Ma Sinan, Ji Jianai, Tong Yuanyuan, Zhu Yuxuan, Dou Junwei, Zhang Xian, Xu Shicheng, Zhu Tianbao, Xu Xiaoli, You Qidong, Jiang Zhengyu
State Key Laboratory of Natural Medicines and Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.
Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Acta Pharm Sin B. 2022 Jul;12(7):2990-3005. doi: 10.1016/j.apsb.2022.02.022. Epub 2022 Feb 26.
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.
蛋白质靶向嵌合体（PROTACs）技术自2001年诞生以来发展迅速，迅速吸引了科研机构和制药公司越来越多的关注。目前，多种小分子PROTACs已进入临床试验阶段。然而，在小分子PROTACs蓬勃发展的同时，近年来肽类PROTACs、核酸PROTACs和抗体PROTACs等非小分子PROTACs（NSM-PROTACs）也取得了长足进展，展现出超越小分子PROTACs的独特特性。在此，我们简要介绍NSM-PROTACs的类型，描述NSM-PROTACs的优势，并详细总结NSM-PROTACs迄今为止的发展情况。我们希望本文不仅能为NSM-PROTACs提供有益的见解，还能拓展对NSM-PROTACs的研究兴趣。
