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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.

Advances in genomics and proteomics methodologies in recent years have made it possible to associate thousands of genes and proteins with specific diseases, biological processes, molecular networks and pathways. However, data from these large-scale initiatives alone have not translated widely into new studies on these disease-associated proteins, and the biomedical-research community still tends to focus on proteins that were already known before the sequencing of the human genome1. For instance, the human kinome, a target class of direct relevance to cancer and other disease areas, is a telling example: among research articles indexed in PubMed in 2011, 75% of the research activity focused on only 10% of the 518 human kinases—largely the same kinases that were the focus of research before sequencing of the human genome—whereas 60% of the kinome (comprising approximately 300 enzymes) was virtually ignored by the community2.

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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.

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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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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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