Polo样激酶1功能及其在肿瘤靶向治疗中的应用

The Function of Polo-like Kinase 1 and Its Implication in Cancer Targeting Therapy

Polo样激酶1(polo-like kinase1,PLK1)是一种广泛存在于真核细胞中的丝/苏氨酸激酶,在细胞周期调控中发挥关键的作用。其主要功能包括参与激活cyclin B/CDK1复合体,协助中心体的功能成熟,活化细胞分裂后期促进复合物(anaphase promoting complex,APC),促进染色体正常分离、分配和调控胞质分裂等。现已发现PLK1在多种肿瘤中表达增高并与某些肿瘤的预后密切相关。利用反义寡核苷酸、RNA干扰技术和化学合成PLK1小分子抑制剂等方法阻断PLK1的表达或降低其激酶活性,能够有效抑制肿瘤细胞的增殖并介导肿瘤细胞的凋亡,但对正常细胞没有明显影响,因此PLK1在肿瘤靶向治疗中具有重要的应用前景。

Polo-like kinase 1 （PLK1）, a high/y conserved serine/threonine kinase, plays pivotal roles in the regulation of cell cycle progression, including the activation of Cdc2/cyclin B, centrosome assembly and maturation, activation of the anaphase-promoting complex （APC） during the metaphase-anaphase transition, mitotic exit and cytokinesis. Recent studies show that PLK1 is generally overexpressed in various human tumors and possesses prognostic potential in cancer. Inhibition of PLK1 expression or activity induces the significant apoptosis of tumor cells, but not normal cells. Here we discuss the study on PLK1 and the application of PLK 1 as a target for therapeutic intervention against cancer.