EZH2
EZH2 (Enhancer of zeste homolog 2) is a histone-lysine N-methyltransferase enzyme EZH2 that participates in DNA methylation and, ultimately, transcriptional repression. EZH2 catalyzes the addition of methyl groups to histone H3 at lysine 27, by using the cofactor S-adenosyl-L-methionine. Methylation activity of EZH2 facilitates heterochromatin formation thereby silences gene function. Remodeling of chromosomal heterochromatin by EZH2 is also required during cell mitosis. Mutation or over-expression of EZH2 has been linked to many forms of cancer.
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GSK126是一种高活性，S-腺苷-蛋氨酸竞争性EZH2甲基转移酶抑制剂，Ki为0.5 nM。
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EPZ-005687是EZH2选择性抑制剂，Ki为24 nM，比作用于EZH1选择性高50倍，对其它15种甲基转移酶有500倍的选择性。
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3-Deazaneplanocin A(DZNep)盐酸盐能抑制EZH2蛋白胞内增强子，具有抗肿瘤活性。
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GSK343是一种选择性EZH2抑制剂，IC50为4 nM，比作用于EZH1选择性高60倍，比作用于其他组蛋白甲基转移酶选择性高1000倍以上。
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