title: Aurora-A kinase inhibitor scaffolds and binding modes.
abstract: 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.
authors.affiliation: State Key Laboratory of Chemical Resource Engineering, Department of Pharmaceutical Engineering, PO Box 53, Beijing University of Chemical Technology, 15 BeiSanHuan East Road, Beijing 100029, China.
authors.forename: Aixia
authors.initials: A
authors.lastname: Yan
authors.forename: Liyu
authors.initials: L
authors.lastname: Wang
authors.forename: Shuyu
authors.initials: S
authors.lastname: Xu
authors.forename: Jun
authors.initials: J
authors.lastname: Xu
mesh_terms: D000818:Animals; D064127:Aurora Kinases; D001665:Binding Sites; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000503:physiopathology; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*
chemical_list: D047428:Protein Kinase Inhibitors; D064127:Aurora Kinases; D017346:Protein Serine-Threonine Kinases