Non-small molecule PROTACs(NSM-PROTACs):Protein degradation kaleidoscope  

作　　者：Sinan Ma Jianai Ji Yuanyuan Tong Yuxuan Zhu Junwei Dou Xian Zhang Shicheng Xu Tianbao Zhu Xiaoli Xu Qidong You Zhengyu Jiang 

机构地区：[1]State Key Laboratory of Natural Medicines and Jiang Su Key Laboratory of Drug Design and Optimization,China Pharmaceutical University,Nanjing 210009,China [2]Department of Medicinal Chemistry,School of Pharmacy,China Pharmaceutical University,Nanjing 210009,China

出　　处：《Acta Pharmaceutica Sinica B》2022年第7期2990-3005,共16页药学学报（英文版）

基　　金：supported by Projects 81773581,82173680 and 81930100 of the National Natural Science Foundation of China;the Priority Academic Program Development of Jiangsu Higher Education Institutions,CPU2018GY02 of Double First Class Innovation Team of China Pharmaceutical University;the Project Program of State Key Laboratory of Natural Medicines,China Pharmaceutical University(No.SKLNMZZ202003);the“Qing Lan”Project of Jiangsu Province;the Young Elite Scientists Sponsorship Program by CAST(No.YESS20180146,China)。

摘　　要：The proteolysis targeting chimeras(PROTACs)technology has been rapidly developed since its birth in 2001,attracting rapidly growing attention of scientific institutes and pharmaceutical companies.At present,a variety of small molecule PROTACs have entered the clinical trial.However,as small molecule PROTACs flourish,non-small molecule PROTACs(NSM-PROTACs)such as peptide PROTACs,nucleic acid PROTACs and antibody PROTACs have also advanced considerably over recent years,exhibiting the unique characters beyond the small molecule PROTACs.Here,we briefly introduce the types of NSM-PROTACs,describe the advantages of NSM-PROTACs,and summarize the development of NSM-PROTACs so far in detail.We hope this article could not only provide useful insights into NSM-PROTACs,but also expand the research interest of NSM-PROTACs.

关 键 词：Non-small molecule PROTACs Protein degradation Peptide PROTACs Nucleic acid PROTACs Antibody PROTACs 

分 类 号：R914[医药卫生—药物化学]