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The recent search for new anti-cancer drugs focuses more on natural compounds from the regular human diet because these compounds rarely exhibit severe side-effects yet efficiently act on a wide range of molecular targets involved in carcinogenesis. One promising compound, which is now being tested in clinical studies, is the tomato-derived carotenoid lycopene. This review summarizes the current knowledge about the cellular action of lycopene and presents the molecular targets responsible for its remarkable chemopreventive and anti-proliferative activity. Its antioxidant effects include a considerable reactive oxygen species (ROS) scavenging activity, which allows lycopene to prevent lipid peroxidation and DNA damage. Simultaneously, lycopene induces enzymes of the cellular antioxidant defense systems by activating the antioxidant response element transcription system. As another chemopreventive …