Cisbio, BioTek Instruments
The study of epigenetic mechanisms affecting a wide range of cellular process has seen dramatic growth over the past several years. Methyltransferases (MTs) have proven to target a wide variety of substrates including histones, oligonucleosomes, DNA, RNA, small molecules and receptors. Many of these are potential therapeutic targets and are heavily investigated in both fundamental research as well as drug discovery efforts. Given the ubiquitous and diverse nature of both enzyme and substrate an easy to use, universal assay method suitable for highthroughput screening (HTS) is highly desirable. MTs catalyze the transfer of a donor methyl group to amino groups on the target molecule such as nitrogenous DNA bases or peptide N-termini and amino acid side chains. The cofactor S-adenosylL-methionine (SAM) is the primary methyl donor providing a reactive methyl group bound to sulfur. The conversion of SAM to S-adenosylL-homocysteine (SAH) can then be used as a measurement of MT activity.