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. Author manuscript; available in PMC: 2016 Jun 18.
Published in final edited form as: Expert Opin Drug Discov. 2015 Jun 18;10(9):991–1010. doi: 10.1517/17460441.2015.1058775

Figure 1. Biochemical model of the Rho GTPase regulatory mechanism.

Figure 1

Rho, Rac and Cdc42 cycle between an inactive GDP-bound and an active GTP-bound state. GEFs catalyze the GDP/GTP nucleotide exchange and activate the Rho GTPases, whereas GAPs enhance the intrinsic GTP-hydrolysis activity and inactivate them. GDIs can sequester Rho GTPases in the cytosol and prevent their activation. Activated Rho GTPases can interact with a variety of effector molecules to trigger downstream signaling events leading to diverse cellular responses.