Skip to main content

Thank you for visiting nature.com. You are using a browser version with limited support for CSS. To obtain the best experience, we recommend you use a more up to date browser (or turn off compatibility mode in Internet Explorer). In the meantime, to ensure continued support, we are displaying the site without styles and JavaScript.

A public-private partnership to unlock the untargeted kinome

Chemical probes are urgently needed to functionally annotate hitherto-untargeted kinases and stimulate new drug discovery efforts to address unmet medical needs. The size of the human kinome combined with the high cost associated with probe generation severely limits access to new probes. We propose a large-scale public-private partnership as a new approach that offers economies of scale, minimized redundancy and sharing of risk and cost.

Your institute does not have access to this article

Relevant articles

Open Access articles citing this article.

Access options

Buy article

Get time limited or full article access on ReadCube.

$32.00

All prices are NET prices.

Figure 1: Value chain of kinase inhibitors based on validation for biological investigations.

References

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

    CAS  Article  Google Scholar 

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

    CAS  Article  Google Scholar 

  3. Bantscheff, M. et al. Nat. Biotechnol. 25, 1035–1044 (2007).

    CAS  Article  Google Scholar 

  4. Patricelli, M.P. et al. Chem. Biol. 18, 699–710 (2011).

    CAS  Article  Google Scholar 

  5. Davis, M.I. et al. Nat. Biotechnol. 29, 1046–1051 (2011).

    CAS  Article  Google Scholar 

  6. Lin, X. et al. J. Med. Chem. 55, 5749–5759 (2012).

    CAS  Article  Google Scholar 

  7. Fedorov, O. et al. Proc. Natl. Acad. Sci. USA 104, 20523–20528 (2007).

    Google Scholar 

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

    CAS  Article  Google Scholar 

  9. Workman, P. & Collins, I. Chem. Biol. 17, 561–577 (2010).

    CAS  Article  Google Scholar 

  10. Weigelt, J. EMBO Rep. 10, 941–945 (2009).

    CAS  Article  Google Scholar 

  11. Cohen, P. Biochem. J. 425, 53–54 (2010).

    CAS  Article  Google Scholar 

  12. Dowling, J.E. et al. ACS Med. Chem. Lett. 3, 278–283 (2012).

    CAS  Article  Google Scholar 

  13. Al-Lazikani, B., Banerji, U. & Workman, P. Nat. Biotechnol. 30, 679–692 (2012).

    CAS  Article  Google Scholar 

  14. Di Paolo, J.A. et al. Nat. Chem. Biol. 7, 41–50 (2011).

    CAS  Article  Google Scholar 

  15. Deng, X. et al. Nat. Chem. Biol. 7, 203–205 (2011).

    CAS  Article  Google Scholar 

  16. Medina, J.R. et al. J. Med. Chem. 54, 1871–1895 (2011).

    CAS  Article  Google Scholar 

  17. Zhang, T. et al. Chem. Biol. 19, 140–154 (2012).

    CAS  Article  Google Scholar 

  18. Zhang, J. et al. Natur. 463, 501–506 (2010).

    CAS  Article  Google Scholar 

  19. Fedorov, O. et al. Chem. Biol. 18, 67–76 (2011).

    CAS  Article  Google Scholar 

  20. Mott, B.T. et al. Bioorg. Med. Chem. Lett. 19, 6700–6705 (2009).

    CAS  Article  Google Scholar 

  21. Shimomura, T. et al. Mol. Cancer Ther. 9, 157–166 (2010).

    CAS  Article  Google Scholar 

  22. Koeberle, S.C. et al. Nat. Chem. Biol. 8, 141–143 (2011).

    Article  Google Scholar 

  23. Bergamini, G. et al. Nat. Chem. Biol. 8, 576–582 (2012); corrigendum 8, 737 (2012).

    CAS  Article  Google Scholar 

  24. Golding, S.E. et al. Mol. Cancer Ther. 8, 2894–2902 (2009).

    CAS  Article  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to William J Zuercher.

Ethics declarations

Competing interests

S.K. and A.E. are in the Structural Genomics Consortium, an organization that is funded in part to generate research tools and place them in the public domain without restriction on use. J.B. and P.W. are employees of the Institute of Cancer Research, which has a commercial interest in inhibitors of several kinases. P.W. has relevant commercial interactions with Piramed Pharma, Genentech, Chroma Therapeutics, Sareum, Cyclacel, Astex Pharmaceuticals and AstraZeneca.

Rights and permissions

Reprints and Permissions

About this article

Cite this article

Knapp, S., Arruda, P., Blagg, J. et al. A public-private partnership to unlock the untargeted kinome. Nat Chem Biol 9, 3–6 (2013). https://doi.org/10.1038/nchembio.1113

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1038/nchembio.1113

Further reading

Search

Quick links

Nature Briefing

Sign up for the Nature Briefing newsletter — what matters in science, free to your inbox daily.

Get the most important science stories of the day, free in your inbox. Sign up for Nature Briefing