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Plk1是一种高度保守的丝氨酸/苏氨酸激酶,经磷酸化激活,在细胞有丝分裂的不同时期都起到十分重要的作用:在G2晚期M初期参与Cdc25C的活化,继而促成cyclin B/Cdc2的激活、协助中心体的功能成熟以及双极性纺锤体的形成,从而促进M期的起始和染色体正常分离、分配;通过调节APC(anaphase-promoting complex)决定细胞能否按期离开M期。正常情况下,DNA的损伤将阻抑细胞进入分裂期(M),Plk1活性受抑在其中起关键性的作用。Plk1可以使细胞周期停滞在G2期或M期的多个时点。Plk1尚参与哺乳动物细胞有丝分裂中高尔基体特异性碎解、分离入子细胞并融合重构的过程。在大多数人类肿瘤中Plk1均高表达。已经建立了针对Plk1 mRNA的反义寡核苷酸,它能特异性地抑制Plk1 mRNA及其蛋白产物,有效抑制培养细胞系或裸鼠肿瘤模型中肿瘤细胞的增殖。
Plk1, a highly conserved serine / threonine kinase, is activated by phosphorylation and plays a very important role in different stages of cell mitosis. It is involved in the activation of Cdc25C in the early phase of G2 and then promotes the expression of cyclin B / Cdc2 Activate, facilitate the functional maturation of centrosomes and the formation of bipolar spindles, thereby promoting the initiation of M phase and the normal chromosome separation and distribution; by adjusting the APC (anaphase-promoting complex) to decide whether the cells can leave the M period. Under normal circumstances, DNA damage will inhibit the cells into the division (M), Plk1 inhibition of which plays a key role. Plk1 can arrest the cell cycle at multiple points in the G2 or M phase. Plk1 is still involved in mammalian cell mitotic Golgi-specific disruption, separation into daughter cells and fusion reconstruction process. Plk1 is highly expressed in most human tumors. Antisense oligonucleotides targeting Plk1 mRNA have been established that specifically inhibit Plk1 mRNA and its protein product and effectively inhibit tumor cell proliferation in cultured cell lines or nude mouse tumor models.