Characterization of EHop-016, a novel small molecule inhibitor of Rac GTPase*
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چکیده
Background: Rac is a central regulator of cancer cell migration/invasion and metastasis. Results: EHop-016 inhibits Rac activity with an IC of 1 M. EHop-016 blocks Rac interaction with the upstream effector Vav2, and inhibits downstream PAK activity, lamellipodia extension, and cell migration. Conclusion: EHop-016 is an effective Rac inhibitor. Significance: EHop-016 has potential as a metastasis therapeutic and for investigations of Rac-regulated cellular responses.
منابع مشابه
Characterization of EHop-016, novel small molecule inhibitor of Rac GTPase.
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 strateg...
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تاریخ انتشار 2012