IMPORTANCE OF THE FIELD: Rho GDP dissociation inhibitor 2 (RhoGDI2) has been 
identified as a regulator of Rho GTPases that play important roles in the 
development of numerous aspects of the malignant phenotype, including cell cycle 
progression, resistance to apoptotic stimuli, neovascularization, tumor cell 
motility, invasiveness, and metastasis. Although RhoGDI2 has been known to be 
expressed only in hematopoietic tissues, recent studies suggest that this 
protein is also aberrantly expressed in several human cancers and contributes to 
aggressive phenotypes, such as invasion and metastasis. Hence, RhoGDI2 appears 
to be a target of interest for therapeutic manipulation.
AREAS COVERED IN THIS REVIEW: Here, we summarize the role of RhoGDI2 in human 
cancers, specifically metastasis-related processes, and discuss its potential as 
a therapeutic target.
WHAT THE READER WILL GAIN: RhoGDI2 modulates the invasiveness and metastatic 
ability of cancer cells through regulation of Rac1 activity.
TAKE HOME MESSAGE: RhoGDI2 may be a useful marker for tumor progression in human 
cancers, and interruption of the RhoGDI2-mediated cancer cell invasion and 
metastasis by an interfacial inhibitor may be a powerful therapeutic approach to 
cancer.