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.
Drug Discov Today. 2011 Mar;16(5-6):260-9. doi: 10.1016/j.drudis.2010.12.003. Epub 2010 Dec 13.
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.
极光激酶（A-C）属于丝氨酸/苏氨酸蛋白激酶家族。近年来，在癌细胞和癌基因转染细胞中发现极光激酶的组成型或升高表达。在这篇综述中，我们总结了极光 A 激酶抑制剂的常见结合模式、结合位点的热点残基和优势抑制剂结构。我们对报道的极光 A 激酶抑制剂的化学骨架及其结合模式的综述，可以为抑制剂的新设计策略的评估或开发提供一个有用的框架。
