天然活性小分子靶标蛋白识别方法学研究进展

药物靶标是指人体内与药物相互作用并赋予药物效应的特定分子。作为传统中药的药效物质基础,天然活性小分子的作用机制阐明,特别是作用靶标的鉴定一直是药学研究者关注的重要课题,然而目前该领域一直未取得长足的进展。作者针对近年来在天然活性小分子靶标蛋白识别鉴定方面出现的新技术、新方法进行了总结,系统介绍了目前该领域的主流研究方法,原理以及成功案例,同时还探讨了每种方法的适用性及不同方法之间的优劣。相信该文对从事天然药物化学、药理学以及化学生物学领域的研究人员有一定的启发和借鉴作用。

Progress of methodology for identifying target protein of natural active small molecules

Drug targets are special molecules that can interact with drugs and exert pharmacological functions in human body. The natural active small molecules are the bioactive basis of traditional Chinese medicine, and the mechanism study is a hot topic now,especially for the identification of their target proteins. However,little progress has been made in this field until now. Here, we summarized the recent technologies and methods for the identification of target proteins of natural bioactive small molecules, and introduced the main research methods, principles and successful cases in this field. We also explored the applicability and discussed the advantages and disadvantages among different methods.We hope this review can be used as a reference for the researchers who engaged in natural pharmaceutical chemistry, pharmacology and chemical biology.