1.Non-small molecule PROTACs (NSM-PROTACs): Protein degradation kaleidoscope.
Sinan MA ; Jianai JI ; Yuanyuan TONG ; Yuxuan ZHU ; Junwei DOU ; Xian ZHANG ; Shicheng XU ; Tianbao ZHU ; Xiaoli XU ; Qidong YOU ; Zhengyu JIANG
Acta Pharmaceutica Sinica B 2022;12(7):2990-3005
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.