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The mechanism by which genetic expression is modified and regulated is of a main interest in the field of epigenetics. It involves various chromatin-modifying and associated proteins, often referred to as “writers”, “readers” and “erasers”, capable of establishing different modification groups (e.g. methyl, acetyl) on histone residues and consequently recruiting various transcription factors in order to further shape the gene expression. Naturally, a strict regulation of the activity of these proteins is necessary for normal cell functioning. Often it is the deregulation of writers, readers and erasers that leads to aberrant gene transcription and cancer. For that reason revealing the epigenetic mechanisms of cancer at molecular level is essential for understanding the initiation and progression of the disease. In addition, aberrant expression of histone modifying proteins can serve as a direct biomarker of certain types of cancer and an indicator of a proper diagnosis. Identifying the cause of gene deregulation also allows for further development of drugs that can target the cause and eliminate it. A novel concept in the fields of cancer research and epigenetics are the epi-drugs – natural or synthetic inhibitors of certain histone modifying enzymes, which are currently considered as potent candidates for anti-cancer therapeutics. The present review aims to introduce the concept of epigenetics, describe its main players, and reveal the possible application of epi-inhibitors in the field of cancer treatment.