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Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases

Nature Chemical Biology volume 9, pages 136–137 (2013)Cite this article

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Chaetocin is a member of a large family of fungal toxins, which all bear the epipolythiodioxopiperazine (ETP) 'warhead'4. Chaetocin has further been shown to affect a number of structurally and functionally unrelated proteins, with compound activity dependent on the disulfide functionality5,6. We therefore questioned whether the molecule could serve as a specific enzyme inhibitor.

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Figure 1: Inhibitory data of chaetocin (1) and analogs against SUV39H1.

References

  1. Copeland, R.A., Solomon, M.E. & Richon, V.M. Nat. Rev. Drug Discov. 8, 724–732 (2009).

    Article  CAS  Google Scholar 

  2. Cherblanc, F., Chapman-Rothe, N., Brown, R. & Fuchter, M.J. Future Med. Chem. 4, 425–446 (2012).

    Article  CAS  Google Scholar 

  3. Greiner, D., Bonaldi, T., Eskeland, R., Roemer, E. & Imhof, A. Nat. Chem. Biol. 1, 143–145 (2005).

    Article  CAS  Google Scholar 

  4. Iwasa, E., Hamashima, Y. & Sodeoka, M. Isr. J. Chem. 51, 420–433 (2011).

    Article  CAS  Google Scholar 

  5. Tibodeau, J.D., Benson, L.M., Isham, C.R., Owen, W.G. & Bible, K.C. Antioxid. Redox Signal. 11, 1097–1106 (2009).

    Article  CAS  Google Scholar 

  6. Cook, K.M. et al. J. Biol. Chem. 284, 26831–26838 (2009).

    Article  CAS  Google Scholar 

  7. Cherblanc, F. et al. Chemistry 17, 11868–11875 (2011).

    Article  CAS  Google Scholar 

  8. Iwasa, E. et al. J. Am. Chem. Soc. 132, 4078–4079 (2010).

    Article  CAS  Google Scholar 

  9. Takahashi, M. et al. J. Antibiot. (Tokyo) 65, 263–265 (2012).

    Article  CAS  Google Scholar 

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Acknowledgements

We would like to acknowledge Cancer Research UK for funding (grant C21484A6944).

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Authors and Affiliations

  1. Department of Chemistry, Imperial College London, London, UK

    Fanny L Cherblanc & Matthew J Fuchter

  2. Department of Surgery and Cancer, Mechanism and Functional Screening Facility, Imperial College London, London, UK

    Kathryn L Chapman

  3. Department of Surgery and Cancer, Ovarian Cancer Action Research Centre, Imperial College London, London, UK

    Robert Brown

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  1. Fanny L Cherblanc
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  2. Kathryn L Chapman
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  3. Robert Brown
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  4. Matthew J Fuchter
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Correspondence to Matthew J Fuchter.

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Cherblanc, F., Chapman, K., Brown, R. et al. Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases. Nat Chem Biol 9, 136–137 (2013). https://doi.org/10.1038/nchembio.1187

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