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化学进展 2010, Vol. 22 Issue (11): 2207-2214 前一篇   后一篇

• 综述与评论 •

超滤质谱技术在药物小分子与生物靶分子相互作用研究中的应用*

周慧1,2  宋凤瑞1   刘志强1**   刘淑莹1   

  1. (1. 中国科学院长春应用化学研究所  长春 13022；中国科学院研究生院  北京  100039)
  • 收稿日期:2010-02-28 修回日期:2010-04-09 出版日期:2010-11-24 发布日期:2010-10-20
  • 通讯作者: 刘志强 E-mail:liuzq@ciac.jl.cn
  • 基金资助:

    国家科技部创新方法研究专项;国家杰出青年基金;吉林省科技发展计划

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Applications of Ultrafiltration Mass Spectrometry in the Studies on  interaction between medicine and biological target

Zhou Hui1,2  Song Fengrui1  Liu Zhiqiang1**  Liu Shuying1   

  1. (1.Changchun Institute of Appilied Chemistry,Chinese Academy of Sciences,Changchun 130022,China ;2.Gradute University of the,Chinese Academy of Sciences,Beijing 100039,China)
  • Received:2010-02-28 Revised:2010-04-09 Online:2010-11-24 Published:2010-10-20
  • Contact: Liu Zhiqiang E-mail:liuzq@ciac.jl.cn

药物小分子与生物体内靶分子之间的相互作用，是药物发挥其药理活性的重要途径之一。因此，高通量地筛选出能够与生物靶分子相互作用且具有生物活性的药物小分子，对于新药开发研究具有重要的理论意义和实际应用价值。超滤质谱技术是超滤装置与质谱技术结合后形成的一种新的分析方法，它能够在液相条件下快速地识别并鉴定出与生物靶分子结合的药物小分子配体。与其它分析方法相比，超滤质谱技术具有快速、灵敏、高通量的特点，因而被广泛应用于研究药物小分子和生物靶分子相互作用。本文综述了超滤质谱技术的原理、特点和实验操作中的一些关键问题。重点介绍了超滤质谱技术在药物小分子与生物靶分子相互作用研究中的应用进展，并对其未来的发展方向进行了展望。

关键词： 药物小分子, 生物靶分子, 相互作用, 超滤质谱

The interaction between medicine and biological target in vivo is one of the most important factors that determine the therapeutic activity of the medicine. Screening medicine that can bind with biological target and show well pharmacological effects will promotes the development of new medicine discovery significantly. therefore, several approaches have been developed to screening of combinatorial libraries and natural product extracts for biologically active compounds. Ultrafiltration mass spectrometry is a combination of ultrafiltration equipment and mass spectrometry, which is a valuable approach for the selection, structure analysis, and identification of low molecular weight compounds that interact with biological target in the solution phase. It has been developed as a powerful tool for the determination of the interaction between medicine and biological target because of its high speed, high sensitivity, and its high throughput screening ability. In this paper, the fundamental principles on which the ultrafiltration mass spectrometry is based, and the experimental details that must be considered during the operation of ultrafiltration equipment are introduced. The developments and applications of the ultrafiltration mass spectrometry in the studies on the interaction between medicine and biological target are reviewed. In addition, the developmental trend of the ultrafiltration mass spectrometry are also discussed．

Contents
1 Introduction
2 The fundamental principles of ultrafiltration mass spectrometry
3 The useful discussion of experimental details that must be considered
4 The recent applications of ultrafiltration mass spectrometry
5 Conclusions and outlook

Key words: small drug medicine, biological target, interaction, ultrafiltration mass spectrometry

中图分类号: 

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