Summary: Epigenetic activation or inactivation of genes plays a critical role in many important human diseases, especially in cancer. A major mechanism for epigenetic inactivation of the genes is methylation of CpG islands in genome DNA caused by DNA methyltransferases. Histone methyltransferases (HMTs) control or regulate DNA methylation through chromatin-dependent transcription repression or activation. HMTs transfer 1-3 methyl groups from S-adenosyl-L-methionine to the lysine and arginine residues of histone proteins. G9a and polycomb group enzymes such as EZH2 are histone methyltransferases that catalyze methylation of histone H3 at lysine 27 (H3-K27) in mammalian cells. Histone H3-K27 monomethylation, a modification enriched at pericentromeric heterochromatin, was observed to be broadly distributed throughout all euchromatic sites and participates in silencing gene expression. Increased H3-K27 methylation is also found to be involved in some pathological processes such as cancer progressio
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