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

D Greiner, T Bonaldi, R Eskeland, E Roemer… - Nature chemical …, 2005 - nature.com
D Greiner, T Bonaldi, R Eskeland, E Roemer, A Imhof
Nature chemical biology, 2005nature.com
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.
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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