Cell migration to participate in the organization form, embryonic development, inflammation, wound healing, such as a variety of physiological and pathological process of atherosclerosis, and throughout the whole process of tumor metastasis. Cell migration to extracellular and intracellular signaling molecules regulate cytoskeleton power unit for driving force, and actin cytoskeleton mediated adhesion between anchorage force provided by the coordinated operation. Small molecule Ras homologue (Rho) protein is to change the cytoskeleton assembly, regulation of cell migration and then the key factors of the involved in tumor metastasis. Rho GTPase played a key role in regulating tumor cell functions, including cell malignant transformation and migration. Members of the family of the reorganization of actin in regulating cell, mobile, cells and cells and cells and extracellular matrix adhesion, cell cycle, gene expression and apoptosis also play an important role in the process, in which each function in cancer occurrence and development are extremely important. Rho GTPase also can increase the susceptibility of cell DNA damage, including antineoplastic drugs and ionizing radiation, the Rho GTPase regulation can influence the effect of the traditional antineoplastic therapy and/or side effects, with Rho GTPase as the target, choose efficient specific Rho GTPase inhibitors can significantly increase the effect of anti-tumor therapy.