文献类型：期刊文献

英文题名：Drug affinity responsive target stability (DARTS) accelerated small molecules target discovery: Principles and application

作者：Ren, Ying-Shan[1,2,3];Li, Hui-Lin[1,2,3];Piao, Xiu-Hong[2,4];Yang, Zhi-You[5];Wang, Shu-Mei[1,2,3];Ge, Yue-Wei[1,2,3]

机构：[1]Guangdong Pharmaceut Univ, Sch Tradit Chinese Med, Guangzhou 510006, Peoples R China;[2]Guangdong Pharmaceut Univ, Key Lab Digital Qual Evaluat Chinese Mat Med Stat, Guangzhou 510006, Peoples R China;[3]Guangdong Pharmaceut Univ, Engn & Technol Res Ctr Chinese Mat Med Qual Univ, Guangzhou 510006, Peoples R China;[4]Guangdong Pharmaceut Univ, Sch Life Sci & Biopharmaceut, Guangzhou 510006, Peoples R China;[5]Guangdong Ocean Univ, Coll Food Sci & Technol, Guangdong Prov Key Lab Aquat Prod Proc & Safety, Zhanjiang 524088, Peoples R China

年份：2021

卷号：194

外文期刊名：BIOCHEMICAL PHARMACOLOGY

收录：SCI-EXPANDED(收录号：WOS:000729042500003)、、Scopus(收录号：2-s2.0-85118319555)、WOS

基金：This study was supported by the National Natural Science Foundation of China (No. 81872988 and 82074117, China), Guangdong Basic and Applied Basic Research Foundation (No. 2020A1515010472, China), Innovation project of Guangdong Provincial Department of Education (No. 2018KTSCX106, China), Youth Innovative Talents Project of Guangdong Provincial Department of Education (No. 2018KQNCX132, China) and Medical Scientific Research Foundation of Guangdong Province of China (No. B2019032 and B2019100, China).

语种：英文

外文关键词：Drug affinity responsive target stability; DARTS; Small molecules; Drug target; Target discovery

外文摘要：Drug affinity responsive target stability (DARTS) is a novel target discovery approach and is particularly adept at screening small molecule (SM) targets without requiring any structural modifications. The DARTS method is capable of revealing drug-target interactions from cells or tissues by tracking changes in the stability of proteins acting as receptors of bioactive SMs. Due to its simple operation and high efficiency, the DARTS method has been applied to uncover the drug-action mechanism. This review summarized analytical principles, protocols, validation approaches, applications, and challenges involved in the DARTS method. Due to the innate advantages of the DARTS method, it is expected to be a powerful tool to accelerate SM target discovery, especially for bioactive natural products with unknown mechanisms.