【摘要】 PLK1(Polo-like kinases1)激酶参与众多细胞有丝分裂过程，且在多种肿瘤细胞中过表达，为一种极具潜力的抗肿瘤治疗靶标。PBD(Polo-box domain)区域是该激酶家族特有的结构，对PLK1在细胞中的定位和底物的磷酸化过程起重要作用。作用于PBD区域的化合物可克服对其他激酶选择性及对PLK1耐药性等问题。本文作者对小分子类PLK1-PBD抑制剂的最新研究进展进行综述，并对其发展前景予以展望。更多还原

【Abstract】 PLK1 kinase is involved in the mitotic process of many cells and overexpressed in cancer cells, making it a potential target for anti-tumor therapy.The PBD region is a unique structure of PLKs, which plays an important role in the localization of PLK1 in cells and the phosphorylation of substrates.Inhibitors based on PBD region can overcome the issues of low selectivity and drug resistance.In this paper, the latest research progress of small molecule PLK1-PBD inhibitors was reviewed, and the development was prospected based on the author′s own research experience.更多还原