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Updated: Aug 13, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9
Dorothea Greiner1, Tiziana Bonaldi, Ragnhild Eskeland
1Adolf Butenandt Institute, Department of Molecular Biology, Histone Modifications Group, Ludwig-Maximillians University of Munich, Schillerstr. 44, 80336 Munich, Germany.
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.

