Stimuli-activatable PROTACs for precise protein degradation and cancer therapy
文献类型：期刊论文
| 作者 | Gao, Jing2; Yang, Lei2; Lei, Shumin2; Zhou, Feng2; Nie, Huijun3; Peng, Bo4; Xu, Tianfeng3; Chen, Xiaohua3,5 ; Yang, Xiaobao6; Sheng, Chunquan7
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| 刊名 | SCIENCE BULLETIN
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| 出版日期 | 2023-05-30 |
| 卷号 | 68期号:10页码:1069-1085 |
| ISSN号 | 2095-9273 |
| 关键词 | PROTAC Stimuli-activatable prodrug Precise protein degradation Nanomedicine Combinatory therapy |
| DOI | 10.1016/j.scib.2023.04.028 |
| 通讯作者 | Xu, Zhiai(xuza@ecnu.edu.cn) ; Yu, Haijun(hjyu@simm.ac.cn) |
| 英文摘要 | The proteolysis targeting chimeras (PROTACs) approach has attracted extensive attention in the past decade, which represents an emerging therapeutic modality with the potential to tackle disease-causing proteins that are historically challengeable for conventional small molecular inhibitors. PROTAC harnesses the endogenic E3 ubiquitin ligase to degrade protein of interest (POI) via ubiquitin-proteasome system in a cycle-catalytic manner. The event-driven pharmacology of PROTAC is poised to pursue those targets that are conventionally undruggable, which enormously extends the space of drug development. Furthermore, PROTAC has the potential to address drug resistance of small molecular inhibitors by degrading the whole POI. Nevertheless, PROTACs display high-efficiency and always-on properties to degrade POI, they may cause severe side effects due to an "on-target but off-tissue" protein degradation profile at the undesirable tissues and cells. Given that, the stimuli-activatable PROTAC prodrugs have been recently exploited to confine precise protein degradation of the favorable targets, which may conquer the adverse effects of PROTAC due to uncontrollable protein degradation. Herein, we summarized the cutting-edge advances of the stimuli-activatable PROTAC prodrugs. We also overviewed the progress of PROTAC prodrug-based nanomedicine to improve PROTAC delivery to the tumors and precise POI degradation in the targeted cells. & COPY; 2023 Science China Press. Published by Elsevier B.V. and Science China Press. All rights reserved. |
| WOS关键词 | TARGETING CHIMERAS PROTACS ; E3 UBIQUITIN LIGASE ; ANTIBODY-MEDIATED DELIVERY ; IN-VIVO ; DRUG DISCOVERY ; SELECTIVE DEGRADATION ; HYDROGEN-PEROXIDE ; SMALL MOLECULES ; PROTEOLYSIS ; NANOMEDICINE |
| 资助项目 | National Natural Science Foundation of China[U22A20328] ; National Natural Science Foundation of China[22074043] ; Science and Technology Commission of Shanghai Municipality[20430711800] ; Science and Technology Commission of Shanghai Municipality[23ZR1475000] ; Lingang Laboratory[LG-QS-202206-04] |
| WOS研究方向 | Science & Technology - Other Topics |
| 语种 | 英语 |
| 出版者 | ELSEVIER |
| WOS记录号 | WOS:001019160200001 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/306406]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Xu, Zhiai; Yu, Haijun |
| 作者单位 | 1.Icahn Sch Med Mt Sinai, Tisch Canc Inst, Mt Sinai Ctr Therapeut Discovery, Dept Neurosci, New York, NY 10029 USA 2.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Pharmaceut, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Med Chem, Shanghai 201203, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Mat Med, Informat Ctr, Shanghai 201203, Peoples R China 5.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China 6.Gluetacs Therapeut Shanghai Co Ltd, Shanghai 201306, Peoples R China 7.Second Mil Med Univ, Sch Pharm, Shanghai 200433, Peoples R China 8.Tsinghua Univ, Sch Pharmaceut Sci, Beijing 100084, Peoples R China 9.Nanyang Technol Univ, Sch Chem & Biomed Engn, Singapore 639798, Singapore 10.Icahn Sch Med Mt Sinai, Mt Sinai Ctr Therapeut Discovery, Tisch Canc Inst, Dept Pharmacol Sci, New York, NY 10029 USA |
| 推荐引用方式 GB/T 7714 | Gao, Jing,Yang, Lei,Lei, Shumin,et al. Stimuli-activatable PROTACs for precise protein degradation and cancer therapy[J]. SCIENCE BULLETIN,2023,68(10):1069-1085. |
| APA | Gao, Jing.,Yang, Lei.,Lei, Shumin.,Zhou, Feng.,Nie, Huijun.,...&Yu, Haijun.(2023).Stimuli-activatable PROTACs for precise protein degradation and cancer therapy.SCIENCE BULLETIN,68(10),1069-1085. |
| MLA | Gao, Jing,et al."Stimuli-activatable PROTACs for precise protein degradation and cancer therapy".SCIENCE BULLETIN 68.10(2023):1069-1085. |
入库方式： OAI收割
来源：上海药物研究所
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