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AURORA-KINASE INHIBITORS AS ANTICANCER AGENTS

机译:作为抗癌剂的极光激酶抑制剂

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Errors in mitosis can provide a source of the genomic instability that is typically associated with tumorigenesis. Many mitotic regulators are aberrantly expressed in tumour cells. These proteins could therefore make useful therapeutic targets. The kinases Aurora-A, -B and -C represent a family of such targets and several small-molecule inhibitors have been shown to block their function. Not only have these inhibitors advanced our understanding of mitosis, but, importantly, their in vivo antitumour activity has recently been reported. What have these studies taught us about the therapeutic potential of inhibiting this family of kinases?
机译:有丝分裂中的错误可以提供通常与肿瘤发生有关的基因组不稳定的来源。许多有丝分裂调节剂在肿瘤细胞中异常表达。这些蛋白质因此可以成为有用的治疗靶标。激酶Aurora-A,-B和-C代表了这类靶标的家族,并且几种小分子抑制剂已被证明可阻断其功能。这些抑制剂不仅提高了我们对有丝分裂的理解,而且重要的是,最近已报道了它们的体内抗肿瘤活性。这些研究告诉我们什么抑制该激酶家族的治疗潜力?

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