Polo样激酶1抑制剂临床前和早期临床研究进展

摘要

Polo-like kinase 1 (PLK1) is a highly conserved serine/threonine protein kinases that plays a key role in regulation of mitosis. In about 80％ of human tumors, of various origins,PLK1 is over expressed. Over-expression of PLK1 is associated with a poor prognosis in several tumor types and a lower overall survival rate. PLK1 inhibitor can interfere with different stages of mitosis, such as centrosome maturation, spindle formation, chromosome separation, and cytokinesis. This review includes an overview of PLK1 inhibitor in clinical and preclinical development.%Polo样激酶1(PLK 1)是一种高度保守的丝氨酸/苏氨酸蛋白激酶,在细胞有丝分裂过程中发挥重要作用.人类80%的肿瘤类型中,PLK1高度表达.PLK1的过表达与部分肿瘤的预后不良和整体存活率较低相关.PLK1抑制剂对有丝分裂的不同阶段具有干扰作用,如中心体的成熟、纺锤体的形成、染色体的分离和胞质分裂等,最终导致肿瘤细胞凋亡.综述PLK1抑制剂临床前和早期临床的研究进展.