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Journal Article

Discovery of selective aminothiazole aurora kinase inhibitors


Musacchio,  Andrea
Abt. I:Mechanistische Zellbiologie, Max Planck Institute of Molecular Physiology, Max Planck Society;

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Andersen, C. B., Wan, Y., Chang, J. W., Riggs, B., Lee, C., Liu, Y., et al. (2008). Discovery of selective aminothiazole aurora kinase inhibitors. ACS CHEMICAL BIOLOGY, 3(3), 180-192. doi:10.1021/cb700200w.

Cite as: https://hdl.handle.net/11858/00-001M-0000-0015-3AF2-F
Aurora family kinases regulate important events during mitosis including centrosome maturation and separation, mitotic spindle assembly, and chromosome segregation. Misregulation of Aurora kinases due to genetic amplification and protein overexpression results in aneuploidy and may contribute to tumorigenesis. Here we report the discovery of new small molecule aminothiazole inhibitors of Aurora kinases with exceptional kinase selectivity and report a 1.7 angstrom cocrystal structure with the Aurora B:INCENP complex from Xenopus laevis. The compounds recapitulate the hallmarks of Aurora kinase inhibition, including decreased histone H3 serine 10 phosphorylation, failure to complete cytokinesis, and endoreduplication.