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Polo样激酶1及其小分子抑制剂的研究进展
引用本文:卢帅,吴梦秋,颜婷婷,陈亚东,陆涛. Polo样激酶1及其小分子抑制剂的研究进展[J]. 药学进展, 2010, 34(3): 97-104. DOI: 10.3969/j.issn.1001-5094.2010.03.001
作者姓名:卢帅  吴梦秋  颜婷婷  陈亚东  陆涛
作者单位:1. 中国药科大学有机化学教研室,江苏,南京,210009
2. 中国药科大学无机化学教研室,江苏,南京,210009
基金项目:2009年度国家大学生实践创新训练计划项目 
摘    要:Polo样激酶1是一种丝氨酸/苏氨酸蛋白激酶,其结构和功能高度保守,参与细胞周期不同阶段检查点的精密调控,是维持细胞周期正常运行的一种关键物质。然而,该激酶在多种肿瘤细胞中高度表达,且其过度表达是肿瘤不良预后的标志之一,因此对其的研究对癌症的诊断和治疗以及新的抗癌药物的开发具有非常重要的意义。综述Polo样激酶1与有丝分裂和肿瘤的关系,介绍若干已进入临床研究的小分子Polo样激酶1抑制剂及其抗肿瘤活性和构效关系。

关 键 词:Polo样激酶1  有丝分裂  肿瘤  小分子抑制剂

Advances in the Research on PLK1 and Its Small Molecular Inhibitors
LU Shuai,WU Meng-qiu,YAN Ting-ting,CHEN Ya-dong,LU Tao. Advances in the Research on PLK1 and Its Small Molecular Inhibitors[J]. Progress in Pharmaceutical Sciences, 2010, 34(3): 97-104. DOI: 10.3969/j.issn.1001-5094.2010.03.001
Authors:LU Shuai  WU Meng-qiu  YAN Ting-ting  CHEN Ya-dong  LU Tao
Affiliation:LU Shuai 1,WU Meng-qiu1,YAN Ting-ting1,CHEN Ya-dong 2,LU Tao 1(1.Department of Organic Chemistry,China Pharmaceutical University,Nanjing 210009,China,2.Department of Inorganic Chemistry,China)
Abstract:Polo-like kinase 1(PLK1) is a highly conserved serine/threonine protein kinase that plays a key role in cell division and checkpoint regulation.PLK1 is over-expressed in many types of human tumors and has prognostic potential in tumors.Therefore,the research on PLK1 has the important significances in the diagnosis and treatment of tumor as well as in new anti-tumor drug development.The involvement of PLK1 in mitosis and tumor was reviewed.The small molecular PLK1 inhibitors in clinical trials and their anti...
Keywords:Polo-like kinase 1  mitosis  tumor  small molecular inhibitor  
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