The past decade has seen tremendous growth in our understanding of epigenetics and chromatin remodeling. Small, organic molecule modulators of a number of chromatin modifying proteins (CMPs) have been reported over this time frame and several of these have advanced to human clinical trials. In this Viewpoint, I summarize the current state of medicinal chemistry efforts focused on epigenetic targets and attempt to provide some insight into future directions on which the community may wish to focus.
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