Aurora 蛋白激酶抑制剂研究综述

Aurora蛋白激酶是一类在细胞增殖过程起重要作用的丝/苏氨酸蛋白激酶,在人体中有Aurora A、Aurora B和Aurora C三个家族成员.Aurora蛋白激酶参与细胞有丝分裂过程,其异常表达会损害有丝分裂进程,并引起遗传不稳定性,最终导致细胞癌变.目前研究发现Aurora蛋白激酶在多种肿瘤细胞中高表达,并参与了这些肿瘤的发生发展.鉴于以上研究,以Aurora激酶为靶点的抗肿瘤药物研发为癌症治疗提供了新的策略.目前,已经有相当多的Aurora激酶抑制剂被开发出来,其中部分抑制剂展现出了显著的抑瘤效果,且已进入临床试验阶段.

Aurora Protein Kinase Inhibitors as Anticancer Agents

Aurora kinase is a family of serine/threonine protein kinases and plays essential roles in cell proliferation. The human Aurora kinase family has three members: Aurora A, Aurora B and Aurora C. Aurora family kinase has critical roles in mitotic progression. Aberrant expression of Aurora kinase causes abnormal mitotic progression and thereby leads to genetic instability and carcinogenesis. Aurora kinase is frequently over-expressed in many types of human tumors and contributes to the tumors development. Thus, development of inhibitors targeting Aurora family kinase provides new strategies for cancer treatment. To date, a considerable number of Aurora family kinase inhibitors have been developed, among which, great antitumor effects were shown in some inhibitors and progressed into clinical studies.