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化学进展 1999, Vol. 11 Issue (03): 265- 前一篇   后一篇

• 综述与评论 •

发现生物大分子高亲和性配体的新方法——SAR-by-NMR

麻锦彪; 吴厚铭*   

  1. （中国科学院上海有机化学研究所 上海 200032）
  • 收稿日期:1998-10-01 修回日期:1999-01-01 出版日期:1999-09-24 发布日期:1999-09-24
  • 通讯作者: 吴厚铭
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A New Method to Discover High-Affinity Ligands for Bio-Macromolecules: SAR-by-NMR

Ma Jinbiao;Wu Houming*   

  1. (Shanghai Institute of Organic Chemis ry,Chinese Academy of Sciences, Shanghai 200032, China)
  • Received:1998-10-01 Revised:1999-01-01 Online:1999-09-24 Published:1999-09-24
  • Contact: Wu Houming

由于许多药物通过和生物体内的大分子(如蛋白质和核酸) 的选择性结合发挥效用, 因此快速、有效地发现靶分子的高亲和性配体成为各种药物发现方法的首要目标。在现代生物技术和NMR 技术高度发展的基础上产生的一种发现生物大分子高亲和性配体的新方法——SAR-by-NMR, 由于采用NMR 技术可以综合多种药物设计方法的优势, 能够在短时间内得到先导化合物, 从而大大加快了药物发现的速度并能节省大量的费用。本文介绍了SAR-by-NMR 发现高亲和性配体的基本原理、特点及其在药物发现中的应用。

关键词： 高亲和性配体, 蛋白质NMR结构, 结构与活性关系, 药物发现

As most drugs work when they selectively bind to biological targets (e. g.proteins and nuclear acids) , to find highaffinity ligands f r a target molecule fast and effectually becomes the key step of various drugdiscovery methods. A new technique to discover highaffinity ligands for biomacromolecules, SAR-by-NMR, comes into being on the bases of high developments of modern biological and NMR technologies, which significantly accelerates the drug discovery and reduces the expenses. This method combines the advantages of many drug design methods and requires only short time to get lead compounds due to the use of NMR technologies. The essential principle of using SAR-by-NMR to find high-affinity ligands, its distinguishing features, and applications in drug discovery are reviewed in this paper.

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