药物亲和反应的靶点稳定性(DARTS)技术研究进展——一种定位药物靶标的方法  

Advances in drugaffinity responsive target stability(DARTS)——a method for locating a drug target

作　　者：李德军[1,2] 石广亮 刘运枫[1,2] LI Dejun;SHI Guangliang;LIU Yunfeng(College of Veterinary Medicine,Northeast Agricultural University,Harbin Heilongjiang 150030,China;Key Laboratory of the Provincial Education Department of Heilongjiang for Common Animal Disease Prevention and Treatment,HarbinHeilongjiang 150030,China)

机构地区：[1]东北农业大学动物医学学院,黑龙江哈尔滨150030 [2]动物普通疾病防治重点实验室,黑龙江哈尔滨150030

出　　处：《中兽医医药杂志》2021年第2期40-43,共4页Journal of Traditional Chinese Veterinary Medicine

基　　金：留学基金委项目(201906615018);黑龙江省博士后启动基金项目(LBH-Z11239);国家自然基金项目(31702282);黑龙江省教育厅项目(UNPYSCT-2016139)。

摘　　要：药物靶点蛋白确定是研究开发新药的一个重要步骤。药物亲和反应的靶点稳定性(DARTS)技术是一种可以快速和直接识别小分子药物潜在靶点蛋白的技术,即靶蛋白与药物结合后,保护靶蛋白不被蛋白酶水解,进而维护靶蛋白的活性和功能。综述DARTS技术的起源、DARTS原理及优缺点、DARTS应用等方面研究进展,为进一步探索药物与靶蛋白的生物相关性、促进该方法在新药研发和靶标鉴定方面的应用提供参考。The determination of drug target proteins is an important step in the development of new drugs. Drug affinity reac-tion target stability(DARTS) technology is a relatively fast and direct method to identify potential target proteins of small molecule drugs. After the target protein is combined with the drug,the target proteinare protected and are hydrolysised by protease. Furthermore,the activity and function of the target protein are maintained. In this paper,the origin,principle,advantages and disadvantages of DARTS technology,DARTS application and other aspects were reviewed,so as to provide reference for further exploring the biological correlation between drugs and target proteins,and promoting the application of this method in new drug development and target identification.

关 键 词：DARTS 靶标 小分子药物 蛋白酶 

分 类 号：S859.1[农业科学—临床兽医学]