Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9 (original) (raw)

Nature Chemical Biology volume 1, pages 143–145 (2005)Cite this article

Abstract

Histone methylation plays a key role in establishing and maintaining stable gene expression patterns during cellular differentiation and embryonic development. Here, we report the characterization of the fungal metabolite chaetocin as the first inhibitor of a lysine-specific histone methyltransferase. Chaetocin is specific for the methyltransferase SU(VAR)3-9 both in vitro and in vivo and may therefore be used to study heterochromatin-mediated gene repression.

This is a preview of subscription content, access via your institution

Access options

Subscribe to this journal

Receive 12 print issues and online access

$259.00 per year

only $21.58 per issue

Buy this article

Prices may be subject to local taxes which are calculated during checkout

Additional access options:

Similar content being viewed by others

Accession codes

Accessions

BINDPlus

References

  1. Wolffe, A.P. Chromatin Structure and Function (Academic Press, San Diego, USA, 1998).
    Google Scholar
  2. Jenuwein, T. & Allis, C.D. Science 293, 1074–1080 (2001).
    Article CAS Google Scholar
  3. Mei, S., Ho, A.D. & Mahlknecht, U. Int. J. Oncol. 25, 1509–1519 (2004).
    CAS PubMed Google Scholar
  4. Hake, S.B., Xiao, A. & Allis, C.D. Br. J. Cancer 90, 761–769 (2004).
    Article CAS Google Scholar
  5. Saveliev, A., Everett, C., Sharpe, T., Webster, Z. & Festenstein, R. Nature 422, 909–913 (2003).
    Article CAS Google Scholar
  6. Rea, S. et al. Nature 406, 593–599 (2000).
    Article CAS Google Scholar
  7. Hauser, D., Weber, H.P. & Sigg, H.P. Helv. Chim. Acta 53, 1061–1073 (1970).
    Article CAS Google Scholar
  8. Baumbusch, L.O. et al. Nucleic Acids Res. 29, 4319–4333 (2001).
    Article CAS Google Scholar
  9. Gardiner, D.M., Waring, P. & Howlett, B.J. Microbiology 151, 1021–1032 (2005).
    Article CAS Google Scholar
  10. Schotta, G. et al. EMBO J. 21, 1121–1131 (2002).
    Article CAS Google Scholar
  11. Bonaldi, T., Imhof, A. & Regula, J.T. Proteomics 4, 1382–1396 (2004).
    Article CAS Google Scholar
  12. Tamaru, H. et al. Nat. Genet. 34, 75–79 (2003).
    Article CAS Google Scholar
  13. Eskeland, R. et al. Biochemistry 43, 3740–3749 (2004).
    Article CAS Google Scholar
  14. Fraga, M.F. et al. Nat. Genet. 37, 391–400 (2005).
    Article CAS Google Scholar

Download references

Acknowledgements

Work in A.I.'s laboratory is funded by grants from the Deutsche Forschungsgemeinschaft (IM23/4-1). D.G. is supported by a predoctoral grant from the University of Munich (FöFoLe #12). T.B. is funded by a long-term postdoctoral fellowship from the European Molecular Biology Organisation (ALTF 642-2003). We thank T. Jenuwein, E. Selker, Y. Shinkai, Y. Cho and P. Singh for valuable reagents, B. Czermin and L. Israel for help with the protein expression and MS analysis, and J. Sutcliffe for critical reading of the manuscript.

Author information

Author notes

  1. Ernst Roemer
    Present address: Institut für Pflanzenbiochemie, Universität Halle, Weinberg 3, Halle (Saale), 06120, Germany

Authors and Affiliations

  1. Department of Molecular Biology, Adolf Butenandt Institute, Histone Modifications Group, Ludwig-Maximillians University of Munich, Schillerstr. 44, Munich, 80336, Germany
    Dorothea Greiner, Tiziana Bonaldi, Ragnhild Eskeland & Axel Imhof
  2. Abteilung Molekulare Naturstoff-Forschung, Leibniz-Institut für Naturstoff-Forschung und Infektionsbiologie–Hans-Knöll-Institut für Naturstoff-Forschung, Beutenbergstrasse 11a, Jena, 07745, Germany
    Ernst Roemer

Authors

  1. Dorothea Greiner
    You can also search for this author inPubMed Google Scholar
  2. Tiziana Bonaldi
    You can also search for this author inPubMed Google Scholar
  3. Ragnhild Eskeland
    You can also search for this author inPubMed Google Scholar
  4. Ernst Roemer
    You can also search for this author inPubMed Google Scholar
  5. Axel Imhof
    You can also search for this author inPubMed Google Scholar

Corresponding author

Correspondence toAxel Imhof.

Ethics declarations

Competing interests

The authors declare no competing financial interests.

Supplementary information

Rights and permissions

About this article

Cite this article

Greiner, D., Bonaldi, T., Eskeland, R. et al. Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9.Nat Chem Biol 1, 143–145 (2005). https://doi.org/10.1038/nchembio721

Download citation

This article is cited by