, M.; Hawtin, R. A Phase 1 Trial of SNS-314, A Novel and Selective Pan-Aurora Kinase Inhibitor, in Advanced Solid Tumor Patients. Age., 2009, 58, 37-73.
111. Renshaw, J.; Patnaik, A.; Gordon, M.; Beeram, M.; Fischer, D.; Gianella-Borradori, A.; Lin, C.; Mendelson, D. In A phase I two arm trial of AS703569 (R763), an orally available aurora kinase inhibitor, in subjects with solid tumors: preliminary results, J. Clin. Oncol., 2007; p. 14130.
112. Mross, K.; Scheulen, M.; Frost, A.; Scharr, D.; Richly, H.; Nokay, B.; Lee, K.; Hilbert, J.; Fleischer, F.; Fietz, O. A phase I doseescalation study of BI 811283, an Aurora B inhibitor, administered every three weeks in patients with advanced solid tumors. J. Clin. Oncol., 2010, 28, 3011.
113. Adams, N. D.; Adams, J. L.; Burgess, J. L.; Chaudhari, A. M.; Copeland, R. A.; Donatelli, C. A.; Drewry, D. H.; Fisher, K. E.; Hamajima, T.; Hardwicke, M. A. Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J. Med. Chem., 2010, 53 (10), 3973-4001.
114. Schoffski, P.; Jones, S. F.; Dumez, H.; Infante, J. R.; Van Mieghem, E.; Fowst, C.; Gerletti, P.; Xu, H.; Jakubczak, J. L.; English, P. A. Phase I, open-label, multicentre, dose-escalation, pharmacokinetic and pharmacodynamic trial of the oral aurora kinase inhibitor PF-03814735 in advanced solid tumours. Eur. J. Cancer., 2011, 47 (15), 2256-2264
115. Jones, S.; Burris III H.; Dumez, H.; Infante, J.; Fowst, C.; Gerletti, P.; Xu, H.; Jakubczak, J.; Mellaerts, N.; Schoffski, P. Phase I accelerated dose-escalation, pharmacokinetic (PK) and pharmacodynamic study of PF-03814735, an oral aurora kinase inhibitor, in patients with advanced solid tumors: Preliminary results. J. Clin. Oncol., 2008, 26 (15S), a2517.
116. Kitzen, J.; de Jonge, M.; Verweij, J. Aurora kinase inhibitors. Crit. Rev. Oncol. Hematol., 2010, 73 (2), 99-110.
117. Dar, A. A.; Goff, L. W.; Majid, S.; Berlin, J.; El-Rifai, W. Aurora kinase inhibitors-rising stars in cancer therapeutics. Mol. Cancer Ther., 2010, 9 (2), 268-278.
118. Santini, V.; Kantarjian, H. M.; Issa, J.-P. Changes in DNA methylation in neoplasia: pathophysiology and therapeutic implications. Ann. Intern. Med., 2001, 134 (7), 573-586.
119. Goffin, J.; Eisenhauer, E. DNA methyltransferase inhibitors—state of the art. Ann. Oncol., 2002, 13 (11), 1699-1716.
120. Kaminskas, E.; Farrell, A.; Abraham, S.; Baird, A.; Hsieh, L.-S.; Lee, S.-L.; Leighton, J. K.; Patel, H.; Rahman, A.; Sridhara, R. Approval summary: azacitidine for treatment of myelodysplastic syndrome subtypes. Clin. cancer. res., 2005, 11 (10), 3604-3608.
121. Issa, J.-P. Decitabine. Curr. Opin. Oncol., 2003, 15 (6), 446-451.
122. Sasaki, M.; Kaneuchi, M.; Fujimoto, S.; Tanaka, Y.; Dahiya, R. Hypermethylation can selectively silence multiple promoters of steroid receptors in cancers. Mol. Cell. Endocrinol., 2003, 202 (1), 201-207.
123. Balch, C.; Huang, T. H.-M.; Brown, R.; Nephew, K. P. The epigenetics of ovarian cancer drug resistance and resensitization. Am. J. Obstet. Gynecol., 2004, 191 (5), 1552-1572.
124. Abbosh, P. H.; Montgomery, J. S.; Starkey, J. A.; Novotny, M.; Zuhowski, E. G.; Egorin, M. J.; Moseman, A. P.; Golas, A.; Brannon, K. M.; Balch, C. Dominant-negative histone H3 lysine 27 mutant derepresses silenced tumor suppressor genes and reverses the drug-resistant phenotype in cancer cells. Cancer. res., 2006, 66 (11), 5582-5591
125. Nguyen, C. T.; Weisenberger, D. J.; Velicescu, M.; Gonzales, F. A.; Lin, J. C.; Liang, G.; Jones, P. A. Histone H3-lysine 9 methylation is associated with aberrant gene silencing in cancer cells and is rapidly reversed by 5-aza-2′-deoxycytidine. Cancer. Res., 2002, 62 (22), 6456-6461.
126. Balch, C.; Yan, P.; Craft, T.; Young, S.; Skalnik, D. G.; Huang, T. H.; Nephew, K. P. Antimitogenic and chemosensitizing effects of the methylation inhibitor zebularine in ovarian cancer. Mol. Cancer Ther., 2005, 4 (10), 1505-1514.
127. Yoo, C. B.; Jeong, S.; Egger, G.; Liang, G.; Phiasivongsa, P.; Tang, C.; Redkar, S.; Jones, P. A. Delivery of 5-aza-2′-deoxycytidine to cells using oligodeoxynucleotides. Cancer. Res. 2007, 67 (13), 6400-6408.
128. Lee, W. J.; Shim, J.-Y.; Zhu, B.T. Mechanisms for the inhibition of DNA methyltransferases by tea catechins and bioflavonoids. Mol. Pharmacol., 2005, 68 (4), 1018-1030.
129. Villar-Garea, A.; Fraga, M. F.; Espada, J.; Esteller, M. Procaine is a DNA-demethylating agent with growth-inhibitory effects in human cancer cells. Cancer. Res., 2003, 63 (16), 4984-4989.
130. Segura-Pacheco, B.; Trejo-Becerril, C.; Perez-Cardenas, E.; Taja-Chayeb, L.; Mariscal, I.; Chavez, A.; Acuna, C.; Salazar, A. M.; Lizano, M.; Duenas-Gonzalez, A. Reactivation of tumor suppressor genes by the cardiovascular drugs hydralazine and procainamide and their potential use in cancer therapy. Clin. Cancer. Res., 2003, 9 (5), 1596-1603.
131. Kornblith, A. B.; Herndon, J. E.; Silverman, L. R.; Demakos, E. P.; Odchimar-Reissig, R.; Holland, J. F.; Powell, B. L.; DeCastro, C.; Ellerton, J.; Larson, R. A. Impact of azacytidine on the quality of life of patients with myelodysplastic syndrome treated in a randomized phase III trial: a Cancer and Leukemia Group B study. J. Clin. Oncol., 2002, 20 (10), 2441-2452.
132. El-Osta, A. On the use of DNA methylation inhibitors and the reversal of transcriptional silencing. Blood, 2003, 101 (4), 1656-1657.
133. Suzuki, M.; Sunaga, N.; Shames, D. S.; Toyooka, S.; Gazdar, A. F.; Minna, J. D. RNA interference-mediated knockdown of DNA methyltransferase 1 leads to promoter demethylation and gene reexpression in human lung and breast cancer cells. Cancer. Res., 2004, 64 (9), 3137-3143.
134. Ting, A. H.; Jair, K.-w.; Suzuki, H.; Yen, R.; Baylin, S. B.; Schuebel, K. E. CpG island hypermethylation is maintained in human colorectal cancer cells after RNAi-mediated depletion of DNMT1. Nature. Genet., 2004, 36 (6), 582-584.
135. Issa, J. P.; Garcia-Manero, G.; Giles, F. J.; Mannari, R.; Thomas, D.; Faderl, S.; Bayar, E.; Lyons, J.; Rosenfeld, C. S.; Cortes, J.; Kantarjian, H. M. Phase 1 study of low-dose prolonged exposure schedules of the hypomethylating agent 5-aza-2'-deoxycytidine (decitabine) in hematopoietic malignancies. Blood., 2004, 103 (5), 1635-40.
136. Kantarjian, H. M.; O'Brien, S.; Cortes, J.; Giles, F. J.; Faderl, S.; Issa, J. P.; Garcia-Manero, G.; Rios, M. B.; Shan, J.; Andreeff, M.; Keating, M.; Talpaz, M. Results of decitabine (5-aza-2'deoxycytidine) therapy in 130 patients with chronic myelogenous leukemia. Cancer., 2003, 98 (3), 522-8.
137. Aparicio, A.; Eads, C. A.; Leong, L. A.; Laird, P. W.; Newman, E. M.; Synold, T. W.; Baker, S. D.; Zhao, M.; Weber, J. S. Phase I trial of continuous infusion 5-aza-2'-deoxycytidine. Cancer Chemother. Pharmacol., 2003, 51 (3), 231-9.
138. Lin, X.; Asgari, K.; Putzi, M. J.; Gage, W. R.; Yu, X.; Cornblatt, B. S.; Kumar, A.; Piantadosi, S.; DeWeese, T.L.; De Marzo, A.M.; Nelson, W.G. Reversal of GSTP1 CpG island hypermethylation and reactivation of pi-class glutathione S-transferase (GSTP1) expression in human prostate cancer cells by treatment with procainamide. Cancer. Res., 2001, 61 (24), 8611-6.
139. Keith, B.; Xu, Y.; Grem, J. L. Measurement of the anti-cancer agent gemcitabine in human plasma by high-performance liquid chromatography. J. Chromatogr B. Analyt. Technol. Biomed. Life. Sci., 2003, 785 (1), 65-72.
140. Cheng, J. C.; Matsen, C. B.; Gonzales, F. A.; Ye, W.; Greer, S.; Marquez, V. E.; Jones, P. A.; Selker, E. U. Inhibition of DNA methylation and reactivation of silenced genes by zebularine. J. Natl. Cancer Inst., 2003, 95 (5), 399-409.
141. Cheng, J. C.; Yoo, C. B.; Weisenberger, D. J.; Chuang, J.; Wozniak, C.; Liang, G.; Marquez, V. E.; Greer, S.; Orntoft, T. F.; Thykjaer, T. Preferential response of cancer cells to zebularine. Cancer. Cell., 2004, 6 (2), 151-158.
142. Williamson, S. K.; Crowley, J. J.; Livingston, R. B.; Panella, T. J.; Goodwin, J. W. Phase II trial and cost analysis of fazarabine in advanced non-small cell carcinoma of the lung: a Southwest Oncology Group study. Invest. New. Drugs., 1995, 13 (1), 67-71.
143. Kees, U. R.; Avramis, V. I. Biochemical pharmacology and DNA methylation studies of arabinosyl 5-azacytidine and 5, 6-dihydro-5-azacytidine in two human leukemia cell lines PER-145 and PER-163. Anticancer. Drugs., 1995, 6 (2), 303-310.
144. Samuels, B. L.; Herndon, J.; Harmon, D. C.; Carey, R.; Aisner, J.; Corson, J. M.; Suzuki, Y.; Green, M. R.; Vogelzang, N. J. Dihydro _5_azacytidine and cisplatin in the treatment of malignant mesothelioma. Cancer, 1998, 82 (8), 1578-1584.
145. Flynn, J.; Fang, J.-Y.; Mikovits, J. A.; Reich, N. O. A potent cellactive allosteric inhibitor of murine DNA cytosine C5 methyltransferase. J. Biol. Chem., 2003, 278 (10), 8238-8243.
146. Fang, M. Z.; Wang, Y.; Ai, N.; Hou, Z.; Sun, Y.; Lu, H.; Welsh, W.; Yang, C. S. Tea polyphenol (−)-epigallocatechin-3-gallate inhibits DNA methyltransferase and reactivates methylation-silenced genes in cancer cell lines. Cancer. Res., 2003, 63 (22), 7563-7570.
147. Stewart, D.; Donehower, R.; Eisenhauer, E.; Wainman, N.; Shah, A.; Bonfils, C.; MacLeod, A.; Besterman, J.; Reid, G. A phase I pharmacokinetic and pharmacodynamic study of the DNA methyltransferase 1 inhibitor MG98 administered twice weekly. Ann. Oncol., 2003, 14 (5), 766-774.
148. Marks, P. A.; Rifkind, R. A.; Richon, V. M.; Breslow, R.; Miller, T.; Kelly, W. K.,\Histone deacetylases and cancer: causes and therapies. Nat. Rev. Cancer., 2001, 1 (3), 194-202.
149. Zeng, L.; Zhang, Y.; Chien, S.; Liu, X.; Shyy, J. Y.-J. The role of p53 deacetylation in p21Waf1 regulation by laminar flow. J. Biol. Chem., 2003, 278 (27), 24594-24599.
150. Blagosklonny, M. V.; Robey, R.; Sackett, D. L.; Du, L.; Traganos, F.; Darzynkiewicz, Z.; Fojo, T.; Bates, S. E. Histone deacetylase inhibitors all induce p21 but differentially cause tubulin acetylation, mitotic arrest, and cytotoxicity. Mol.Cancer. Ther., 2002, 1 (11), 937-941.
151. Takai, N.; Kawamata, N.; Gui, D.; Said, J. W.; Miyakawa, I.; Koeffler, H. P. Human ovarian carcinoma cells: histone deacetylase inhibitors exhibit antiproliferative activity and potently induce apoptosis. Cancer., 2004, 101 (12), 2760-2770.
152. Modesitt, S. C.; Sill, M.; Hoffman, J. S.; Bender, D. P. A phase II study of vorinostat in the treatment of persistent or recurrent epithelial ovarian or primary peritoneal carcinoma: a Gynecologic Oncology Group study. Gynecol. Oncol., 2008, 109 (2), 182-186.
153. Plumb, J. A.; Finn, P. W.; Williams, R. J.; Bandara, M. J.; Romero, M. R.; Watkins, C. J.; La Thangue, N. B.; Brown, R. Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101. Mol. Cancer. Ther., 2003, 2 (8), 721-728.
154. Takai, N.; Ueda, T.; Nishida, M.; Nasu, K.; Narahara, H. A novel histone deacetylase inhibitor, Scriptaid, induces growth inhibition, cell cycle arrest and apoptosis in human endometrial cancer and ovarian cancer cells. Int. J. Mol. Med., 2006, 17 (2), 323-330.
155. Arts, J.; Angibaud, P.; Marien, A.; Floren, W.; Janssens, B.; King, P.; Van Dun, J.; Janssen, L.; Geerts, T.; Tuman, R. R306465 is a novel potent inhibitor of class I histone deacetylases with broadspectrum antitumoral activity against solid and haematological malignancies. Br. J. Cancer., 2007, 97 (10), 1344-1353.
156. Duvic, M.; Vu, J. Vorinostat: a new oral histone deacetylase inhibitor approved for cutaneous T-cell lymphoma. Expert Opin. Investig. Drugs., 2007, 16 (7), 1111-20.
157. Piekarz, R.; Bates, S. A review of depsipeptide and other histone deacetylase inhibitors in clinical trials. Curr. Pharm. Des., 2004, 10 (19), 2289-2298.
158. Lane, A. A.; Chabner, B. A. Histone deacetylase inhibitors in cancer therapy. J. Clin. Oncol., 2009, 27 (32), 5459-5468.
159. Ramalingam, S. S.; Belani, C. P.; Ruel, C.; Frankel, P.; Gitlitz, B.; Koczywas, M.; Espinoza-Delgado, I.; Gandara, D. Phase II study of belinostat (PXD101), a histone deacetylase inhibitor, for second line therapy of advanced malignant pleural mesothelioma. J. Thorac. Oncol., 2009, 4 (1), 97.
160. Marks, P. A. The clinical development of histone deacetylase inhibitors as targeted anticancer drugs. Expert. Opin. Investig. Drugs., 2010, 19 (9), 1049-1066.
161. Reid, T.; Valone, F.; Lipera, W.; Irwin, D.; Paroly, W.; Natale, R.; Sreedharan, S.; Keer, H.; Lum, B.; Scappaticci, F. Phase II trial of the histone deacetylase inhibitor pivaloyloxymethyl butyrate (Pivanex, AN-9) in advanced non-small cell lung cancer. Lung Cancer., 2004, 45 (3), 381-386.
162. Glick, R. D.; Swendeman, S. L.; Coffey, D. C.; Rifkind, R. A.; Marks, P. A.; Richon, V. M.; La Quaglia, M. P. Hybrid polar histone deacetylase inhibitor induces apoptosis and CD95/CD95 ligand expression in human neuroblastoma. Cancer Res., 1999, 59 (17), 4392-4399.
163. Coffey, D. C.; Kutko, M. C.; Glick, R. D.; Butler, L. M.; Heller, G.; Rifkind, R. A.; Marks, P. A.; Richon, V. M.; La Quaglia, M. P. The histone deacetylase inhibitor, CBHA, inhibits growth of human neuroblastoma xenografts in vivo, alone and synergistically with all-trans retinoic acid. Cancer Res., 2001, 61 (9), 3591-3594.
164. Ma, X.; Ezzeldin, H. H.; Diasio, R. B. Histone Deacetylase Inhibitors. Drugs., 2009, 69 (14), 1911-1934.
165. Furlan, A.; Monzani, V.; Reznikov, L. L.; Leoni, F.; Fossati, G.; Modena, D.; Mascagni, P.; Dinarello, C. A. Pharmacokinetics, safety and inducible cytokine responses during a phase 1 trial of the oral histone deacetylase inhibitor ITF2357 (givinostat). Mol. Med., 2011, 17 (5-6), 353.
166. Venugopal, B.; Baird, R.; Kristeleit, R. S.; Plummer, R.; Cowan, R.; Stewart, A.; Fourneau, N.; Hellemans, P.; Elsayed, Y.; McClue, S. A phase I study of quisinostat (JNJ-26481585), an oral hydroxamate histone deacetylase inhibitor with evidence of target modulation and antitumor activity, in patients with advanced solid tumors. Clin. Cancer. Res., 2013, 19 (15), 4262-4272.
167. Schreml, J.; Riessland, M.; Paterno, M.; Garbes, L.; Rosbach, K.; Ackermann, B.; Kramer, J.; Somers, E.; Parson, S. H.; Heller, R. Severe SMA mice show organ impairment that cannot be rescued by therapy with the HDACi JNJ-26481585. Eur. J. Human. Genet., 2012, 21 (6), 643-652.
168. Tong, W.-G.; Wei, Y.; Stevenson, W.; Kuang, S.-Q.; Fang, Z.; Zhang, M.; Arts, J.; Garcia-Manero, G. Preclinical antileukemia activity of JNJ-26481585, a potent second-generation histone deacetylase inhibitor. Leuk. Res., 2010, 34 (2), 221-228.
169. Banerji, U.; van Doorn, L.; Papadatos-Pastos, D.; Kristeleit, R.; Debnam, P.; Tall, M.; Stewart, A.; Raynaud, F.; Garrett, M. D.; Toal, M. A phase I pharmacokinetic and pharmacodynamic study of CHR-3996, an oral class I selective histone deacetylase inhibitor in refractory solid tumors. Clin. Cancer. Res., 2012, 18 (9), 2687-2694.
170. Moffat, D.; Patel, S.; Day, F.; Belfield, A.; Donald, A.; Rowlands, M.; Wibawa, J.; Brotherton, D.; Stimson, L.; Clark, V. Discovery of 2-(6-{((6-Fluoroquinolin-2-yl) methyl) amino} bicyclo (3.1. 0) hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a Class I Selective Orally Active Histone Deacetylase Inhibitor. J. Med. Chem., 2010, 53 (24), 8663-8678.
171. Atadja, P.; Gao, L.; Kwon, P.; Trogani, N.; Walker, H.; Hsu, M.; Yeleswarapu, L.; Chandramouli, N.; Perez, L.; Versace, R. Selective growth inhibition of tumor cells by a novel histone deacetylase inhibitor, NVP-LAQ824. Cancer. Res., 2004, 64 (2), 689-695.
172. Xu, W.; Parmigiani, R.; Marks, P. Histone deacetylase inhibitors: molecular mechanisms of action. Oncogene., 2007, 26 (37), 5541-5552.
173. Prince, H. M.; Bishton, M. J.; Harrison, S. J. Clinical studies of histone deacetylase inhibitors. Clin. Cancer. Res., 2009, 15 (12), 3958-3969.
174. Tumber, A.; Collins, L. S.; Petersen, K. D.; Thougaard, A.; Christiansen, S. J.; Dejligbjerg, M.; Jensen, P. B.; Sehested, M.; Ritchie, J. W. The histone deacetylase inhibitor PXD101 synergises with 5-fluorouracil to inhibit colon cancer cell growth in vitro and in vivo. Cancer. Chemother. Pharmacol., 2007, 60 (2), 275-283.
175. Novotny-Diermayr, V.; Sangthongpitag, K.; Hu, C. Y.; Wu, X.; Sausgruber, N.; Yeo, P.; Greicius, G.; Pettersson, S.; Liang, A. L.; Loh, Y. K. SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer. Mol. Cancer. Ther., 2010, 9 (3), 642-652.
176. Razak, A.; Hotte, S.; Siu, L.; Chen, E.; Hirte, H.; Powers, J.; Walsh, W.; Stayner, L.; Laughlin, A.; Novotny-Diermayr, V. Phase I clinical, pharmacokinetic and pharmacodynamic study of SB939, an oral histone deacetylase (HDAC) inhibitor, in patients with advanced solid tumours. Br. J. cancer., 2011, 104 (5), 756-762.
177. Liu, T.; Kuljaca, S.; Tee, A.; Marshall, G. M. Histone deacetylase inhibitors: multifunctional anticancer agents. Cancer. Treat. Rev., 2006, 32 (3), 157-165.
178. Marks, P. A.; Richon, V. M.; Rifkind, R. A. Histone deacetylase inhibitors: inducers of differentiation or apoptosis of transformed cells. J. Natl. Cancer Inst., 2000, 92 (15), 1210-1216.
179. Drummond, D. C.; Noble, C. O.; Kirpotin, D. B.; Guo, Z.; Scott, G. K.; Benz, C. C. Clinical development of histone deacetylase inhibitors as anticancer agents*. Annu. Rev. Pharmacol. Toxicol., 2005, 45, 495-528.
180. Komatsu, Y.; Tomizaki, K.-y.; Tsukamoto, M.; Kato, T.; Nishino, N.; Sato, S.; Yamori, T.; Tsuruo, T.; Furumai, R.; Yoshida, M. Cyclic hydroxamic-acid-containing peptide 31, a potent synthetic histone deacetylase inhibitor with antitumor activity. Cancer. Res., 2001, 61 (11), 4459-4466.
181. Monneret, C. Histone deacetylase inhibitors. Eur. J. Med. Chem., 2005, 40 (1), 1-13.
182. Khan, S.; Maududi, T.; Barton, K.; Ayers, J.; Alkan, S. Analysis of histone deacetylase inhibitor, depsipeptide (FR901228), effect on multiple myeloma. _Br. J. Haematol., 2004, 125 (2), 156-161.
183. Butler, L. M.; Webb, Y.; Agus, D. B.; Higgins, B.; Tolentino, T. R.; Kutko, M. C.; LaQuaglia, M. P.; Drobnjak, M.; Cordon-Cardo, C.; Scher, H.I. Inhibition of transformed cell growth and induction of cellular differentiation by pyroxamide, an inhibitor of histone deacetylase. Clin. Cancer. Res., 2001, 7 (4), 962-970.
184. Cameron, E. E.; Bachman, K. E.; Myohanen, S.; Herman, J.G.; Baylin, S.B. Synergy of demethylation and histone deacetylase inhibition in the re-expression of genes silenced in cancer. Nat. Genet., 1999, 21 (1), 103-107.
185. Minucci, S.; Pelicci, P. G. Histone deacetylase inhibitors and the promise of epigenetic (and more) treatments for cancer. Nat. Rev. Cancer., 2006, 6 (1), 38-51.
186. Zhang, X. D.; Gillespie, S. K.; Borrow, J. M.; Hersey, P. The histone deacetylase inhibitor suberic bishydroxamate regulates the expression of multiple apoptotic mediators and induces mitochondriadependent apoptosis of melanoma cells. Mol. Cancer. Ther., 2004, 3 (4), 425-435.
187. Furumai, R.; Komatsu, Y.; Nishino, N.; Khochbin, S.; Yoshida, M.; Horinouchi, S. Potent histone deacetylase inhibitors built from trichostatin A and cyclic tetrapeptide antibiotics including trapoxin. Proc. Natl. Acad. Sci., 2001, 98 (1), 87-92.
188. Gurvich, N.; Tsygankova, O. M.; Meinkoth, J. L.; Klein, P. S. Histone deacetylase is a target of valproic acid-mediated cellular differentiation. Cancer. Res., 2004, 64 (3), 1079-1086.
189. Azmi, A. S.; Beck, F. W.; Bao, B.; Mohammad, R. M.; Sarkar, F. H. Aberrant epigenetic grooming of miRNAs in pancreatic cancer: a systems biology perspective. Epigenomics., 2011, 3 (6), 747-59.
190. Cortez, C. C.; Jones, P. A. Chromatin, cancer and drug therapies. Mutat. Res. Fund. Mol. Mech. Mut., 2008, 647 (1), 44-51.
191. Wang, Y.; Toh, H. C.; Chow, P.; Chung, A. Y.; Meyers, D. J.; Cole, P. A.; Ooi, L. L.; Lee, C. G. MicroRNA-224 is up-regulated in hepatocellular carcinoma through epigenetic mechanisms. FASEB. J., 2012, 26 (7), 3032-3041.
192. Yang, X.; Feng, M.; Jiang, X.; Wu, Z.; Li, Z.; Aau, M.; Yu, Q. miR-449a and miR-449b are direct transcriptional targets of E2F1 and negatively regulate pRb–E2F1 activity through a feedback loop by targeting CDK6 and CDC25A. Genes. Dev., 2009, 23 (20), 2388-2393.
193. Liao, W. T.; Li, T. T.; Wang, Z. G.; Wang, S. Y.; He, M. R.; Ye, Y. P.; Qi, L.; Cui, Y. M.; Wu, P.; Jiao, H. L.; Zhang, C.; Xie, Y. J.; Wang, J. X.; Ding, Y. Q. microRNA-224 promotes cell proliferation and tumor growth in human colorectal cancer by repressing PHLPP1 and PHLPP2. Clin. Cancer. Res., 2013, 19 (17), 4662-72.
194. Wang, Y.; Toh, H. C.; Chow, P.; Chung, A. Y.; Meyers, D. J.; Cole, P. A.; Ooi, L. L.; Lee, C. G. MicroRNA-224 is up-regulated in hepatocellular carcinoma through epigenetic mechanisms. FASEB. J., 2012, 26 (7), 3032-41.
195. Robles, A. I.; Okayama, H.; Kumar, S. A.; Franklin, Z.; Bowman, E. D.; Edelman, D.; Stevenson, H.; Petersen, D.; Mathe, E.; Kanai, Y. Epigenetic regulation of microRNAs in early stage lung adenocarcinoma. Cancer. Res., 2013, 73 (19), A47-A47.
196. Gao, W.; Gu, Y.; Li, Z.; Cai, H.; Peng, Q.; Tu, M.; Kondo, Y.; Shinjo, K.; Zhu, Y.; Zhang, J.; Sekido, Y.; Han, B.; Qian, Z.; Miao, Y. miR-615-5p is epigenetically inactivated and functions as a tumor suppressor in pancreatic ductal adenocarcinoma. Oncogene, 2015, 34 (13), 1629-40.
197. Hu, H.; Li, S.; Cui, X.; Lv, X.; Jiao, Y.; Yu, F.; Yao, H.; Song, E.; Chen, Y.; Wang, M. The overexpression of hypomethylated miR-663 induces chemotherapy resistance in human breast cancer cells by targeting heparin sulfate proteoglycan 2 (HSPG2). J. Biol. Chem., 2013, 288 (16), 10973-10985.
198. Yang, Y.; Wang, L. L.; Wang, H. X.; Guo, Z. K.; Gao, X. F.; Cen, J.; Li, Y. H.; Dou, L. P.; Yu, L. The epigenetically-regulated miR-663 targets H-ras in K-562 cells. FEBS. J., 2013, 280 (20), 5109-17.
199. Liu, S. Q.; Jiang, S.; Li, C.; Zhang, B.; Li, Q. J. miR-17-92 cluster targets phosphatase and tensin homology and Ikaros Family Zinc Finger 4 to promote TH17-mediated inflammation. J. Biol. Chem., 2014, 289 (18), 12446-56.
200. Humphreys, K. J.; Cobiac, L.; Le Leu, R. K.; Van der Hoek, M. B.; Michael, M. Z. Histone deacetylase inhibition in colorectal cancer cells reveals competing roles for members of the oncogenic miR-17-92 cluster. Mol. Carcinog., 2013, 52 (6), 459-74.
201. Lee, K.-H.; Lotterman, C.; Karikari, C.; Omura, N.; Feldmann, G.; Habbe, N.; Goggins, M. G.; Mendell, J. T.; Maitra, A. Epigenetic silencing of MicroRNA miR-107 regulates cyclin-dependent kinase 6 expression in pancreatic cancer. Pancreatology., 2009, 9 (3), 293-301.
202. Li, C.-L.; Nie, H.; Wang, M.; Su, L.-P.; Li, J.-F.; Yu, Y.-Y.; Yan, M.; Qu, Q.-L.; Zhu, Z.-G.; Liu, B.-Y. microRNA-155 is downregulated in gastric cancer cells and involved in cell metastasis. Oncol. Rep., 2012, 27 (6), 1960-1966.
203. Chang, S.; Wang, R. H.; Akagi, K.; Kim, K. A.; Martin, B. K.; Cavallone, L.; Haines, D. C.; Basik, M.; Mai, P.; Poggi, E.; Isaacs, C.; Looi, L. M.; Mun, K. S.; Greene, M. H.; Byers, S. W.; Teo, S. H.; Deng, C. X.; Sharan, S. K. Tumor suppressor BRCA1 epigenetically controls oncogenic microRNA-155. Nat. Med., 2011, 17 (10), 1275-82.
204. Li, A.; Omura, N.; Hong, S.-M.; Vincent, A.; Walter, K.; Griffith, M.; Borges, M.; Goggins, M. Pancreatic cancers epigenetically silence SIP1 and hypomethylate and overexpress miR-200a/200b in association with elevated circulating miR-200a and miR-200b levels. Cancer. Res., 2010, 70 (13), 5226-5237.
205. Kurashige, J.; Mima, K.; Sawada, G.; Takahashi, Y.; Eguchi, H.; Sugimachi, K.; Mori, M.; Yanagihara, K.; Yashiro, M.; Hirakawa, K.; Baba, H.; Mimori, K. Epigenetic modulation and repression of miR-200b by cancer-associated fibroblasts contribute to cancer invasion and peritoneal dissemination in gastric cancer. Carcinogenesis., 2015, 36 (1), 133-41.
206. Wagner, S.; Ngezahayo, A.; Murua Escobar, H.; Nolte, I. Role of miRNA let-7 and its major targets in prostate cancer. BioMed. Res. Int., 2014, 2014, 376326.
207. Wong, T. S.; Man, O. Y.; Tsang, C. M.; Tsao, S. W.; Tsang, R. K.; Chan, J. Y.; Ho, W. K.; Wei, W. I.; To, V. S. MicroRNA let-7 suppresses nasopharyngeal carcinoma cells proliferation through downregulating c-Myc expression. J. Cancer. Res. Clin. Oncol., 2011, 137 (3), 415-22.
208. Cai, J.; Fang, L.; Huang, Y.; Li, R.; Yuan, J.; Yang, Y.; Zhu, X.; Chen, B.; Wu, J.; Li, M. miR-205 targets PTEN and PHLPP2 to augment AKT signaling and drive malignant phenotypes in nonsmall cell lung cancer. Cancer. Res., 2013, 73 (17), 5402-15.
209. Bhatnagar, N.; Li, X.; Padi, S. K.; Zhang, Q.; Tang, M S.; Guo, B. Downregulation of miR-205 and miR-31 confers resistance to chemotherapy-induced apoptosis in prostate cancer cells. Cell. Death. Dis., 2010, 1, e105.
210. Dohi, O.; Yasui, K.; Gen, Y.; Takada, H.; Endo, M.; Tsuji, K.; Konishi, C.; Yamada, N.; Mitsuyoshi, H.; Yagi, N.; Naito, Y.; Tanaka, S.; Arii, S.; Yoshikawa, T. Epigenetic silencing of miR-335 and its host gene MEST in hepatocellular carcinoma. Int. J. Oncol., 2013, 42 (2), 411-8.
211. Xu, Q.; Liu, L. Z.; Qian, X.; Chen, Q.; Jiang, Y.; Li, D.; Lai, L.; Jiang, B. H. MiR-145 directly targets p70S6K1 in cancer cells to inhibit tumor growth and angiogenesis. Nucleic. Acids. Res., 2012, 40 (2), 761-74.
212. Zaman, M. S.; Chen, Y.; Deng, G.; Shahryari, V.; Suh, S. O.; Saini, S.; Majid, S.; Liu, J.; Khatri, G.; Tanaka, Y.; Dahiya, R. The functional significance of microRNA-145 in prostate cancer. Br. J. Cancer., 2010, 103 (2), 256-64.
213. Bou Kheir, T.; Futoma-Kazmierczak, E.; Jacobsen, A.; Krogh, A.; Bardram, L.; Hother, C.; Gronbaek, K.; Federspiel, B.; Lund, A. H.; Friis-Hansen, L. miR-449 inhibits cell proliferation and is down-regulated in gastric cancer. Mol. Cancer., 2011, 10, 29.
214. Zhou, Y.; Feng, X.; Liu, Y. L.; Ye, S. C.; Wang, H.; Tan, W. K.; Tian, T.; Qiu, Y. M.; Luo, H. S. Down-regulation of miR-126 is associated with colorectal cancer cells proliferation, migration and invasion by targeting IRS-1 via the AKT and ERK1/2 signaling pathways. PlosOne., 2013, 8 (11), e81203.
215. Lodygin, D.; Tarasov, V.; Epanchintsev, A.; Berking, C.; Knyazeva, T.; Korner, H.; Knyazev, P.; Diebold, J.; Hermeking, H. Inactivation of miR-34a by aberrant CpG methylation in multiple types of cancer. Cell Cycle., 2008, 7 (16), 2591-2600.
216. Asangani, I. A.; Harms, P. W.; Dodson, L.; Pandhi, M.; Kunju, L. P.; Maher, C. A.; Fullen, D. R.; Johnson, T. M.; Giordano, T. J.; Palanisamy, N. Genetic and epigenetic loss of microRNA-31 leads to feed-forward expression of EZH2 in melanoma. Oncotarget., 2012, 3 (9), 1011.
217. Alpini, G.; Glaser, S. S.; Zhang, J.-P.; Francis, H.; Han, Y.; Gong, J.; Stokes, A.; Francis, T.; Hughart, N.; Hubble, L. Regulation of placenta growth factor by microRNA-125b in hepatocellular cancer. J. Hepatol., 2011, 55 (6), 1339-1345.
218. Wotschofsky, Z.; Liep, J.; Meyer, H.-A.; Jung, M.; Wagner, I.; Disch, A. C.; Schaser, K. D.; Melcher, I.; Kilic, E.; Busch, J. Identification of metastamirs as metastasis-associated microRNAs in clear cell renal cell carcinomas. Int. J. Biol. Sci., 2012, 8 (10), 1363.
219. Zhang, X.; Zhao, X.; Fiskus, W.; Lin, J.; Lwin, T.; Rao, R.; Zhang, Y.; Chan, J. C.; Fu, K.; Marquez, V. E. Coordinated silencing of MYC-mediated miR-29 by HDAC3 and EZH2 as a therapeutic target of histone modification in aggressive B-Cell lymphomas. Cancer cell., 2012, 22 (4), 506-523.
220. Liu, S.; Wu, L.-C.; Pang, J.; Santhanam, R.; Schwind, S.; Wu, Y.-Z.; Hickey, C. J.; Yu, J.; Becker, H.; Maharry, K. Sp1/NFκB/HDAC/miR-29b regulatory network in KIT-driven myeloid leukemia. Cancer. Cell., 2010, 17 (4), 333-347.
221. Sampath, D.; Liu, C.; Vasan, K.; Sulda, M.; Puduvalli, V. K.; Wierda, W. G.; Keating, M. J. Histone deacetylases mediate the silencing of miR-15a, miR-16, and miR-29b in chronic lymphocytic leukemia. Blood., 2012, 119 (5), 1162-1172.
222. Hulf, T.; Sibbritt, T.; Wiklund, E. D.; Bert, S.; Strbenac, D.; Statham, A. L.; Robinson, M. D.; Clark, S. J. Discovery pipeline for epigenetically deregulated miRNAs in cancer: integration of primary miRNA transcription. BMC. Genomics., 2011, 12 (1), 54.
223. Chang, K. W.; Chu, T. H.; Gong, N. R.; Chiang, W. F.; Yang, C. C.; Liu, C. J.; Wu, C. H.; Lin, S. C. miR_370 modulates insulin receptor substrate_1 expression and inhibits the tumor phenotypes of oral carcinoma. Oral. Dis., 2013, 19 (6), 611-619.
224. Formosa, A.; Lena, A. M.; Markert, E. K.; Cortelli, S.; Miano, R.; Mauriello, A.; Croce, N.; Vandesompele, J.; Mestdagh, P.; Finazzi-Agro, E.; Levine, A. J.; Melino, G.; Bernardini, S.; Candi, E. DNA methylation silences miR-132 in prostate cancer. Oncogene., 2013, 32 (1), 127-34.
225. Chen, Y.; Gao, W.; Luo, J.; Tian, R.; Sun, H.; Zou, S. Methyl-CpG binding protein MBD2 is implicated in methylation-mediated suppression of miR-373 in hilar cholangiocarcinoma. Oncol. Rep., 2011, 25 (2), 443-51.
226. Rauhala, H. E.; Jalava, S. E.; Isotalo, J.; Bracken, H.; Lehmusvaara, S.; Tammela, T. L.; Oja, H.; Visakorpi, T. miR-193b is an epigenetically regulated putative tumor suppressor in prostate cancer. Int. J. Cancer., 2010, 127 (6), 1363-72.
227. Dohi, O.; Yasui, K.; Gen, Y.; Takada, H.; Endo, M.; Tsuji, K.; Konishi, C.; Yamada, N.; Mitsuyoshi, H.; Yagi, N. Epigenetic silencing of miR-335 and its host gene MEST in hepatocellular carcinoma. Int. J. Oncol., 2013, 42 (2), 411-418.
228. Cao, Q.; Mani, R.-S.; Ateeq, B.; Dhanasekaran, S.M.; Asangani, I.A.; Prensner, J. R.; Kim, J. H.; Brenner, J. C.; Jing, X.; Cao, X. Coordinated regulation of polycomb group complexes through microRNAs in cancer. Cancer. Cell., 2011, 20 (2), 187-199.
229. Datta, J.; Kutay, H.; Nasser, M. W.; Nuovo, G. J.; Wang, B.; Majumder, S.; Liu, C.-G.; Volinia, S.; Croce, C. M.; Schmittgen, T. D. Methylation mediated silencing of MicroRNA-1 gene and its role in hepatocellular carcinogenesis. Cancer. Res., 2008, 68 (13), 5049-5058.
230. Balaguer, F.; Link, A.; Lozano, J. J.; Cuatrecasas, M.; Nagasaka, T.; Boland, C. R.; Goel, A. Epigenetic silencing of miR-137 is an early event in colorectal carcinogenesis. Cancer. Res., 2010, 70 (16), 6609-6618.
231. Zhu, X.; Li, Y.; Shen, H.; Li, H.; Long, L.; Hui, L.; Xu, W. miR-137 inhibits the proliferation of lung cancer cells by targeting Cdc42 and Cdk6. FEBS. lett., 2013, 587 (1), 73-81.
232. Suzuki, H.; Maruyama, R.; Yamamoto, E.; Kai, M. DNA methylation and microRNA dysregulation in cancer. Mol. Oncol., 2012, 6 (6), 567-578.
233. Harel, S. A.; Ben-Moshe, N. B.; Aylon, Y.; Bublik, D.; Moskovits, N.; Toperoff, G.; Azaiza, D.; Biagoni, F.; Fuchs, G.; Wilder, S. Reactivation of epigenetically silenced miR-512 and miR-373 sensitizes lung cancer cells to cisplatin and restricts tumor growth. Cell Death Differ., 2015, 22 (8), 1328-40.
234. Adi Harel, S.; Bossel Ben-Moshe, N.; Aylon, Y.; Bublik, D. R.; Moskovits, N.; Toperoff, G.; Azaiza, D.; Biagoni, F.; Fuchs, G.; Wilder, S.; Hellman, A.; Blandino, G.; Domany, E.; Oren, M. Reactivation of epigenetically silenced miR-512 and miR-373 sensitizes lung cancer cells to cisplatin and restricts tumor growth. Cell Death Differ., 2015, 22 (8), 1328-40.
235. Campbell, R.M.; Tummino, P. J. Cancer epigenetics drug discovery and development: the challenge of hitting the mark. _J. Clin. Invest., 2014, 124 (124 (1)), 64-69.
236. Diaz, E.; Machutta, C. A.; Chen, S.; Jiang, Y.; Nixon, C.; Hofmann, G.; Key, D.; Sweitzer, S.; Patel, M.; Wu, Z. Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens. _ J. Biomol. Scre., 2012, 17 (10), 1279-1292.
237. Seton-Rogers, S. Epigenetics: Place your BETs. Nat. Rev. Cancer., 2015, 15 (11), 638.
238. Okosun, J.; Packham, G.; Fitzgibbon, J. Investigational epigenetically targeted drugs in early phase trials for the treatment of haematological malignancies. Expert. Opin. Investig. Drugs., 2014, 23 (10), 1321-1332.
239. Sato, T.; Cesaroni, M.; Jelinek, J.; Issa, J.-P. Combined targeting of DNA and histone methylation improves the efficacy and specificity of epigenetic therapy. Cancer. Res., 2015, 75 (15), 3521-3521.
240. van Groen, B.; Brook, P.; Adcock, I.; Durham, A. Late-breaking abstract: Epigenetic inhibition of proliferation and inflammation in airway epithelium._Eur. Respir. J., 2014, 44 (Suppl 58), 2911.
241. Feliciano, P. Inhibitors of mutant IDH1 and IDH2. _Nat. Genet., 2013, 45 (5), 477-477.
242. Valente, S.; Rodriguez, V.; Mercurio, C.; Vianello, P.; Saponara, B.; Cirilli, R.; Ciossani, G.; Labella, D.; Marrocco, B.; Ruoppolo, G. Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies. ACS Med. Chem. Lett., 2014, 6 (2), 173-177.
243. Maes, T.; Carceller, E.; Salas, J.; Ortega, A.; Buesa, C. Advances in the development of histone lysine demethylase inhibitors. Curr. Opin. Pharmacol., 2015, 23, 52-60.
244. Feng, C.; Sun, Y.; Ding, G.; Wu, Z.; Jiang, H.; Wang, L.; Ding, Q.; Wen, H. PI3Kβ Inhibitor TGX221 Selectively Inhibits Renal Cell Carcinoma Cells with Both VHL and SETD2 mutations and Links Multiple Pathways. Sci. Rep., 2015, 8 (5), 9465.
245. di Luccio, E. Inhibition of Nuclear Receptor Binding SET Domain 2/Multiple Myeloma SET Domain by LEM-06 Implication for Epigenetic Cancer Therapies. J. Cancer. Prev., 2015, 20 (2), 113.
246. Long, J.; Li, B.; Rodriguez-Blanco, J.; Pastori, C.; Volmar, C.-H.; Wahlestedt, C.; Capobianco, A.; Bai, F.; Pei, X.-H.; Ayad, N. G. The BET Bromodomain Inhibitor I-BET151 Acts Downstream of Smoothened Protein to Abrogate the Growth of Hedgehog Proteindriven Cancers. J. Biol. Chem., 2014, 289 (51), 35494-35502.
247. Vangamudi, B.; Paul, T. A.; Shah, P. K.; Kost-Alimova, M.; Nottebaum, L.; Shi, X.; Zhan, Y.; Leo, E.; Mahadeshwar, H. S.; Protopopov, A. The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies. Cancer. Res., 2015, 75 (18), 3865-3878.
248. Qiu Wang, J.; Juey Wu, K. Epigenetic Regulation of Epithelial-Mesenchymal Transition by Hypoxia in Cancer: Targets and Therapy. Curr. Pharm. Des., 2015, 21 (10), 1272-1278.