Departments of Medical Oncology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA.
Anticancer Drugs. 2010 Apr;21(4):339-50. doi: 10.1097/CAD.0b013e3283350dd1.
Aurora kinases are serine and threonine kinases that function as key regulators of the mitosis process. There are three distinct human aurora kinases known as Aurora A, Aurora B, and Aurora C. Aurora A and Aurora B are overexpressed in a number of human cancers including non-small cell lung cancer, glioblastomas, and upper gastrointestinal adenocarcinomas. Given their association with tumorigenesis, both Aurora A and Aurora B have been targeted for cancer therapy. Currently, a number of selective and nonselective aurora kinase inhibitors are being tested in preclinical and clinical settings as anti-tumor agents. We review the biology of human aurora kinases, followed by an overview of inhibitors undergoing current clinical investigations.
极光激酶是丝氨酸和苏氨酸激酶，作为有丝分裂过程的关键调节剂。已知有三种不同的人类极光激酶，分别称为 Aurora A、Aurora B 和 Aurora C。Aurora A 和 Aurora B 在多种人类癌症中过度表达，包括非小细胞肺癌、神经胶质瘤和上胃肠道腺癌。鉴于它们与肿瘤发生的关联，Aurora A 和 Aurora B 都已被作为癌症治疗的靶点。目前，许多选择性和非选择性极光激酶抑制剂正在临床前和临床环境中作为抗肿瘤药物进行测试。我们综述了人类极光激酶的生物学特性，随后概述了正在进行的临床研究的抑制剂。
