Acetylation of histones epigenetically mediates transcriptional dynamics of gene activation and suppression in response to physiological regulatory signals. The acetylated states of histone proteins define the activities of gene promoter and enhancer elements by contributing to competency for regulatory protein interactions and control of chromatin organization including higher-order inter and intra-chromosomal interactions. Cell transformation and tumor progression are associated with and functionally related to histone acetylation. Targeting the regulatory machinery for histone acetylation provides treatment options for cancer-compromised gene expression with specificity and reduced off-target consequences.