CHAPTER 10: Fragment-Based Approaches to Epigenetic Targets

Drugs that target aberrant epigenetic states of disease offer the prospect for long-lasting and effective treatments through the control of multiple genes. Although the proteins and mechanisms responsible for epigenetic regulation are becoming better understood, these processes are highly complex, and there is a great need for high-quality small-molecule probes to unravel their biology. This chapter focuses on the so-called histone code, the modules that read it, and the enzymes that control it. It describes recent case studies, discusses the challenges remaining and outlines the prospects for the future of fragment-based drug discovery in this rapidly evolving area of biology.