Epigenetic control is essential for development and differentiation, and this control mechanism is very frequently deregulated in cancer. Several small molecule inhibitors have been developed in recent years that have either been approved for clinical use or are in preclinical and clinical trials. This conference will focus on basic and clinical aspects of targeting a broad panel of epigenetic proteins in cancer, either as monotherapies, or as combination therapies, including the use of immune checkpoint inhibitors to increase drug sensitivity and overcome chemoresistance. Topics to be covered include epigenetic regulation in cancer development and maintenance, novel epigenetic targets, drug resistance, combination therapies, and applications in clinical trials.