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妇科恶性肿瘤中极光激酶抑制剂的最新进展

Update on aurora kinase inhibitors in gynecologic malignancies.

作者信息

Tao Xia, Chon Hye S, Fu Siqing, Kavanagh John J, Hu Wei

机构信息

Department of Gynecologic Oncology, The University of Texas M. D. Anderson Cancer Center, 1515 Holcombe Boulevard, Houston, TX 77030, USA.

出版信息

Recent Pat Anticancer Drug Discov. 2008 Nov;3(3):162-77. doi: 10.2174/157489208786242322.

Abstract

Aurora kinases are essential for the regulation of chromosome segregation and cytokinesis during mitosis and play a role in tumorigenesis and tumor progression in humans. Aurora kinase A and Aurora kinase B are overexpressed in some gynecologic cancers, and their overexpression is associated with poor prognosis. Thus, targeting of Aurora kinases has become an attractive strategy for pharmaceutical companies, who have developed more than 30 Aurora kinase inhibitors for treatment of cancers. Some of these inhibitors have been shown to be effective in targeted therapies for human cancer, and others are currently being investigated. In this review, we summarize the most recent advances in preclinical studies and clinical trials of patented Aurora kinase inhibitors for gynecologic tumors.

摘要

极光激酶对于有丝分裂过程中染色体分离和胞质分裂的调控至关重要,并且在人类肿瘤发生和肿瘤进展中发挥作用。极光激酶A和极光激酶B在某些妇科癌症中过度表达,它们的过度表达与预后不良相关。因此,靶向极光激酶已成为制药公司颇具吸引力的策略,这些公司已开发出30多种用于治疗癌症的极光激酶抑制剂。其中一些抑制剂已被证明在人类癌症的靶向治疗中有效,其他抑制剂目前正在研究中。在本综述中,我们总结了专利极光激酶抑制剂用于妇科肿瘤的临床前研究和临床试验的最新进展。

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