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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Drosophila Proteins / antagonists & inhibitors
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Drosophila Proteins / genetics
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Histone Methyltransferases
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Histone-Lysine N-Methyltransferase / antagonists & inhibitors*
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Histone-Lysine N-Methyltransferase / classification
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Methyltransferases / antagonists & inhibitors*
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Molecular Structure
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Mycotoxins / pharmacology*
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Piperazines / pharmacology
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Poisons / pharmacology*
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Protein Methyltransferases
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Recombinant Proteins / antagonists & inhibitors
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Recombinant Proteins / genetics
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Substrate Specificity
Substances
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Drosophila Proteins
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Mycotoxins
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Piperazines
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Poisons
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Recombinant Proteins
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chaetocin
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Histone Methyltransferases
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Methyltransferases
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Protein Methyltransferases
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SU(VAR)3-9
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Histone-Lysine N-Methyltransferase