Targeting epigenetic readers in cancer

New England Journal of Medicine

Volumn 367, Issue 7, 2012, Pages 647-657

  Dawson, Mark A ^a,b,c   Kouzarides, Tony ^c   Huntly, Brian J P ^a,b,d  

^a UNIVERSITY OF CAMBRIDGE   (United Kingdom)

^b CAMBRIDGE UNIVERSITY HOSPITALS NHS FOUNDATION TRUST   (United Kingdom)

^c UNIVERSITY OF CAMBRIDGE   (United Kingdom)

^d UNIVERSITY OF CAMBRIDGE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; BROMODOMAIN AND EXTRATERMINAL PROTEIN 2; BROMODOMAIN AND EXTRATERMINAL PROTEIN 3; BROMODOMAIN AND EXTRATERMINAL PROTEIN 4; I BET 151; I BET 762; JQ 1; TUMOR PROTEIN; UNCLASSIFIED DRUG;

ACUTE GRANULOCYTIC LEUKEMIA; BINDING AFFINITY; BINDING SITE; BURKITT LYMPHOMA; CANCER GENETICS; CANCER RESEARCH; CARCINOGENESIS; CHROMATIN; DISEASE ASSOCIATION; DRUG PROTEIN BINDING; DRUG STRUCTURE; DRUG TARGETING; EPIGENETICS; GENE FUNCTION; GENOME ANALYSIS; HUMAN; MIXED LINEAGE LEUKEMIA GENE; MOLECULAR DYNAMICS; MOLECULAR PATHOLOGY; MULTIPLE MYELOMA; NONHUMAN; ONCOGENE; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN EXPRESSION; PROTEIN PROTEIN INTERACTION; REVIEW;

EID: 84865005165     PISSN: 00284793     EISSN: 15334406     Source Type: Journal    
DOI: 10.1056/NEJMra1112635     Document Type: Review

References (60)

1. Rowley JD. Chromosomal translocations: revisited yet again. Blood 2008; 112:2183-9.
2. Chen J, Odenike O, Rowley JD. Leukaemogenesis: more than mutant genes. Nat Rev Cancer 2010;10:23-36.
3. Wouters BJ, Löwenberg B, Delwel R. A decade of genome-wide gene expression profiling in acute myeloid leukemia: flashback and prospects. Blood 2009;113:291-8.
4. Stratton MR, Campbell PJ, Futreal PA. The cancer genome. Nature 2009;458:719-24.
5. Forbes SA, Bindal N, Bamford S, et al. COSMIC: mining complete cancer genomes in the Catalogue of Somatic Mutations in Cancer. Nucleic Acids Res 2011;39:D945-D950.
6. Allis CD, Jenuwein T, Reinberg D. Epigenetics. Cold Spring Harbor, NY: Cold Spring Harbor Laboratory Press, 2007.
7. Berger SL, Kouzarides T, Shiekhattar R, Shilatifard A. An operational definition of epigenetics. Genes Dev 2009;23:781-3.
8. Segal E, Widom J. What controls nucleosome positions? Trends Genet 2009;25:335-43.
9. Kouzarides T. Chromatin modifications and their function. Cell 2007;128:693-705. (Pubitemid 46273577)
10. Baylin SB, Jones PA. A decade of exploring the cancer epigenome - biological and translational implications. Nat Rev Cancer 2011;11:726-34.
11. Wu H, Zhang Y. Mechanisms and functions of Tet protein-mediated 5-methylcytosine oxidation. Genes Dev 2011;25:2436-52.
12. Tan M, Luo H, Lee S, et al. Identification of 67 histone marks and histone lysine crotonylation as a new type of histone modification. Cell 2011;146:1016-28.
13. Barski A, Cuddapah S, Cui K, et al. High-resolution profiling of histone methylations in the human genome. Cell 2007;129:823-37. (Pubitemid 46802390)
14. Rando OJ, Chang HY. Genome-wide views of chromatin structure. Annu Rev Biochem 2009;78:245-71.
15. Taverna SD, Li H, Ruthenburg AJ, Allis CD, Patel DJ. How chromatin-binding modules interpret histone modifications: lessons from professional pocket pickers. Nat Struct Mol Biol 2007;14:1025-40. (Pubitemid 350060344)
16. Bannister AJ, Kouzarides T. Regulation of chromatin by histone modifications. Cell Res 2011;21:381-95.
17. Tefferi A, Vardiman JW. Myelodysplastic syndromes. N Engl J Med 2009;361:1872-85.
18. Garcia-Manero G, Fenaux P. Hypomethylating agents and other novel strategies in myelodysplastic syndromes. J Clin Oncol 2011;29:516-23.
19. Foss FM, Zinzani PL, Vose JM, Gascoyne RD, Rosen ST, Tobinai K. Peripheral T-cell lymphoma. Blood 2011;117:6756-67.
20. Lan F, Collins RE, De Cegli R, et al. Recognition of unmethylated histone H3 lysine 4 links BHC80 to LSD1-mediated gene repression. Nature 2007;448:718-22. (Pubitemid 47236862)
21. Ooi SK, Qiu C, Bernstein E, et al. DNMT3L connects unmethylated lysine 4 of histone H3 to de novo methylation of DNA. Nature 2007;448:714-7. (Pubitemid 47236857)
22. Peña PV, Davrazou F, Shi X, et al. Molecular mechanism of histone H3K4me3 recognition by plant homeodomain of ING2. Nature 2006;442:100-3. (Pubitemid 44064217)
23. Shi X, Hong T, Walter KL, et al. ING2 PHD domain links histone H3 lysine 4 methylation to active gene repression. Nature 2006;442:96-9. (Pubitemid 44064216)
24. Bannister AJ, Zegerman P, Partridge JF, et al. Selective recognition of methylated lysine 9 on histone H3 by the HP1 chromo domain. Nature 2001;410:120-4. (Pubitemid 32225848)
25. Lachner M, O'Carroll D, Rea S, Mechtler K, Jenuwein T. Methylation of histone H3 lysine 9 creates a binding site for HP1 proteins. Nature 2001;410:116-20. (Pubitemid 32225847)
26. Fischle W, Wang Y, Jacobs SA, Kim Y, Allis CD, Khorasanizadeh S. Molecular basis for the discrimination of repressive methyl-lysine marks in histone H3 by Polycomb and HP1 chromodomains. Genes Dev 2003;17:1870-81. (Pubitemid 36944564)
27. Dhalluin C, Carlson JE, Zeng L, He C, Aggarwal AK, Zhou MM. Structure and ligand of a histone acetyltransferase bromodomain. Nature 1999;399:491-6. (Pubitemid 29258857)
28. Jacobson RH, Ladurner AG, King DS, Tjian R. Structure and function of a human TAFII250 double bromodomain module. Science 2000;288:1422-5. (Pubitemid 30366328)
29. Ruthenburg AJ, Li H, Patel DJ, Allis CD. Multivalent engagement of chromatin modifications by linked binding modules. Nat Rev Mol Cell Biol 2007;8:983-94. (Pubitemid 350174643)
30. Matthews AG, Kuo AJ, Ramón-Maiques S, et al. RAG2 PHD finger couples histone H3 lysine 4 trimethylation with V(D)J recombination. Nature 2007;450:1106-10. (Pubitemid 350273622)
31. Chi P, Allis CD, Wang GG. Covalent histone modifications - miswritten, misinterpreted and mis-erased in human cancers. Nat Rev Cancer 2010;10:457-69.
32. Dawson MA, Prinjha RK, Dittmann A, et al. Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature 2011;478:529-33.
33. Filippakopoulos P, Qi J, Picaud S, et al. Selective inhibition of BET bromodomains. Nature 2010;468:1067-73.
34. Nicodeme E, Jeffrey KL, Schaefer U, et al. Suppression of inflammation by a synthetic histone mimic. Nature 2010;468:1119-23.
35. Chung CW, Dean AW, Woolven JM, Bamborough P. Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery. J Med Chem 2012;55:576-86.
36. Bamborough P, Diallo H, Goodacre JD, et al. Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides. J Med Chem 2012;55:587-96.
37. Chiang CM. Brd4 engagement from chromatin targeting to transcriptional regulation: selective contact with acetylated histone H3 and H4. F1000 Biol Rep 2009;1:98.
38. Jiang YW, Veschambre P, Erdjument-Bromage H, et al. Mammalian mediator of transcriptional regulation and its possible role as an end-point of signal transduction pathways. Proc Natl Acad Sci U S A 1998;95:8538-43. (Pubitemid 28350523)
39. Malik S, Roeder RG. The metazoan Mediator co-activator complex as an integrative hub for transcriptional regulation. Nat Rev Genet 2010;11:761-72.
40. Yang Z, Yik JH, Chen R, et al. Recruitment of P-TEFb for stimulation of transcriptional elongation by the bromodomain protein Brd4. Mol Cell 2005;19:535-45. (Pubitemid 41140010)
41. Jang MK, Mochizuki K, Zhou M, Jeong HS, Brady JN, Ozato K. The bromodomain protein Brd4 is a positive regulatory component of P-TEFb and stimulates RNA polymerase II-dependent transcription. Mol Cell 2005;19:523-34. (Pubitemid 41140009)
42. Zhao R, Nakamura T, Fu Y, Lazar Z, Spector DL. Gene bookmarking accelerates the kinetics of post-mitotic transcriptional re-activation. Nat Cell Biol 2011;13:1295-304.
43. Shang E, Wang X, Wen D, Greenberg DA, Wolgemuth DJ. Double bromodomain-containing gene Brd2 is essential for embryonic development in mouse. Dev Dyn 2009;238:908-17.
44. Houzelstein D, Bullock SL, Lynch DE, Grigorieva EF, Wilson VA, Beddington RS. Growth and early postimplantation defects in mice deficient for the bromodomain-containing protein Brd4. Mol Cell Biol 2002;22:3794-802. (Pubitemid 34525221)
45. Zuber J, Shi J, Wang E, et al. RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia. Nature 2011;478:524-8.
46. Delmore JE, Issa GC, Lemieux ME, et al. BET bromodomain inhibition as a therapeutic strategy to target c-Myc. Cell 2011;146:904-17.
47. Mertz JA, Conery AR, Bryant BM, et al. Targeting MYC dependence in cancer by inhibiting BET bromodomains. Proc Natl Acad Sci U S A 2011;108:16669-74.
48. French CA. Demystified molecular pathology of NUT midline carcinomas. J Clin Pathol 2010;63:492-6.
49. Krivtsov AV, Armstrong SA. MLL translocations, histone modifications and leukaemia stem-cell development. Nat Rev Cancer 2007;7:823-33. (Pubitemid 350006257)
50. Mohan M, Lin C, Guest E, Shilatifard A. Licensed to elongate: a molecular mechanism for MLL-based leukaemogenesis. Nat Rev Cancer 2010;10:721-8.
51. Mueller D, García-Cuellar MP, Bach C, Buhl S, Maethner E, Slany RK. Misguided transcriptional elongation causes mixed lineage leukemia. PLoS Biol 2009;7(11):e1000249.
52. Lin C, Smith ER, Takahashi H, et al. 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;37:429-37.
53. Yokoyama A, Lin M, Naresh A, Kitabayashi I, Cleary ML. A higher-order complex containing AF4 and ENL family proteins with P-TEFb facilitates oncogenic and physiologic MLL-dependent transcription. Cancer Cell 2010;17:198-212.
54. Milne TA, Kim J, Wang GG, et al. Multiple interactions recruit MLL1 and MLL1 fusion proteins to the HOXA9 locus in leukemogenesis. Mol Cell 2010;38:853-63.
55. Muntean AG, Tan J, Sitwala K, et al. The PAF complex synergizes with MLL fusion proteins at HOX loci to promote leukemogenesis. Cancer Cell 2010;17:609-21.
56. Chapman MA, Lawrence MS, Keats JJ, et al. Initial genome sequencing and analysis of multiple myeloma. Nature 2011;471:467-72.
57. Shou Y, Martelli ML, Gabrea A, et al. Diverse karyotypic abnormalities of the c-myc locus associated with c-myc dysregulation and tumor progression in multiple myeloma. Proc Natl Acad Sci U S A 2000;97:228-33. (Pubitemid 30055813)
58. Meyer N, Penn LZ. Reflecting on 25 years with MYC. Nat Rev Cancer 2008;8:976-90.
59. Garnett MJ, Edelman EJ, Heidorn SJ, et al. Systematic identification of genomic markers of drug sensitivity in cancer cells. Nature 2012;483:570-5.
60. Barretina J, Caponigro G, Stransky N, et al. The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity. Nature 2012;483:603-7.