Aurora A Kinase Is a Priority Pharmaceutical Target for the Treatment of Cancers

被引:86
作者
Damodaran, Arun Prasath [1 ,2 ]
Vaufrey, Lucie [1 ,2 ]
Gavard, Olivia [1 ,2 ]
Prigent, Claude [1 ,2 ]
机构
[1] CNRS, UMR 6290, Equipe Labellisee Ligue Canc 2014 2016, F-35000 Rennes, France
[2] Univ Rennes 1, Inst Genet & Dev Rennes, F-35000 Rennes, France
关键词
SQUAMOUS-CELL CARCINOMA; AURORA/IP11-RELATED PROTEIN-KINASE; CAENORHABDITIS-ELEGANS EMBRYOS; LAEVIS OOCYTE MATURATION; SMALL-MOLECULE INHIBITOR; HUMAN BREAST-CANCER; A KINASE; PANCREATIC-CANCER; SPINDLE ORIENTATION; SELF-RENEWAL;
D O I
10.1016/j.tips.2017.05.003
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Aurora kinases control multiple events during cell cycle progression and are essential for mitotic and meiotic bipolar spindle assembly and function. There are three Aurora kinases in mammals, some of which have oncogenic properties and all of which are overexpressed in multiple cancers. Pharmaceutical companies quickly made these kinases priority targets for the development of inhibitors to be used as cancer treatments. In this review, we focus on Aurora A, against which several inhibiting compounds have been discovered and made available; however, even though some of these compounds underwent clinical trials, none have yet gone beyond Phase III trials. The varying efficiencies and particularities of these drugs raise several questions that are explored in this review: is Aurora A even a good target? What biomarkers can we use to measure its activity in vivo? How can we improve the Aurora A-inhibiting drugs?
引用
收藏
页码:687 / 700
页数:14
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