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Epigenetic processes, such as DNA methylation and histone acetylation, regulate the genome-environment interactions that may play important roles in a wide range of brain disorders, including Alzheimer’s disease (AD). Indeed, the role of epigenetic machinery in learning and memory processes is well documented. In this review, we will focus on the most recent literature on tools that target epigenetic mechanisms, particularly on histone acetylation, and we will discuss the use of chemical probes to validate these targets in therapeutic strategies for AD.