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Aurora kinase inhibitors.

机译:极光激酶抑制剂。

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摘要

Most human cancer cells are characterized by changes in the amount or organization of DNA resulting in chromosome instability and aneuploidy. Several mitotic kinases, Aurora kinases amongst others, regulate the progression of the cell through mitosis. So far three Aurora kinases have been identified in man: Aurora-A, Aurora-B and Aurora-C. Aurora kinases were recently identified as a potential target in anticancer therapy, and various Aurora-A and Aurora-B kinase inhibitors are in development. In this review we provide a brief insight into the mechanism of action as far as currently available. We review the available pre-clinical data, discuss the clinical phase I data and try to give a direction for future headings.
机译:大多数人类癌细胞的特征是DNA数量或组织的变化,导致染色体不稳定和非整倍性。几种有丝分裂激酶,尤其是Aurora激酶,通过有丝分裂调节细胞的进程。迄今为止,已在人体中鉴定出三种Aurora激酶:Aurora-A,Aurora-B和Aurora-C。最近,Aurora激酶被确定为抗癌治疗的潜在靶标,并且各种Aurora-A和Aurora-B激酶抑制剂正在开发中。在这篇综述中,我们对当前的作用机理进行了简要的介绍。我们审查了可用的临床前数据,讨论了临床I期数据,并试图为今后的发展方向指明方向。

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