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

Author: Sinan MA ¹ ; Jianai JI ¹ ; Yuanyuan TONG ¹ ; Yuxuan ZHU ¹ ; Junwei DOU ¹ ; Xian ZHANG ¹ ; Shicheng XU ¹ ; Tianbao ZHU ¹ ; Xiaoli XU ¹ ; Qidong YOU ¹ ; Zhengyu JIANG ¹
Author Information

1. State Key Laboratory of Natural Medicines and Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.
Publication Type:Review
Keywords: Antibody PROTACs; Non-small molecule PROTACs; Nucleic acid PROTACs; Peptide PROTACs; Protein degradation
From: Acta Pharmaceutica Sinica B 2022;12(7):2990-3005
CountryChina
Language:English
Abstract: 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.