Characterization of a highly selective inhibitor of the Aurora kinases. Issue 18 (15th September 2017) - Ferguson, Fleur M.
Graphical abstract: Abstract: Aurora kinases play an essential role in mitosis and cell cycle regulation. In recent years Aurora kinases have proved popular cancer targets and many inhibitors have been developed. The majority of these clinical candidates are multi-targeted, rendering them inappropriate as tools for studying Aurora kinase mediated signaling. Here we report discovery of a highly selective inhibitor of Aurora kinases A, B and C, with potent cellular activity and minimal off-target activity (PLK4). The X-ray co-crystal structure of Aurora A in complex with compound2 is reported, and provides insights into the structural determinants of ligand binding and selectivity.