DNA Methyltransferase
DNA methyltransferase (DNA MTase) family of enzymes catalyze the transfer of a methyl group to DNA. DNA methylation serves a wide variety of biological functions. All the known DNA methyltransferases use S-adenosyl methionine (SAM) as the methyl donor. Three active DNA methyltransferases have been identified in mammals. They are named DNMT1, DNMT3A, and DNMT3B. A fourth enzyme previously known as DNMT2 is not a DNA methyltransferase.
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Decitabine是一种有效的DNA甲基化抑制剂,作用于HL-60和KG1a细胞时,IC50分别为100 ng/mL和1 ng/mL。
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Zebularine(NSC309132; 4-Deoxyuridine)是DNA甲基化抑制剂,能与DNA甲基化酶共价结合,也能抑制Cytidinedeaminase酶活性,Ki值为2uM。
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SGI-1027是DNA甲基转移酶(DNMT)抑制剂,对DNMT1,DNMT3A和DNMT3B的IC50分别为6,8和7.5 μM。
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RG108是非核苷类DNA甲基转移酶抑制剂,IC50为115 nM。
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Azacitidine 是胞苷的核苷类似物,通过捕获DNA甲基,特异性抑制DNA methylation(DNA甲基化)。
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