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. SET1, SET7/9, Ash1, ALL-1, MLL, ALR, Trx, and SMYD3 are histone methyltransferases that catalyze methylation of histone H3 at lysine 4 (H3-K4) in mammalian cells. H3-K4 monomethylation is associated with silenced euchromatin regions in the genome and may serve as a epigenetic mark and function in gene repression. The H3-K4 mono-methylation can be also changed by inhibition or activation of HMTs. Thus quantitative detectionof mono-methyl histone H3-K4 would provide useful inform
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