Enniatins are mycotoxins produced by pathogenic Fusarium fungi and are commonly found contaminants of cereal grains, animal feeds, and food commodities. Due to their remarkable resistance against heat, acid and digestion, they can propagate through food and feed chains. This group of molecules is therefore of increasing concern for human and animal health at chronic exposure. However, at the same time, enniatins have come to attention as potential anticancer agents due to their specific cytotoxic properties against malignant cells. Enniatins are well known for their ionophoric behaviour by which they exert antibacterial, antifungal, antihelmintic and antiviral activity. The same behaviour is considered to be responsible for the primary mechanism of toxicity against cancer cells, which disturbs the physiological homeostasis by transporting cations through cell membranes leading to apoptotic cell death. Since enniatins can be conveniently derivatized using the concept of hybrid modular non-ribosomal peptide synthetases, they present a promising class of anticancer agents that need to be explored in terms of their detailed molecular mechanism of action. Figure . A: Chemical structure of enniatin B with hydroxyvaleric acid and Lvaline units highlighted in red and blue, respectively. B, C: Schematic representations of EBn:M z+ 1:1 and 2:1 "sandwich" complex. The metal ion, amide and ester carbonyl oxygen atoms are depicted in grey, red and blue, respectively.