Advances in the development of Rho GTPase inhibitors

[Display omitted] Rho guanosine triphosphatases (Rho GTPases), as members of the Ras superfamily, are GDP/GTP binding proteins that behave as molecular switches for the transduction of signals from external stimuli. Rho GTPases play essential roles in a number of cellular processes including cell cycle, cell polarity as well as cell migration. The dysregulations of Rho GTPases are related with various diseases, especially with cancers. Accumulating evidence supports that Rho GTPases play important roles in cancer development and progression. Rho GTPases become potential therapeutic targets for cancer therapy. And a number of inhibitors targeting Rho GTPases have been developed. In this review, we discuss their structural features, summarize their roles in cancer, and focus on the recent progress of their inhibitors, which are beneficial for the drug discovery targeting Rho GTPases.