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Polo样激酶1抑制剂临床前和早期临床研究进展
引用本文:孙天宇,孙建国,王广基.Polo样激酶1抑制剂临床前和早期临床研究进展[J].药学与临床研究,2011,19(2):146-150.
作者姓名:孙天宇  孙建国  王广基
作者单位:中国药科大学药代重点实验室,南京,210009
摘    要: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。

关 键 词:Polo样激酶1  有丝分裂  Polo样激酶1抑制剂  肿瘤
收稿时间:2010/12/24 0:00:00
修稿时间:2011/1/18 0:00:00

Preclinical Research and Early Clinical Research of Polo-like Kinase 1 Inhibitors
SUN Tian-yu,SUN Jian-guo and WANG Guang-ji.Preclinical Research and Early Clinical Research of Polo-like Kinase 1 Inhibitors[J].Pharmacertical and Clinical Research,2011,19(2):146-150.
Authors:SUN Tian-yu  SUN Jian-guo and WANG Guang-ji
Affiliation:SUN Tian-yu,SUN Jian-guo,WANG Guang-ji Laboratory of Pharmacokinetics,China Pharmaceutical University,Nanjing 210009,China
Abstract: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 inhibito...
Keywords:Polo-like kinase  Mitosis  Polo-like kinase 1 inhibitor  Tumor  
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