Future strategies in epigenetic drug discovery

Drug Discovery Today: Therapeutic Strategies

Volumn 9, Issue 2-3, 2012, Pages

  Drewes, Gerard ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ADAPTOR PROTEIN BRD4; BETA CATENIN; HISTONE DEACETYLASE 1; HISTONE DEACETYLASE INHIBITOR; HISTONE DEMETHYLASE; HISTONE METHYLTRANSFERASE; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE 5; PROTEIN; PROTEIN KINASE INHIBITOR; SHORT HAIRPIN RNA; TANKYRASE; UNCLASSIFIED DRUG;

ACUTE GRANULOCYTIC LEUKEMIA; AFFINITY CHROMATOGRAPHY; ARTICLE; BINDING SITE; CELL CYCLE ARREST; CELL DIFFERENTIATION; CHROMATIN; DISSOCIATION CONSTANT; DNA METHYLATION; DNA MODIFICATION; DRUG BINDING; DRUG DEVELOPMENT; DRUG POTENCY; DRUG SELECTIVITY; DRUG TARGETING; ENZYME BINDING; ENZYME INHIBITION; EPIGENETICS; GENE CONTROL; HIGH THROUGHPUT SCREENING; HISTONE ACETYLATION; HISTONE MODIFICATION; HUMAN; MASS SPECTROMETRY; NONHUMAN; PATHOPHYSIOLOGY; PHENOTYPE; PROTEIN DOMAIN; PROTEIN EXPRESSION; PROTEIN PROTEIN INTERACTION; PROTEOMICS; RNA INTERFERENCE; STRUCTURAL GENOMICS; STRUCTURE ACTIVITY RELATION;

EID: 84871451955     PISSN: None     EISSN: 17406773     Source Type: Journal    
DOI: 10.1016/j.ddstr.2011.12.001     Document Type: Review

References (42)

1. Bannister, A.J. and Kouzarides, T. (2011) Regulation of chromatin by histone modifications. Cell Res. 21, 381-395
2. Heightman, T.D. (2011) Therapeutic prospects for epigenetic modulation. Expert. Opin. Ther. Targets 15, 729-740
3. Alberts, B. (1998) The cell as a collection of protein machines: preparing the next generation of molecular biologists. Cell 92, 291-294 (Pubitemid 28093007)
4. Malovannaya, A. et al. (2011) Analysis of the human endogenous coregulator complexome. Cell 145, 787-799
5. Margueron, R. and Reinberg, D. (2010) Chromatin structure and the inheritance of epigenetic information. Nat. Rev. Genet. 11, 285-296
6. Low, J. et al. (2008) Prioritizing hits from phenotypic high-content screens. Curr. Opin. Drug Discov. Dev. 11, 338-345 (Pubitemid 351572443)
7. Quon, K. and Kassner, P.D. (2009) RNA interference screening for the discovery of oncology targets. Expert Opin. Ther. Targets 13, 1027-1035
8. Zuber, J. et al. (2011) Toolkit for evaluating genes required for proliferation and survival using tetracycline-regulated RNAi. Nat. Biotechnol. 29, 79-83
9. Zuber, J. et al. (2011) RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia. Nature 478, 524-528
10. Jackson, A.L. and Linsley, P.S. (2010) Recognizing and avoiding siRNA off-target effects for target identification and therapeutic application. Nat. Rev. Drug Discov. 9, 57-67
11. Knight, Z.A. and Shokat, K.M. (2005) Features of selective kinase inhibitors. Chem. Biol. 12, 621-637 (Pubitemid 43142039)
12. Copeland, R.A. et al. (2009) Protein methyltransferases as a target class for drug discovery. Nat. Rev. Drug Discov. 8, 724-732
13. Rose, N.R. et al. (2011) Inhibition of 2-oxoglutarate dependent oxygenases. Chem. Soc. Rev. 40, 4364-4397
14. Karaman, M.W. et al. (2008) A quantitative analysis of kinase inhibitor selectivity. Nat. Biotechnol. 26, 127-132
15. Feng, Y. et al. (2009) Multi-parameter phenotypic profiling: using cellular effectsto characterize small-molecule compounds. Nat. Rev. Drug Discov. 8, 567-578
16. Swinney, D.C. and Anthony, J. (2011) How were new medicines discovered? Nat. Rev. Drug Discov. 10, 507-519
17. Terstappen, G.C. et al. (2007) Target deconvolution strategies in drug discovery. Nat. Rev. Drug Discov. 6, 891-903 (Pubitemid 350042397)
18. Brown, E.J. et al. (1994) A mammalian protein targeted by G1-arresting rapamycin-receptor complex. Nature 369, 756-758
19. Harding, M.W. et al. (1989) A receptor for the immunosuppressant FK506 is a cis-trans peptidyl-prolyl isomerase. Nature 341, 758-760 (Pubitemid 19260893)
20. Taunton, J. et al. (1996) A mammalian histone deacetylase related to the yeast transcriptional regulator Rpd3p. Science 272, 408-411 (Pubitemid 26138177)
21. Richon, V.M. et al. (1996) Second generation hybrid polar compounds are potent inducers of transformed cell differentiation. Proc. Natl. Acad. Sci. U. S. A. 93, 5705-5708 (Pubitemid 26191313)
22. Marks, P.A. (2010) The clinical development of histone deacetylase inhibitors as targeted anticancer drugs. Expert Opin. Investig. Drugs 19, 1049-1066
23. Marks, P.A. and Breslow, R. (2007) Dimethyl sulfoxide to vorinostat: development of this histone deacetylase inhibitor as an anticancer drug. Nat. Biotechnol. 25, 84-90 (Pubitemid 46087907)
24. Mayr, L.M. and Bojanic, D. (2009) Novel trends in high-throughput screening. Curr. Opin. Pharmacol. 9, 580-588
25. Emami, K.H. et al. (2004) A small molecule inhibitor of beta-catenin/CREB-binding protein transcription [corrected]. Proc. Natl. Acad. Sci. U. S. A. 101, 12682-12687 (Pubitemid 39122083)
26. Huang, S.M. et al. (2009) Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature 461, 614-620
27. Chung, C.W. et al. (2011) Discovery and characterization of small molecule inhibitors of the BET family bromodomains. J. Med. Chem. 54, 3827-3838
28. Nicodeme, E. et al. (2010) Suppression of inflammation by a synthetic histone mimic. Nature 468, 1119-1123
29. Domon, B. and Aebersold, R. (2010) Options and considerations when selecting a quantitative proteomics strategy. Nat. Biotechnol. 28, 710-721
30. Mallick, P. and Kuster, B. (2010) Proteomics: a pragmatic perspective. Nat. Biotechnol. 28, 695-709
31. Pasini, D. et al. (2004) Suz12 is essential for mouse development and for EZH2 histone methyltransferase activity. EMBO J. 23, 4061-4071 (Pubitemid 39472427)
32. Guenther, M.G. et al. (2001) The SMRT and N-CoR corepressors are activating cofactors for histone deacetylase 3. Mol. Cell Biol. 21, 6091-6101 (Pubitemid 34263509)
33. Zhang, Y. et al. (1999) Analysis of the NuRD subunits reveals a histone deacetylase core complex and a connection with DNA methylation. Genes Dev. 13, 1924-1935 (Pubitemid 29407360)
34. Eberl, H.C. et al. (2011) Quantitative proteomics for epigenetics. Chembiochem 12, 224-234
35. Bartke, T. et al. (2010) Nucleosome-interacting proteins regulated by DNA and histone methylation. Cell 143, 470-484
36. Vermeulen, M. et al. (2010) Quantitative interaction proteomics and genome-wide profiling of epigenetic histone marks and their readers. Cell 142, 967-980
37. Bantscheff, M. et al. (2011) Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes. Nat. Biotechnol. 29, 255-265
38. Holson, E.B. and Schreiber, S.L. (2011) Chemoproteomics quantifies complexity. Nat. Biotechnol. 29, 235-236
39. Ramsden, N. et al. (2011) Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons. ACS Chem. Biol. 6, 1021-1028
40. Dawson, M.A. et al. (2011) Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature 478, 529-533
41. Koehler, A.N. (2010) A complex task? Direct modulation of transcription factors with small molecules Curr. Opin. Chem. Biol. 14, 331-340
42. Wells, J.A. and McClendon, C.L. (2007) Reaching for high-hanging fruit in drug discovery at protein-protein interfaces. Nature 450, 1001-1009 (Pubitemid 350273630)