PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy

doi:10.3389/fphar.2021.692574

	PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy
	Qi, Si-Min 1; Dong, Jinyun 3; Xu, Zhi-Yuan 3; Cheng, Xiang-Dong 3; Zhang, Wei-Dong 2; Qin, Jiang-Jiang 1,3
刊名	FRONTIERS IN PHARMACOLOGY
	2021-05-07
卷号	12
关键词	PROTAC E3 ubiquitin ligase protein degradation ubiquitin-proteasome system cancer therapy
ISSN号	1663-9812
DOI	10.3389/fphar.2021.692574
通讯作者	Zhang, Wei-Dong(wdzhangy@hotmail.com) ; Qin, Jiang-Jiang(jqin@zcmu.edu.cn)
英文摘要	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.
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]
WOS关键词	SMALL-MOLECULE PROTACS ; ANDROGEN RECEPTOR AR ; TYROSINE KINASE ; DEGRADERS ; POTENT ; CELLS ; VHL ; UBIQUITINATION ; INHIBITORS ; DISCOVERY
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	FRONTIERS MEDIA SA
WOS记录号	WOS:000652576100001
资助机构	Zhejiang Provincial Natural Science Foundation of China ; Program of Zhejiang Provincial TCM Sci-tech Plan ; National Natural Science Foundation of China
内容类型	期刊论文
源URL	[http://ir.hfcas.ac.cn:8080/handle/334002/122170]
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.Naval Med Univ, Sch Pharm, Shanghai, Peoples R China 3.Chinese Acad Sci, Inst Basic Med & Canc IBMC, Zhejiang Canc Hosp, Univ Chinese Acad Sci,Canc Hosp, Hangzhou, 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).