Targeting Rho GTPase signaling for cancer therapy

Future Oncology
Katerina MardilovichMark Baugh

Abstract

Accumulating evidence from basic and clinical studies supports the concept that signaling pathways downstream of Rho GTPases play important roles in tumor development and progression. As a result, there has been considerable interest in the possibility that specific proteins in these signal transduction pathways could be potential targets for cancer therapy. A number of inhibitors targeting critical effector proteins, activators or the Rho GTPases themselves, have been developed. We will review the strategies currently being used to develop inhibitors of Rho GTPases and downstream signaling kinases and discuss candidate entities. Although molecularly targeted drugs that inhibit Rho GTPase signaling have not yet been widely adopted for clinical use, their potential value as cancer therapeutics continues to drive considerable pharmaceutical research and development.

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Methods Mentioned

BETA
GTPase
GTPases
nucleotide exchange
nucleotide
two-hybrid
flow
surface plasmon resonance
xenograft
x-ray crystallography

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