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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.

DOI:10.1038/nchembio721
PMID:16408017
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.

摘要

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。

相似文献

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Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9.组蛋白甲基转移酶SU(VAR)3-9特异性抑制剂的鉴定。
Nat Chem Biol. 2005 Aug;1(3):143-5. doi: 10.1038/nchembio721. Epub 2005 Jul 17.
2
Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases.Chaetocin是组蛋白赖氨酸甲基转移酶的非特异性抑制剂。
Nat Chem Biol. 2013 Mar;9(3):136-7. doi: 10.1038/nchembio.1187.
3
Reply to "Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases".对《Chaetocin是组蛋白赖氨酸甲基转移酶的非特异性抑制剂》的回复
Nat Chem Biol. 2013 Mar;9(3):137. doi: 10.1038/nchembio.1188.
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The N-terminus of Drosophila SU(VAR)3-9 mediates dimerization and regulates its methyltransferase activity.果蝇SU(VAR)3-9的N端介导二聚化并调节其甲基转移酶活性。
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Regulation of chromatin structure by site-specific histone H3 methyltransferases.位点特异性组蛋白H3甲基转移酶对染色质结构的调控
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Heterochromatin formation in Drosophila is initiated through active removal of H3K4 methylation by the LSD1 homolog SU(VAR)3-3.果蝇中异染色质的形成是通过LSD1同源物SU(VAR)3-3主动去除H3K4甲基化来启动的。
Mol Cell. 2007 Apr 13;26(1):103-15. doi: 10.1016/j.molcel.2007.02.025.
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The evolution of the histone methyltransferase gene Su(var)3-9 in metazoans includes a fusion with and a re-fission from a functionally unrelated gene.后生动物中组蛋白甲基转移酶基因Su(var)3-9的进化包括与一个功能不相关基因的融合及再次分裂。
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Saccharomyces cerevisiae Set1p is a methyltransferase specific for lysine 4 of histone H3 and is required for efficient gene expression.酿酒酵母Set1p是一种特异性作用于组蛋白H3赖氨酸4位点的甲基转移酶,是高效基因表达所必需的。
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