药学学报, 2021, 56(4): 996-1005
引用本文:
刘翠翠, 王奇升, 田永奇*, 汪少芸. 配体垂钓:一种从生物提取物中快速筛选活性化合物的方法[J]. 药学学报, 2021, 56(4): 996-1005.
LIU Cui-cui, WANG Qi-sheng, TIAN Yong-qi*, WANG Shao-yun. Ligand fishing: a strategy for rapidly screening bioactive compounds from organism extracts[J]. Acta Pharmaceutica Sinica, 2021, 56(4): 996-1005.

配体垂钓:一种从生物提取物中快速筛选活性化合物的方法
刘翠翠, 王奇升, 田永奇*, 汪少芸
福州大学生物科学与工程学院, 福建 福州 350108
摘要:
天然产物是新药发现的宝贵资源。迄今为止,从生物提取物中快速筛选活性化合物仍是一项重要而富有挑战性的任务。传统的活性追踪法涉及重复的分离和活性测试步骤,耗时耗力且低效。配体垂钓是一种基于分子间的亲和作用,从复杂的生物样品中亲和选择配体的生物分析方法,具有特异性强、效率高、对样品预处理要求少等特点。本综述总结了配体垂钓的分类以及在酶抑制剂筛选中的应用,并对该技术的发展前景进行了展望。
关键词:    天然产物      配体垂钓      活性化合物     
Ligand fishing: a strategy for rapidly screening bioactive compounds from organism extracts
LIU Cui-cui, WANG Qi-sheng, TIAN Yong-qi*, WANG Shao-yun
College of Biological Science and Engineering, Fuzhou University, Fuzhou 350108, China
Abstract:
Natural products are valuable resources for discovering new drugs. So far, screening bioactive compounds from organism extracts is still an important and challenging task. Traditional biometric guided method involves repeated fractionation steps and bioactivity tests, which are time-consuming, labor-consuming, and inefficient. Ligand fishing is a bioanalysis method for screening ligands from complex organism extracts based on intermolecular affinity interactions. It has the characteristics of strong specificity, high efficiency, and less requirement for sample pretreatment. In this review, we summarize the classification of ligand fishing strategy and its application in enzyme inhibitors screening. Finally, the development prospects of this technology are forecasted.
Key words:    natural product    ligand fishing    bioactive compound   
收稿日期: 2020-09-09
DOI: 10.16438/j.0513-4870.2020-1465
基金项目: 国家自然科学基金资助项目(42006094);福建省自然科学基金资助项目(2019J05032);中央财政奖补项目资金(202006).
通讯作者: 田永奇,E-mail:tianyongqi@fzu.edu.cn
Email: tianyongqi@fzu.edu.cn
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