Ａｕｒｏｒａ激酶抑制剂的抗肿瘤作用

Ａｕｒｏｒａ激酶抑制剂是分子靶向治疗的新领域，Ａｕｒｏｒａ激酶不仅与肿瘤密切相关，而且Ａｕｒｏｒａ激酶抑制剂也显示了很强的抗肿瘤能力，部分抑制剂都进入了Ⅰ期临床实验。Ａｕｒｏｒａ激酶抑制剂与传统的化疗药物如紫杉类药物、替莫唑胺、长春新碱、顺铂、足叶乙甙联合作用比单药作用更为显著；Ａｕｒｏｒａ激酶抑制剂可以克服Ｅ２引起的化疗耐药；Ａｕｒｏｒａ激酶抑制剂可以增强放疗的敏感性，然而Ａｕｒｏｒａ激酶抑制剂的作用依赖ｐ５３状态，只增强突变型ｐ５３或无功能ｐ５３肿瘤细胞对放疗或替莫唑胺化疗的敏感性。

The anticancer role of aurora kinase inhibitors

Aurora kinase inhibitors are new member of the family of targeted agents. Not only aurora kinases have strong correlation with tumor but also the anticancer efficacy of aurora kinase inhibitors, as monotherapy, were demonstrated in variety of cancer types, even, some of the inhibitors are ongoing phase I clinical trails. The emerging research in cancer cell lines showed that the combination of aurora kinase inhibitors and traditional chemotherapy agents such as taxanes, TMZ, vincristine, CDDP, and VP-16 was more effective than the each treatment alone. Aurora kinase inhibitors can override the chemoresistance caused by E2; aurora kinase inhibitors can enhance the sensitivity of radiotherapy to cancer. However, the role of aurora kinase inhibitors depends strongly on the p53 status： only the cancer cells with mutated p53 or no-functional p53 can benefit from the combination with radiotherapy or TMZ.