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?

Aurora激酶控制细胞周期进程中的多个事件，对于有丝分裂和减数分裂双极纺锤体的组装和功能至关重要。哺乳动物中存在三种Aurora激酶，其中一些具有致癌特性，并且在多种癌症中均过表达。制药公司迅速将这些激酶确定为开发用于癌症治疗的抑制剂的优先目标。在这篇综述中，我们集中于Aurora A，针对它发现了几种抑制性化合物并使其可用。但是，即使其中一些化合物已进行了临床试验，但都没有超出III期试验范围。这些药物的不同效率和特殊性引起了本综述中探讨的几个问题：Aurora A甚至是一个不错的目标吗？我们可以使用哪些生物标志物来衡量其活性体内？我们如何改善抑制Aurora A的药物？