组蛋白甲基转移酶SU(VAR)3-9特异性抑制剂的鉴定。
Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9.
作者信息
Greiner Dorothea, Bonaldi Tiziana, Eskeland Ragnhild, Roemer Ernst, Imhof Axel
机构信息
Adolf Butenandt Institute, Department of Molecular Biology, Histone Modifications Group, Ludwig-Maximillians University of Munich, Schillerstr. 44, 80336 Munich, Germany.
出版信息
Nat Chem Biol. 2005 Aug;1(3):143-5. doi: 10.1038/nchembio721. Epub 2005 Jul 17.
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.
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发挥着关键作用。在此，我们报道了真菌代谢产物杀 chaetocin 的特性，它是赖氨酸特异性组蛋白甲基转移酶的首个抑制剂。Chaetocin 在体外和体内对甲基转移酶 SU(VAR)3-9 具有特异性，因此可用于研究异染色质介导的基因抑制。
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