Emerging Epigenetic Therapies in Neuroscience: Focus on Bromodomain-Containing Drug Targets

Failure to appropriately control gene expression is a salient feature of most human diseases. Therefore, the field of epigenetic therapeutics has rapidly grown into one of the most active areas of drug discovery. This is fueled by the fact that there exist hundreds of so-called druggable (by small molecules) epigenetic targets, many of which affect the state of chromatin and therefore gene expression. The result of this type of drug action, exemplified here by bromodomain inhibitors, is typically an alteration of the expression of a number of genes (up- as well as down-regulation). While some genes are more susceptible to this type of regulation, there is marked context dependency that represents both a challenge and an opportunity to drug hunters