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Probing the epigenome

Nature Chemical Biology volume 11, pages 542–545 (2015)Cite this article

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Epigenetic chemical probes are having a strong impact in biological discovery and target validation. Systematic coverage of emerging epigenetic target classes with these potent, selective, cell-active chemical tools will profoundly influence understanding of the human biology and pathology of chromatin-templated mechanisms.

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Figure 1: Leveling the landscape of epigenetics research (a,b).
Figure 2: Epigenetic chemical probes are extensively used.
Figure 3: Chemical biology tools for epigenetic drug discovery.

References

  1. Edwards, A.M. et al. Nature 470, 163–165 (2011).

    Article  CAS  Google Scholar 

  2. Fedorov, O., Muller, S. & Knapp, S. Nat. Chem. Biol. 6, 166–169 (2010).

    Article  CAS  Google Scholar 

  3. Bunnage, M.E., Chekler, E.L. & Jones, L.H. Nat. Chem. Biol. 9, 195–199 (2013).

    Article  CAS  Google Scholar 

  4. Arrowsmith, C.H., Bountra, C., Fish, P.V., Lee, K. & Schapira, M. Nat. Rev. Drug Discov. 11, 384–400 (2012).

    Article  CAS  Google Scholar 

  5. Welter, D. et al. Nucleic Acids Res. 42, D1001–D1006 (2014).

    Article  CAS  Google Scholar 

  6. Cheung, H.W. et al. Proc. Natl. Acad. Sci. USA 108, 12372–12377 (2011).

    Article  CAS  Google Scholar 

  7. Baldwin, R.M. et al. Oncotarget 6, 3013–3032 (2015).

    Article  Google Scholar 

  8. Yao, R. et al. Cancer Res. 74, 5656–5667 (2014).

    Article  CAS  Google Scholar 

  9. Meyer, T.E. et al. PLoS Genet. 6, e1001045 (2010).

    Article  Google Scholar 

  10. Filippakopoulos, P. et al. Nature 468, 1067–1073 (2010).

    Article  CAS  Google Scholar 

  11. Nicodeme, E. et al. Nature 468, 1119–1123 (2010).

    Article  CAS  Google Scholar 

  12. Filippakopoulos, P. & Knapp, S. Nat. Rev. Drug Discov. 13, 337–356 (2014).

    Article  CAS  Google Scholar 

  13. Chan-Penebre, E. et al. Nat. Chem. Biol. 11, 432–437 (2015).

    Article  CAS  Google Scholar 

  14. Copeland, R.A. Clin. Cancer Res. 19, 6344–6350 (2013).

    Article  CAS  Google Scholar 

  15. Bitler, B.G. et al. Nat. Med. 21, 231–238 (2015).

    Article  CAS  Google Scholar 

  16. Mack, S.C. et al. Nature 506, 445–450 (2014).

    Article  CAS  Google Scholar 

  17. Chen, C.W. et al. Nat. Med. 21, 335–343 (2015).

    Article  CAS  Google Scholar 

  18. Stratikopoulos, E.E. et al. Cancer Cell 27, 837–851 (2015).

    Article  CAS  Google Scholar 

  19. Borkin, D. et al. Cancer Cell 27, 589–602 (2015).

    Article  CAS  Google Scholar 

  20. Cao, F. et al. Mol. Cell 53, 247–261 (2014).

    Article  CAS  Google Scholar 

  21. Malik, R. et al. Nat. Med. 21, 344–352 (2015).

    Article  CAS  Google Scholar 

  22. Grebien, F. Nat. Chem. Biol. doi:10.1038/nchembio.1859 (13 July 2015).

    Article  CAS  Google Scholar 

  23. Shi, Y. et al. Cell Stem Cell 3, 568–574 (2008).

    Article  CAS  Google Scholar 

  24. Shi, Y. et al. Cell Stem Cell 2, 525–528 (2008).

    Article  CAS  Google Scholar 

  25. Schones, D.E., Chen, X., Trac, C., Setten, R. & Paddison, P.J. Epigenetics Chromatin 7, 23 (2014).

    Article  Google Scholar 

  26. Yu, H. et al. Cell Death Dis. 4, e506 (2013).

    Article  CAS  Google Scholar 

  27. Gibaja, V. et al. Oncogene doi:10.1038/onc.2015.114 (20 April 2015).

    Article  CAS  Google Scholar 

  28. Frye, S.V. Nat. Chem. Biol. 6, 159–161 (2010).

    Article  CAS  Google Scholar 

  29. James, L.I. et al. Nat. Chem. Biol. 9, 184–191 (2013).

    Article  CAS  Google Scholar 

  30. Xhemalce, B., Robson, S.C. & Kouzarides, T. Cell 151, 278–288 (2012).

    Article  CAS  Google Scholar 

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Author information

Authors and Affiliations

  1. Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada

    Andrea Huston, Cheryl H Arrowsmith & Matthieu Schapira

  2. Princess Margaret Cancer Centre, University of Toronto, Toronto, Ontario, Canada

    Cheryl H Arrowsmith

  3. Department of Medical Biophysics, University of Toronto, Toronto, Ontario, Canada

    Cheryl H Arrowsmith

  4. Nuffield Department of Clinical Medicine, University of Oxford, Oxford, UK

    Stefan Knapp

  5. Target Discovery Institute, University of Oxford, Oxford, UK

    Stefan Knapp

  6. Structural Genomic Consortium, University of Oxford, Oxford, UK

    Stefan Knapp

  7. Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe University, Frankfurt am Main, Germany

    Stefan Knapp

  8. Department of Pharmacology and Toxicology, University of Toronto, Toronto, Ontario, Canada

    Matthieu Schapira

Authors
  1. Andrea Huston
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  2. Cheryl H Arrowsmith
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  3. Stefan Knapp
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  4. Matthieu Schapira
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Corresponding authors

Correspondence to Stefan Knapp or Matthieu Schapira.

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The authors declare no competing financial interests.

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Supplementary Figures 1–2 and Supplementary Tables 1–2 (PDF 1504 kb)

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Huston, A., Arrowsmith, C., Knapp, S. et al. Probing the epigenome. Nat Chem Biol 11, 542–545 (2015). https://doi.org/10.1038/nchembio.1871

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