Optimization of Enzyme Reactions for Screening and Profiling Wild Type EZH2 with the Transcreener EPIGEN Methyltransferase Assay

Post translational modification of histone proteins by Histone Methyltransferases plays an important role in gene regulation. Misregulation of these enzymes has been implicated in initiation and progression of several diseases, including cancer. EZH2 is the catalytic component of the polycomb group repressive Complex (PRC2), that selectively methylates histone H3 lysine 27 (H3K27). Numerous studies have shown that EZH2 is overexpressed in prostate, breast, bladder, brain, and other tumor types and is recognized as a molecular marker for cancer progression and aggressiveness. This poster describes the development, optimization and validation of Transcreener EPIGEN Methyltransferase assay for EZH2. To aid in drug discovery Bellbrook Labs developed an EZH2 Transzyme Methyltransferase Assay kit which contains enzyme, substrate and the Epigen Methyltransferase kit.