| 双膦酸化合物对基质金属蛋白酶的抑制效应及机理 |
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| 引用本文： | 刘星辰,李洪伟,王烨,蒋坤,房学迅,吴玉清.双膦酸化合物对基质金属蛋白酶的抑制效应及机理[J].高等学校化学学报,2010,31(1):88-93. |
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| 作者姓名： | 刘星辰 李洪伟 王烨 蒋坤 房学迅 吴玉清 |
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| 作者单位： | 1. 吉林大学超分子结构与材料国家重点实验室, 长春130012;
2. 吉林大学分子酶学工程教育部重点实验室, 长春130021 |
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| 基金项目： | 国家自然科学基金(批准号:20973073,20773051);;国家“九七三”计划项目(批准号:2007CB808006);;吉林省科技发展计划项目(批准号:20070926-01);;教育部新世纪优秀人才支持计划资助 |
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| 摘 要： | 根据基质金属蛋白酶(MMPs)的活性位点附近三维空间结构, 设计合成了4种双膦酸类化合物, 利用酶促反应动力学方法对比测试了双膦酸化合物及阿伦磷酸钠(Alendronate)对MMPs的抑制效果; 结合分子对接方法以及荧光滴定光谱研究了双膦酸化合物与MMPs的分子识别和作用机理, 并得到了二者的结合模型.
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| 关 键 词： | 基质金属蛋白酶 抑制剂 双膦酸 分子识别 机理 |
| 收稿时间： | 2008-12-19 |
Activity Assay and Mechanism Study of Bisphosphonates as Matrix Metalloproteinase Inhibitors |
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| LIU Xing-Chen,LI Hong-Wei,WANG Ye,JIANG Kun,FANG Xue-Xun,WU Yu-Qing.Activity Assay and Mechanism Study of Bisphosphonates as Matrix Metalloproteinase Inhibitors[J].Chemical Research In Chinese Universities,2010,31(1):88-93. |
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| Authors: | LIU Xing-Chen LI Hong-Wei WANG Ye JIANG Kun FANG Xue-Xun WU Yu-Qing |
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| Institution: | 1. State Key Laboratory of Supramolecular Structure and Materials, Jilin University, Changchun 130012, China;
2. Key Laboratory for Molecular Enzymology and Engineering, the Ministry of Education, Jilin University, Changchun 130021, China |
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| Abstract: | Matrix metalloproteinases(MMPs),a group of zinc-dependent metalloproteinases,are responsible for the hydrolytic breakdown of extracellular matrix. Aberrantly over expression of MMPs has been associated with much human pathology including cancer,arthritis,and heart disease etc. Therefore,the development of MMPs inhibitors to drugs has always been of great interest to scientific institutions. Bisphosphonates were reported to be a new kind of MMPs inhibitors with great potential. According to the 3-dimensional... |
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| Keywords: | Matrix metalloproteinases(MMPs) Inhibitor Bisphosphonate Molecular recognition Mechanism |
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