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

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.

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Figure 1: In vitro inhibition of dSU(VAR)3-9.
Figure 2: In vivo inhibition of SU(VAR)3-9.

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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.

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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

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  1. Dorothea Greiner
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  2. Tiziana Bonaldi
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  3. Ragnhild Eskeland
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  4. Ernst Roemer
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Correspondence to Axel Imhof.

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The authors declare no competing financial interests.

Supplementary information

Supplementary Fig. 1

Chaetocin assays. (PDF 446 kb)

Supplementary Fig. 2

Chemical characterization of chaetocin. (PDF 561 kb)

Supplementary Fig. 3

Effect of chaetocin on tissue culture cells. (PDF 405 kb)

Supplementary Methods (PDF 64 kb)

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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

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