Aurora-A kinase inhibitor scaffolds and binding modes

Aixia Yan; Liyu Wang; Shuyu Xu; Jun Xu

doi:10.1016/j.drudis.2010.12.003

Aurora-A kinase inhibitor scaffolds and binding modes

Drug Discov Today. 2011 Mar;16(5-6):260-9. doi: 10.1016/j.drudis.2010.12.003. Epub 2010 Dec 13.

Authors

Aixia Yan¹, Liyu Wang, Shuyu Xu, Jun Xu

Affiliation

¹ 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.

PMID: 21147253
DOI: 10.1016/j.drudis.2010.12.003

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.

Publication types

Research Support, Non-U.S. Gov't
Review

MeSH terms

Animals
Aurora Kinases
Binding Sites
Drug Delivery Systems*
Drug Design
Humans
Neoplasms / drug therapy
Neoplasms / physiopathology
Protein Binding
Protein Kinase Inhibitors / pharmacology*
Protein Serine-Threonine Kinases / antagonists & inhibitors*

Substances

Protein Kinase Inhibitors
Aurora Kinases
Protein Serine-Threonine Kinases