Aurora-A kinase inhibitor scaffolds and binding modes

Aurora kinases (A–C) belong to the serine/threonine protein kinase family. In recent years, the constitutive or elevated expression of Aurora kinases has been found in cancer cells and oncogene transfected cells. In this review, we summarize the common binding modes of Aurora-A kinase inhibitors, the hot spot residues in the binding sites and the privileged inhibitor structures. Our review of the reported chemical scaffolds of Aurora-A kinase inhibitors and their binding modes could provide a useful framework from which new design strategies for inhibitors might be assessed or developed.