Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Cancer

Ras homolog gene family member A (RHOA); leukemia-associated Rho guanine nucleotide exchange factor (LARG)

In vitro studies identified a small molecule inhibitor of the interaction between LARG and RHOA that could help treat cancers. In human fibroblasts, a compound designed to specifically block the RHOA binding site on LARG inhibited RHOA activity and disrupted actin cytoskeletal organization and adhesion. In human breast cancer cells, the compound inhibited growth, migration, invasion and mammary sphere formation at double-digit micromolar concentrations.
Next steps include identifying improved lead compounds for clinical testing.

SciBX 6(6); doi:10.1038/scibx.2013.135
Published online Feb. 14, 2013

Patent application filed; available for licensing

Shang, X. et al. Proc. Natl. Acad. Sci. USA; published online Feb. 4, 2013;
doi:10.1073/pnas.1212324110
Contact: Yi Zheng, Children's Hospital Medical Center, Cincinnati, Ohio
e-mail:

yi.zheng@cchmc.org