Ras and Rho GTPases are among the best studied signaling molecules in molecular biology. Essential cellular processes, such as cell growth, lipid metabolism, cytoarchitecture, membrane trafficking, transcriptional regulation, apoptosis, and response to genotoxic agents, are directly modulated by different members of this superfamily of proteins. Not until recently have we begun to understand the physiological implications of Ras and Rho GTPases, linking them to processes such as embryonic development, tissue remodeling, tumorigenesis and metastasis. In this sense, uncontrolled activation, due to overexpression of different members of the Rho family in a variety of tissues, leads to uncontrolled proliferation and invasiveness of human tumors. In this review, an attempt to briefly integrate recent findings in transcriptional regulation by Rho GTPases in the context of carcinogenesis and metastasis as well as apoptosis is made.