[HTML][HTML] Characterization of EHop-016, novel small molecule inhibitor of Rac GTPase
BL Montalvo-Ortiz, L Castillo-Pichardo… - Journal of Biological …, 2012 - ASBMB
The Rho GTPase Rac regulates actin cytoskeleton reorganization to form cell surface
extensions (lamellipodia) required for cell migration/invasion during cancer metastasis. Rac
hyperactivation and overexpression are associated with aggressive cancers; thus,
interference of the interaction of Rac with its direct upstream activators, guanine nucleotide
exchange factors (GEFs), is a viable strategy for inhibiting Rac activity. We synthesized
EHop-016, a novel inhibitor of Rac activity, based on the structure of the established …
extensions (lamellipodia) required for cell migration/invasion during cancer metastasis. Rac
hyperactivation and overexpression are associated with aggressive cancers; thus,
interference of the interaction of Rac with its direct upstream activators, guanine nucleotide
exchange factors (GEFs), is a viable strategy for inhibiting Rac activity. We synthesized
EHop-016, a novel inhibitor of Rac activity, based on the structure of the established …