Knowledge Management System of Hefei Institute of Physical Science,CAS
PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy | |
Qi, Si-Min1; Dong, Jinyun2; Xu, Zhi-Yuan2; Cheng, Xiang-Dong2; Zhang, Wei-Dong3; Qin, Jiang-Jiang1,2 | |
2021-05-07 | |
发表期刊 | FRONTIERS IN PHARMACOLOGY |
ISSN | 1663-9812 |
通讯作者 | Zhang, Wei-Dong(wdzhangy@hotmail.com) ; Qin, Jiang-Jiang(jqin@zcmu.edu.cn) |
摘要 | Proteolysis targeting chimeric (PROTAC) technology is an effective endogenous protein degradation tool developed in recent years that can ubiquitinate the target proteins through the ubiquitin-proteasome system (UPS) to achieve an effect on tumor growth. A number of literature studies on PROTAC technology have proved an insight into the feasibility of PROTAC technology to degrade target proteins. Additionally, the first oral PROTACs (ARV-110 and ARV-471) have shown encouraging results in clinical trials for prostate and breast cancer treatment, which inspires a greater enthusiasm for PROTAC research. Here we focus on the structures and mechanisms of PROTACs and describe several classes of effective PROTAC degraders based on E3 ligases. |
关键词 | PROTAC E3 ubiquitin ligase protein degradation ubiquitin-proteasome system cancer therapy |
DOI | 10.3389/fphar.2021.692574 |
关键词[WOS] | SMALL-MOLECULE PROTACS ; ANDROGEN RECEPTOR AR ; TYROSINE KINASE ; DEGRADERS ; POTENT ; CELLS ; VHL ; UBIQUITINATION ; INHIBITORS ; DISCOVERY |
收录类别 | SCI |
语种 | 英语 |
资助项目 | Zhejiang Provincial Natural Science Foundation of China[LQ21B020003] ; Zhejiang Provincial Natural Science Foundation of China[LR21H280001] ; Program of Zhejiang Provincial TCM Sci-tech Plan[2020ZZ005] ; National Natural Science Foundation of China[81903842] |
项目资助者 | Zhejiang Provincial Natural Science Foundation of China ; Program of Zhejiang Provincial TCM Sci-tech Plan ; National Natural Science Foundation of China |
WOS研究方向 | Pharmacology & Pharmacy |
WOS类目 | Pharmacology & Pharmacy |
WOS记录号 | WOS:000652576100001 |
出版者 | FRONTIERS MEDIA SA |
引用统计 | |
文献类型 | 期刊论文 |
条目标识符 | http://ir.hfcas.ac.cn:8080/handle/334002/122171 |
专题 | 中国科学院合肥物质科学研究院 |
通讯作者 | Zhang, Wei-Dong; Qin, Jiang-Jiang |
作者单位 | 1.Zhejiang Chinese Med Univ, Sch Pharmaceut Sci, Hangzhou, Peoples R China 2.Chinese Acad Sci, Inst Basic Med & Canc IBMC, Zhejiang Canc Hosp, Univ Chinese Acad Sci,Canc Hosp, Hangzhou, Peoples R China 3.Naval Med Univ, Sch Pharm, Shanghai, Peoples R China |
推荐引用方式 GB/T 7714 | Qi, Si-Min,Dong, Jinyun,Xu, Zhi-Yuan,et al. PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy[J]. FRONTIERS IN PHARMACOLOGY,2021,12. |
APA | Qi, Si-Min,Dong, Jinyun,Xu, Zhi-Yuan,Cheng, Xiang-Dong,Zhang, Wei-Dong,&Qin, Jiang-Jiang.(2021).PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy.FRONTIERS IN PHARMACOLOGY,12. |
MLA | Qi, Si-Min,et al."PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy".FRONTIERS IN PHARMACOLOGY 12(2021). |
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