Department of Pathophysiology, School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, 450001, Henan, China.
China-US (Henan) Hormel Cancer Institute, No. 127, Dongming Road, Jinshui District, Zhengzhou, 450008, Henan, China.
Mol Cancer. 2021 Jan 15;20(1):15. doi: 10.1186/s12943-020-01305-3.
Aurora kinase A (AURKA) belongs to the family of serine/threonine kinases, whose activation is necessary for cell division processes via regulation of mitosis. AURKA shows significantly higher expression in cancer tissues than in normal control tissues for multiple tumor types according to the TCGA database. Activation of AURKA has been demonstrated to play an important role in a wide range of cancers, and numerous AURKA substrates have been identified. AURKA-mediated phosphorylation can regulate the functions of AURKA substrates, some of which are mitosis regulators, tumor suppressors or oncogenes. In addition, enrichment of AURKA-interacting proteins with KEGG pathway and GO analysis have demonstrated that these proteins are involved in classic oncogenic pathways. All of this evidence favors the idea of AURKA as a target for cancer therapy, and some small molecules targeting AURKA have been discovered. These AURKA inhibitors (AKIs) have been tested in preclinical studies, and some of them have been subjected to clinical trials as monotherapies or in combination with classic chemotherapy or other targeted therapies.
极光激酶 A（AURKA）属于丝氨酸/苏氨酸激酶家族，其通过调节有丝分裂，对细胞分裂过程的激活是必需的。根据 TCGA 数据库，AURKA 在多种肿瘤类型的癌症组织中的表达明显高于正常对照组织。AURKA 的激活已被证明在广泛的癌症中发挥重要作用，并且已经鉴定出许多 AURKA 底物。AURKA 介导的磷酸化可以调节 AURKA 底物的功能，其中一些是有丝分裂调节剂、肿瘤抑制因子或癌基因。此外，通过 KEGG 途径和 GO 分析富集 AURKA 相互作用蛋白表明，这些蛋白参与经典致癌途径。所有这些证据都支持将 AURKA 作为癌症治疗的靶点的想法，并且已经发现了一些针对 AURKA 的小分子。这些 AURKA 抑制剂（AKIs）已在临床前研究中进行了测试，其中一些已作为单药或与经典化疗或其他靶向治疗联合进行临床试验。
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