Inhibitors Of Rho Signaling

Inhibitors Of Rho Signaling

Background Cancer metastasis is a significant medical problem in the US, where it is estimated ~ 90% of cancer deaths in 2003 were a result of metastatic tumors. Several reports suggest a potential role for the small GTPase, Rho, in metastasizing cancers. Rho signaling plays an important role in cancer cell proliferation. Inhibition of this pathway may lead to a better understanding of the pathways underlying metastasis and compounds targeted to decrease tumor metastasis.

Technology Description University of Michigan researchers utilized a cell-based high-throughput screening luciferase assay to identify small molecule inhibitors of the Rho-stimulated gene transcription in mammalian cells. Two structurally related active compounds, CCG977 and CCG1423, were identified with low micromolar IC50 values. They were further tested and found to also inhibit LPA (G-protein coupled receptor) receptor-stimulated cancer cell DNA synthesis at similar concentrations. Currently, characterization of these two compounds and their signaling pathway interactions is underway.

Applications
¥ Targeted disruption of cancer metastasis.
¥ Research tool to study the metastaticRho signaling pathways.

Advantages
¥ Novel compound that specifically inhibitRho-stimulated signaling.

Inventor(s): Richard Neubig, Chris Evelyn

Type of Offer: Licensing

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Inhibitors Of Rho Signaling