Epigenetic modulators of DNA methylation

DNA Methylation is a common epigenetic signaling tool that is is used to control gene expression in eukaryotes. DNA methyltransferase enzymes (DNMTs) catalyze the transfer of a methyl group from S-adenosyl methionine to the 5'-position of cytosines. In mammalian cells, DNA methylation is generally associated with gene silencing and effects numerous cellular processes, including embryonic development, genomic imprinting, X-chromosome inactivation and preservation of chromosome stability. Hypermethylation of the promoters of tumor suppressor genes often occur in certain types of cancers.

Active Motif offers several small molecules that can be used to modify DNA methylation levels. Some molecules act as chemical analogs for the nucleoside cytidine that, when incorporated into growing DNA strands, will inhibit the DNMT enzymes that normally methylated DNA. Other compounds act as non-nucleoside DNA methylation inhibitors.