摘要Polo-like kinase1(PLK1)是一种保守的丝氨酸-苏氨酸蛋白激酶，属于polo-like蛋白激酶家族，在调节细胞有丝分裂、DNA损伤反应及维持基因组稳定性中发挥重要作用。PLK1在多种肿瘤组织中表达水平明显升高，并且在恶性肿瘤的发生发展过程中发挥重要作用，与多种癌症患者的不良预后密切相关。尽管PLK1的小分子抑制剂在细胞及动物模型中显示出强烈的抑瘤作用，但是单独应用PLK1靶向药物在多数临床试验中并未取得令人满意的疗效，因此将靶向抑制PLK1与放化疗或其他靶向治疗药物联合应用的恶性肿瘤治疗策略成为新的研究方向和热点。本文将在介绍PLK1异常表达与肿瘤发生发展关系的基础上，重点介绍以PLK1为靶点的单药及联合治疗在恶性肿瘤治疗中的最新进展和面临的挑战。

abstractsPolo-like kinase1 (PLK1) is a conserved serine-threonine protein kinase, belonging to the polo-like protein kinase family, which plays an important role in regulating cell mitosis, DNA damage response and maintaining genomic stability. The expression of PLK1 is significantly increased in various of tumor tissues, and plays an important role in the occurrence and development of malignant tumors, which is closely related to the poor prognosis of many cancer patients. Although small molecular inhibitors of PLK1 have shown strong anti-tumor effects in cells and animal models, the application of PLK1 targeting drugs alone has not achieved satisfactory efficacy in most clinical trials, so the targeted inhibition of PLK1 combined with radiotherapy, chemotherapy or other targeted drugs in the treatment of malignant tumors has become a new research direction and hotspot. Based on the introduction of the relationship between abnormal expression of PLK1 and tumorigenesis, this article will focus on the latest progress and challenges of monotherapy and combination therapy targeting PLK1 in the treatment of malignant tumors.