Chapter 2: Assay Development and Screening Strategies for Epigenetic Targets

The field of epigenetics has grown substantially in the last 20 years with the discovery of novel post-translational modifications (PTMs) and the expansion of substrates beyond chromatin. This growth has been matched by an increase in the sensitivity and diversity of in vitro and cellular assays which has enabled the rapid identification of tool compounds and characterization of their effects in cellular systems to further facilitate drug discovery. This chapter aims to introduce the newcomer to epigenetics to the screening strategies and assay formats commonly used for epigenetic targets.