Nature Chemical Biology 2005-08-01

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

Dorothea Greiner, Tiziana Bonaldi, Ragnhild Eskeland, Ernst Roemer, Axel Imhof

Index: Nat. Chem. Biol. 1 , 143, (2005)

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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.