Introduction of Epigenetic Targets in Drug Discovery and Current Status of Epi-Drugs and Epi-Probes

In this chapter we provide an overview of epigenetics and epigenomics and their contribution to understand their participation in disease. It is acknowledged that this is a promising research area for the treatment of cancer and the increasing list of diseases with a proven or suggested etiopathogenic component of epigenetics. In the context of recent progress in understanding epigenetic targets and mechanisms involved in disease initiation and progression, this chapter discusses the current status of epi-drugs, including the ones already approved for cancer treatment. The increasing awareness of the high complexity of the epigenetic machinery has prompted the need to develop selective compounds toward different targets. Thus, progress and current status of epi-probes are also addressed in this chapter. Finally, major challenges and potential solutions to further advance epigenetics/epigenomics to improve health are discussed.