Monitor The Effect Of Histone Methylase And Demethylase Inhibitors That Induce Apoptosis In Cancer Cell Lines
By Brad Larson and Peter Banks, Applications Department, BioTek Instruments, Inc.
Histone lysine methylation is a reversible process, dynamically regulated by both lysine methyltransferases and demethylases. In general, methylation of histone H3 lysine 4 (H3K4me), H3K36, or H3K79 is associated with active transcription, whereas methylation of H3K9, H3K27, or H4K20 is associated with gene silencing.
EZH2 is a highly conserved histone methyltransferase that specifically targets H3K27 and functions as a transcriptional repressor1. Tissue microarray analysis of breast cancers identified consistent overexpression of EZH2, which was strongly associated with tumor aggressiveness. The compound DZNep has been shown to inhibit EZH2, decrease methylation of H3K27 and selectively induce apoptosis of cancer cell lines, including MCF-72.
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