Exploiting epigenetic vulnerabilities for cancer therapeutics

Trends in Pharmacological Sciences

Volumn 35, Issue 3, 2014, Pages 136-145

  Mair, Barbara ^a   Kubicek, Stefan ^a   Nijman, Sebastian M B ^a  

^a ERICH SCHMID INSTITUTE OF MATERIALS SCIENCE   (Austria)

Author keywords

chromatin modifying enzymes; drugs; non oncogene addiction; synthetic lethality; therapeutics

Indexed keywords

5 AZA 2' DEOXYCYTIDINE; AZACITIDINE; DNA METHYLTRANSFERASE; EPZ 5676; EPZ 7438; GSK 525762; HISTONE DEACETYLASE; HYDROLASE INHIBITOR; METHIONINE; METHYLTRANSFERASE; METHYLTRANSFERASE INHIBITOR; MIXED LINEAGE LEUKEMIA PROTEIN; ORY 1001; OTX 015; OXYGENASE INHIBITOR; PROTEIN DOT1L; ROMIDEPSIN; RVX 208; TRANYLCYPROMINE; UNCLASSIFIED DRUG; VORINOSTAT;

ACUTE GRANULOCYTIC LEUKEMIA; CANCER SUSCEPTIBILITY; CANCER THERAPY; CARCINOMA; CARDIOVASCULAR DISEASE; CHROMATIN; CUTANEOUS T CELL LYMPHOMA; DEPRESSION; DNA METHYLATION; DRUG MECHANISM; EPIGENETICS; GENE INTERACTION; GENE MUTATION; HEMATOLOGIC MALIGNANCY; HUMAN; LEUKEMIA; MYELODYSPLASTIC SYNDROME; NONHODGKIN LYMPHOMA; NONHUMAN; ONCOGENE; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; REVIEW;

CHROMATIN-MODIFYING ENZYMES; DRUGS; NON-ONCOGENE ADDICTION; SYNTHETIC LETHALITY; THERAPEUTICS;

EPIGENOMICS; GENETIC THERAPY; HUMANS; NEOPLASMS;

EID: 84896707316     PISSN: 01656147     EISSN: 18733735     Source Type: Journal    
DOI: 10.1016/j.tips.2014.01.001     Document Type: Review

References (76)

1. S.B. Baylin, and P.A. Jones A decade of exploring the cancer epigenome - biological and translational implications Nat. Rev. Cancer 11 2011 726 734
2. R. Brough et al. Searching for synthetic lethality in cancer Curr. Opin. Genet. Dev. 21 2011 34 41
3. D.A. Chan, and A.J. Giaccia Harnessing synthetic lethal interactions in anticancer drug discovery Nat. Rev. Drug Discov. 10 2011 351 364
4. M.A. Dawson, and T. Kouzarides Cancer epigenetics: from mechanism to therapy Cell 150 2012 12 27
5. K. Helin, and D. Dhanak Chromatin proteins and modifications as drug targets Nature 502 2013 480 488
6. W.G. Kaelin Jr The concept of synthetic lethality in the context of anticancer therapy Nat. Rev. Cancer 5 2005 689 698
7. M. Rodriguez-Paredes, and M. Esteller Cancer epigenetics reaches mainstream oncology Nat. Med. 17 2011 330 339
8. P.J. Skene, and S. Henikoff Histone variants in pluripotency and disease Development 140 2013 2513 2524
9. D. Hanahan, and R.A. Weinberg The hallmarks of cancer Cell 100 2000 57 70
10. D. Hanahan, and R.A. Weinberg Hallmarks of cancer: the next generation Cell 144 2011 646 674
11. J. Luo et al. Principles of cancer therapy: oncogene and non-oncogene addiction Cell 136 2009 823 837
12. A.M. Gonzalez-Angulo et al. Future of personalized medicine in oncology: a systems biology approach J. Clin. Oncol. 28 2010 2777 2783
13. M. Vidal et al. Interactome networks and human disease Cell 144 2011 986 998
14. C.B. Bridges The origin of variation Am. Nat. 56 1922 51 63
15. T. Dobzhansky Genetics of natural populations. XIII. Recombination and variability in populations of Drosphila pseudoobscura Genetics 31 1946 269 290
16. J.C. Lucchesi Synthetic lethality and semi-lethality among functionally related mutants of Drosophila melanogaster Genetics 59 1968 37 44
17. A.H. Sturtevant A highly specific complementary lethal system in Drosophila melanogaster Genetics 41 1956 118 123
18. L.H. Hartwell et al. Integrating genetic approaches into the discovery of anticancer drugs Science 278 1997 1064 1068
19. W.G. Kaelin Jr Choosing anticancer drug targets in the postgenomic era J. Clin. Invest. 104 1999 1503 1506
20. W.G. Kaelin Jr Synthetic lethality: a framework for the development of wiser cancer therapeutics Genome Med. 1 2009 99
21. H.C. Reinhardt et al. Exploiting synthetic lethal interactions for targeted cancer therapy Cell Cycle 8 2009 3112 3119
22. B. Lehner et al. Systematic mapping of genetic interactions in Caenorhabditis elegans identifies common modifiers of diverse signaling pathways Nat. Genet. 38 2006 896 903
23. C. Queitsch et al. Hsp90 as a capacitor of phenotypic variation Nature 417 2002 618 624
24. M. Costanzo et al. The genetic landscape of a cell Science 327 2010 425 431
25. M. Bots, and R.W. Johnstone Rational combinations using HDAC inhibitors Clin. Cancer Res. 15 2009 3970 3977
26. G. Soria et al. Prime, repair, restore: the active role of chromatin in the DNA damage response Mol. Cell 46 2012 722 734
27. P.A. Marks, and R. Breslow Dimethyl sulfoxide to vorinostat: development of this histone deacetylase inhibitor as an anticancer drug Nat. Biotechnol. 25 2007 84 90
28. O. Khan, and N.B. La Thangue HDAC inhibitors in cancer biology: emerging mechanisms and clinical applications Immunol. Cell Biol. 90 2012 85 94
29. L.A. Petruccelli et al. Expression of leukemia-associated fusion proteins increases sensitivity to histone deacetylase inhibitor-induced DNA damage and apoptosis Mol. Cancer Ther. 12 2013 1591 1604
30. S. Ropero, and M. Esteller The role of histone deacetylases (HDACs) in human cancer Mol. Oncol. 1 2007 19 25
31. H. Shen, and P.W. Laird Interplay between the cancer genome and epigenome Cell 153 2013 38 55
32. Z. Wang et al. Genome-wide mapping of HATs and HDACs reveals distinct functions in active and inactive genes Cell 138 2009 1019 1031
33. S. Kubicek et al. Chromatin-targeting small molecules cause class-specific transcriptional changes in pancreatic endocrine cells Proc. Natl. Acad. Sci. U.S.A. 109 2012 5364 5369
34. X. Yang et al. Targeting DNA, methylation for epigenetic therapy Trends Pharmacol. Sci. 31 2010 536 546
35. J.K. Christman 5-Azacytidine and 5-aza-2′-deoxycytidine as inhibitors of DNA methylation: mechanistic studies and their implications for cancer therapy Oncogene 21 2002 5483 5495
36. R. Juttermann et al. Toxicity of 5-aza-2′-deoxycytidine to mammalian cells is mediated primarily by covalent trapping of DNA methyltransferase rather than DNA demethylation Proc. Natl. Acad. Sci. U.S.A. 91 1994 11797 11801
37. M.L. Orta et al. 5-Aza-2′-deoxycytidine causes replication lesions that require Fanconi anemia-dependent homologous recombination for repair Nucleic Acids Res. 41 2013 5827 5836
38. T.J. Ley et al. DNMT3A mutations in acute myeloid leukemia N. Engl. J. Med. 363 2010 2424 2433
39. M.J. Walter et al. Recurrent DNMT3A mutations in patients with myelodysplastic syndromes Leukemia 25 2011 1153 1158
40. K.H. Metzeler et al. DNMT3A mutations and response to the hypomethylating agent decitabine in acute myeloid leukemia Leukemia 26 2012 1106 1107
41. L. Di Croce et al. Methyltransferase recruitment and DNA hypermethylation of target promoters by an oncogenic transcription factor Science 295 2002 1079 1082
42. E. Vire et al. The polycomb group protein EZH2 directly controls DNA methylation Nature 439 2006 871 874
43. J.E. Bradner et al. Chemical phylogenetics of histone deacetylases Nat. Chem. Biol. 6 2010 238 243
44. L.A. Garraway, and E.S. Lander Lessons from the cancer genome Cell 153 2013 17 37
45. C. Kandoth et al. Mutational landscape and significance across 12 major cancer types Nature 502 2013 333 339
46. W. Timp, and A.P. Feinberg Cancer as a dysregulated epigenome allowing cellular growth advantage at the expense of the host Nat. Rev. Cancer 13 2013 497 510
47. E.J. Geutjes et al. Targeting the epigenome for treatment of cancer Oncogene 31 2012 3827 3844
48. R.D. Morin et al. Somatic mutations altering EZH2 (Tyr641) in follicular and diffuse large B-cell lymphomas of germinal-center origin Nat. Genet. 42 2010 181 185
49. S.K. Knutson et al. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells Nat. Chem. Biol. 8 2012 890 896
50. M.T. McCabe et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations Nature 492 2012 108 112
51. W. Qi et al. Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation Proc. Natl. Acad. Sci. U.S.A. 109 2012 21360 21365
52. C.I. Ene et al. Histone demethylase Jumonji D3 (JMJD3) as a tumor suppressor by regulating p53 protein nuclear stabilization PLoS ONE 7 2012 e51407
53. G. van Haaften et al. Somatic mutations of the histone H3K27 demethylase gene UTX in human cancer Nat. Genet. 41 2009 521 523
54. C.A. French et al. Midline carcinoma of children and young adults with NUT rearrangement J. Clin. Oncol. 22 2004 4135 4139
55. B.E. Schwartz et al. Differentiation of NUT midline carcinoma by epigenomic reprogramming Cancer Res. 71 2011 2686 2696
56. P. Filippakopoulos et al. Selective inhibition of BET bromodomains Nature 468 2010 1067 1073
57. E. Nicodeme et al. Suppression of inflammation by a synthetic histone mimic Nature 468 2010 1119 1123
58. M.F. Segura et al. BRD4 sustains melanoma proliferation and represents a new target for epigenetic therapy Cancer Res. 73 2013 6264 6276
59. J.E. Delmore et al. BET bromodomain inhibition as a therapeutic strategy to target c-Myc Cell 146 2011 904 917
60. J. Zuber et al. RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia Nature 478 2011 524 528
61. M.A. Dawson et al. Targeting epigenetic readers in cancer N. Engl. J. Med. 367 2012 647 657
62. R. Popovic, and J.D. Licht Emerging epigenetic targets and therapies in cancer medicine Cancer Discov. 2 2012 405 413
63. J. Loven et al. Selective inhibition of tumor oncogenes by disruption of super-enhancers Cell 153 2013 320 334
64. A.G. Muntean, and J.L. Hess The pathogenesis of mixed-lineage leukemia Annu. Rev. Pathol. 7 2012 283 301
65. K.M. Bernt et al. MLL-rearranged leukemia is dependent on aberrant H3K79 methylation by DOT1L Cancer Cell 20 2011 66 78
66. M.J. Chang et al. Histone H3 lysine 79 methyltransferase Dot1 is required for immortalization by MLL oncogenes Cancer Res. 70 2010 10234 10242
67. S.Y. Jo et al. Requirement for Dot1l in murine postnatal hematopoiesis and leukemogenesis by MLL translocation Blood 117 2011 4759 4768
68. A.T. Nguyen et al. DOT1L, the H3K79 methyltransferase, is required for MLL-AF9-mediated leukemogenesis Blood 117 2011 6912 6922
69. S.R. Daigle et al. Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor Cancer Cell 20 2011 53 65
70. T. Neff, and S.A. Armstrong Recent progress toward epigenetic therapies: the example of mixed lineage leukemia Blood 121 2013 4847 4853
71. S.R. Daigle et al. Potent inhibition of DOT1L as treatment of MLL-fusion leukemia Blood 122 2013 1017 1025
72. J. Grembecka et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia Nat. Chem. Biol. 8 2012 277 284
73. A. Yokoyama et al. The menin tumor suppressor protein is an essential oncogenic cofactor for MLL-associated leukemogenesis Cell 123 2005 207 218
74. H.P. Kuo et al. Epigenetic roles of MLL oncoproteins are dependent on NF-kappaB Cancer Cell 24 2013 423 437
75. P.G. Miller et al. In vivo RNAi screening identifies a leukemia-specific dependence on integrin beta 3 signaling Cancer Cell 24 2013 45 58
76. T. Pemovska et al. Individualized systems medicine (ISM) strategy to tailor treatments for patients with chemorefractory acute myeloid leukemia Cancer Discov. 3 2013 1416 1429