Malignant cells are characterized by the accumulation of genetic alterations, which result in the disregulation of signal transduction pathways that control proliferation, differentiation and apoptosis. The identification of the molecular components involved in these aberrant processes is necessary for the development of chemotherapeutic interventions to restore or selectively destroy the transformed cells. Discovery of new chemotherapeutic agents is probably one of the most reliable ways to improve our success against cancer, and intelligent drug design is a key factor to achieve this goal. Thus, the identification of novel targets for anticancer drug discovery is needed. This review provides evidence to support choline kinase as one such target.