Aurora激酶是一类在细胞周期调控中具有重要作用的丝/苏氨酸蛋白激酶,包括三个成员:AuroraA、B、C。Aurora激酶在大多数肿瘤中均高表达,其异常调控与肿瘤的发生发展密切相关。近年来,Aurora激酶抑制剂作为抗肿瘤候选药物受到广泛的关注,已有一些进入临床试验,且表现出良好的抗肿瘤活性。本文围绕Aurora家族的三个成员,讨论了其在细胞有丝分裂过程中的生物学功能、与肿瘤发生发展的关系及其抑制剂的研究进展,指出其作为抗肿瘤药物靶点的潜在价值。
Aurora kinases, which are involved in the regulation of cell cycle, belong to serine/threonine subclass ofkinases. The three mammalian members, Aurora A, B and C, are strongly expressed in a broad range of cancer types and their aberrant regulations are involved in tumorigenesis. Recently, Aurora kinase inhibitors as antitumor drugs have been developed and a number of these novel agents are currently being studied in phase I and II clinical trials exhibiting a promising clinical efficacy. In this review, we discuss Aurora kinases' biological function in mitosis events,involvement in tumorigenesis and the development of their inhibitors and indicate Aurora kinases as potential anticancer targets.