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蛋白激酶在细胞周期的各个阶段及细胞周期检测点发挥着重要的调控作用,而异常的细胞分裂往往是肿瘤发生的标志之一。多种有丝分裂激酶与肿瘤的发生密切相关,被检测在多种肿瘤细胞中过度表达,使其成为抗肿瘤药物研究的靶点。目前一些抗肿瘤药物的研究集中在有丝分裂激酶的抑制剂上,许多小分子抑制剂已经进入临床实验研究阶段。文章就3类主要的有丝分裂激酶——Polo like激酶(PLKs)、Aurora激酶和Cyclin-dependent激酶(CDKs)及其小分子抑制剂研究现状进行综述,为今后有丝分裂激酶抑制剂的研究提供思路。
Protein kinases play an important regulatory role at all stages of the cell cycle and at cell cycle checkpoints, and aberrant cell division is often one of the hallmarks of tumorigenesis. A variety of mitotic kinases are closely related to tumorigenesis, and are over-expressed in a variety of tumor cells, making them a target of antitumor drug research. At present, some antitumor drug research has focused on inhibitors of mitotic kinases, and many small molecule inhibitors have entered the clinical experimental phase. This review summarizes the research status of three major mitotic kinases, such as PLKs, Aurora kinases and cyclin-dependent kinases (CDKs) and their small molecule inhibitors, and provides ideas for the future research of mitotic kinase inhibitors.