Epigenetic modulators from “The Big Blue”: A treasure to fight against cancer

• Deregulation of the epigenetic machinery is a hallmark of cancer.
• Natural marine compounds possess epigenetic modulatory activities.
• Natural marine compounds provide potent anti-cancer drugs.
• Epigenetic activity of largazole, psammaplin, trichostatin, azumamide are described.

Cancer remains a major public health problem in our society. The development of potent novel anti-cancer drugs selective for tumor cells is therefore still required. Deregulation of the epigenetic machinery including DNA methylation, histone modifications and non-coding RNAs is a hallmark of cancer, which provides potential new therapeutic targets. Natural products or their derivatives represent a major class of anti-cancer drugs in the arsenal available to the clinician. However, regarding epigenetically active anti-cancer agents for clinics, the oceans represent a largely untapped resource. This review focuses on marine natural compounds with epigenetic activities and their synthetic derivatives displaying anti-cancer properties including largazole, psammaplins, trichostatins and azumamides.