2. Academic Validation
  3. Non-small molecule PROTACs (NSM-PROTACs): Protein degradation kaleidoscope

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

  • Acta Pharm Sin B. 2022 Jul;12(7):2990-3005. doi: 10.1016/j.apsb.2022.02.022.
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 2,  Qidong You 1 2,  Zhengyu Jiang 1 2
Affiliations

Affiliations

  • 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.
PMID: 35865099 DOI: 10.1016/j.apsb.2022.02.022
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.

Keywords

Antibody PROTACs; Non-small molecule PROTACs; Nucleic acid PROTACs; Peptide PROTACs; Protein degradation.

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