微量热泳动技术在药物靶点发现中的应用进展  

Advances in the Application of Microscale Thermophoresis in Drug Target Discovery

作　　者：卢慧 于莹[2] 凌建亚 程肖蕊[2] LU Hui;YU Ying;LING Jianya;CHENG Xiaorui(Department of Pharmacy,Shandong University of Traditional Chinese Medicine,Jinan 250355,China;Innovative Institute of Chinese Medicine and Pharmacy,Shandong University of Traditional Chinese Medicine,Jinan 250355,China;State Key Laboratory of Microbial Technology,Shandong University,Qingdao 266237,China)

机构地区：[1]山东中医药大学药学院,济南250355 [2]山东中医药大学中医药创新研究院,济南250355 [3]山东大学微生物技术国家重点实验室,山东青岛266237

出　　处：《中国药学杂志》2024年第22期2099-2106,共8页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金面上项目资助(82374062);中央引导地方科技发展专项资金项目资助(YDZX2023003);西藏自治区科技计划重点研发计划资助(XZ202201ZY0026G);山东省2023年度中央引导地方科技发展资金项目资助(YDZX2023137)。

摘　　要：药物靶点的发现对于理解药物作用机制和新药开发至关重要。微量热泳动技术(microscale thermophoresis,MST)以其具有样本用量少、检测速度快、灵敏度高且无须固定蛋白的特点,成为药物靶点研究中的重要工具之一。文章简述了药物靶点的发现策略,重点介绍了MST技术的原理及其在药物靶点发现中的应用,并总结了其应用前景。MST技术在靶点发现的正向和逆向策略中均有应用,可以用于化合物、中药单体成分及复方的靶点蛋白确定或药物筛选。此外,MST与其他分子互作技术如表面等离子体共振技术(surface plasmon resonance,SPR)等联用,为药物与靶点相互作用的研究提供了有力工具。尽管MST技术存在一定的局限性,但它在新药研发和药物机制研究领域仍具有广阔的应用前景。The discovery of drug targets is crucial for understanding the mechanism of drug action and facilitating the development of novel drug therapeutics.Microscale thermophoresis(MST),renowned for its minimal sample consumption,rapid detection speed,high sensitivity,and the absence of the need for protein immobilization,has emerged as a pivotal tool in drug target research.This article outlines the strategies for identifying drug targets,with a focus on elucidating the principles of MST and its application in drug target discovery.Furthermore,it summarizes the promising prospects of MST in this field.The applications of MST are found in both forward and reverse strategies for target discovery,enabling the identification of target proteins for compounds,single herbal ingredients,and compound prescriptions,as well as facilitating drug screening.Additionally,the integration of MST with other molecular interaction techniques,such as surface plasmon resonance(SPR),provides a potent arsenal for studying the interactions between drugs and their targets.Despite certain limitations,MST holds immense potential for application in the realms of novel drug development and drug mechanism research.

关 键 词：微量热泳动 药物靶点 分子互作技术 

分 类 号：R966[医药卫生—药理学]