Abstract: Cancer is now one of the leading causes of mortality that has become a serious threat to public health. The applications of nanostructures in cancer diagnosis and therapy show promising prospects. Graphene oxide (GO), which is a novel one-atom-thick two-dimensional carbon network containing carboxylic acid groups at the sheet edges and hydroxyl and epoxy groups on the graphitic plane, has received considerable attention due to its excellent physical and chemical properties, and potential applications in multidisciplinary. Herein, the applications of GO as a novel nano-theranostic agent in cancer research are reviewed.