VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor grow
Author: ["Elizabeth A Harrington","David Bebbington","Jeff Moore","Richele K Rasmussen","Abi O Ajose-Adeogun","Tomoko Nakayama","Joanne A Graham","Cecile Demur","Thierry Hercend","Anita Diu-Hercend","Michael Su","Julian M C Golec","Karen M Miller"]
Publication: Nature Medicine
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Abstract
The Aurora kinases are essential for the regulation of chromosome segregation and cytokinesis during mitosis. Aberrant expression and activity of these kinases occur in a wide range of human tumors, and lead to aneuploidy and tumorigenesis. Here we report the discovery of a highly potent and selective small-molecule inhibitor of Aurora kinases, VX-680, that blocks cell-cycle progression and induces apoptosis in a diverse range of human tumor types. This compound causes profound inhibition of tumor growth in a variety of in vivo xenograft models, leading to regression of leukemia, colon and pancreatic tumors at well-tolerated doses. Our data indicate that Aurora kinase inhibition provides a new approach for the treatment of multiple human malignancies.
Cite this article
Harrington, E., Bebbington, D., Moore, J. et al. VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat Med 10, 262–267 (2004). https://doi.org/10.1038/nm1003
