Methyltransferases use S-adenosyl-L-methionine (SAM) to deposit methyl marks. Many of these epigenetic ‘writers’ are associated with gene regulation. As cancer etiology is highly correlated with misregulated methylation patterns, methyltransferases are emerging therapeutic targets. Successful assignment of methyltransferases’ roles within intricate biological networks relies on 1) the access to enzyme mechanistic insights and 2) the efficient screening of chemical probes against these targets.
