Histone Methyltransferase
Histone methyltransferases (HMT) are histone-modifying enzymes), that catalyze the transfer of one, two, or three methyl groups to lysine and arginine residues of histone proteins. Methylation of histones is important biologically because it is the principal epigenetic modification of chromatin that determines gene expression, genomic stability, stem cell maturation, cell lineage development, genetic imprinting, DNA methylation, and cell mitosis.
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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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UNC1999一种有效的具有口服活性的EZH1、EZH2选择性抑制剂，其IC50分别为2 nM和45 nM，对很多表观遗传学相关或不相关的靶点选择性大于1000倍。
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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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EPZ004777是高活性DOT1L抑制剂，IC50为0.4 nM。
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EPZ5676是蛋白甲基转移酶DOT1L的S-腺苷甲硫氨酸(SAM)竞争性抑制剂，Ki为80 pM，比作用于所有其他PMTs选择性高37，000以上，抑制肿瘤H3K79甲基化。
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