文献类型：期刊文献

英文题名：Small molecule PROTACs in targeted therapy: An emerging strategy to induce protein degradation

作者：Xi, Meiyang[1];Chen, Yi[1];Yang, Hongyu[2];Xu, Huiting[1];Du, Kui[1];Wu, Chunlei[1];Xu, Yanfei[1];Deng, Liping[1];Luo, Xiang[1];Yu, Lemao[1];Wu, Yonghua[1];Gao, Xiaozhong[1];Cai, Tao[1];Chen, Bin[1];Shen, Runpu[1];Sun, Haopeng[2]

机构：[1]Shaoxing Univ, Coll Chem & Chem Engn, Shaoxing 312000, Peoples R China;[2]China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Jiangsu, Peoples R China

年份：2019

卷号：174

起止页码：159

外文期刊名：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

收录：SCI-EXPANDED(收录号：WOS:000469159800013)、、Scopus(收录号：2-s2.0-85064628227)、WOS

基金：The authors greatly acknowledge the support from the Science Foundation of Shaoxing University (No. 20175022, 2018LG1001) and the grants of National Natural Science Foundation of China (No. 81573281, 81602949). We declare no other conflicts of interest.

语种：英文

外文关键词：PROTACs; E3 ligase; Proteasome; Degradation

外文摘要：Inhibitors and nucleic acid based techniques were two main approaches to interfere with protein signaling and respective cascade in the past. Until recently, a new class of small molecules named proteolysis-targeting chimeras (PROTACs) have emerged. Each contains a target warhead, a linker and an E3 ligand. These bifunctional molecules recruit E3 ligases and target specific proteins for degradation via the ubiquitin (Ub) proteasome system (UPS). The degradation provides several advantages over inhibition in potency, selectivity and drug resistance. Thus, a variety of small molecule PROTACs have been discovered so far. In this review, we summarize the biological mechanism, advantages and recent progress of PROTACs, trying to offer an outlook in development of drugs targeting degradation in future. (C) 2019 Elsevier Masson SAS. All rights reserved.