Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9
Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9
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DOI：
10.1038/nchembio721
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发表时间：
2005-08-01
影响因子：
14.8
通讯作者：
Imhof, A
中科院分区：
文献类型：
--
作者：
Greiner, D;Bonaldi, T;Imhof, A
组蛋白甲基化在细胞分化和胚胎发育过程中建立和维持稳定的基因表达模式方面起着关键作用。在此，我们报道了真菌代谢产物毛壳菌素作为第一种赖氨酸特异性组蛋白甲基转移酶抑制剂的特性。毛壳菌素在体外和体内对甲基转移酶SU(VAR)3 - 9均具有特异性，因此可用于研究异染色质介导的基因抑制。
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.