Mitochondrial functions are altered in many human diseases including cancer. 
Development of mitochondria-targeted therapies, either through restoring normal 
mitochondrial function or promoting mitochondrial-induced cell death, is one of 
the attractive strategies to improve the outcome of cancer treatment. Recent 
advances have revealed the important functional involvement of mitochondrial 
dynamics in cancer biology. Dynamin-related protein 1 (Drp1), a member of the 
dynamin family of GTPases required for mitochondrial fission, has been found 
upregulated in certain types of cancers, such as lung and breast cancers. In 
addition, the roles of Drp1 in cell cycle progression, genome instability, cell 
migration and apoptosis in cancer cells have also been recently uncovered. These 
findings raise the possibility of targeting Drp1-mediated mitochondrial fission 
as an effective therapy for treating cancer. This article explores the function 
of Drp1 in cancer cells and discusses the theoretical basis for the development 
of potential targeted therapy.