Aurora-A kinase inhibitor scaffolds and binding modes

被引：47
|
作者：
Yan, Aixia [1 ]
Wang, Liyu [1 ]
Xu, Shuyu [1 ]
Xu, Jun [2 ]
机构：
[1] Beijing Univ Chem Technol, Dept Pharmaceut Engn, State Key Lab Chem Resource Engn, Beijing 100029, Peoples R China
[2] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China
来源：
DRUG DISCOVERY TODAY | 2011年 / 16卷 / 5-6期
基金：
中国国家自然科学基金;
关键词：
CHROMOSOMAL PASSENGER PROTEIN; SMALL-MOLECULE INHIBITOR; STRUCTURAL BASIS; POTENT; IDENTIFICATION; DISCOVERY; MLN8054; VX-680; CANCER; SAR;
D O I：
10.1016/j.drudis.2010.12.003
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
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.
引用
收藏
页码：260 / 269
页数：10
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