Pterisolic Acid B is a Nrf2 Activator by Targeting C171 within Keap1-BTB   Domain

doi:10.1038/srep19231

CORC > 北京大学 > 化学与分子工程学院

	Pterisolic Acid B is a Nrf2 Activator by Targeting C171 within Keap1-BTB Domain
	Dong, Ting ; Liu, Weilong ; Shen, Zhirong ; Li, Lin ; Chen, She ; Lei, Xiaoguang
刊名	SCIENTIFIC REPORTS
	2016
关键词	ANTIOXIDANT RESPONSE ELEMENT SUBSTRATE ADAPTER PROTEIN OXIDATIVE STRESS CHEMOPROTECTIVE AGENTS INDUCTION PATHWAY GLUTATHIONE ENZYMES UBIQUITINATION CHEMOTHERAPY
DOI	10.1038/srep19231
英文摘要	The use of chemoprotective agents to minimize the side effects of the chemotherapy, primarily via activation of the Nrf2 pathway, is an emerging research field, which has attracted broad attention from both academia and pharmaceutical industry. Through high-throughput chemical screens we have disclosed that pterisolic acid B (J19), a naturally occuring diterpenoid, is an effective Nrf2 activator. We have also identified a more potent natural product analogue J19-1 by semisynthesis and the subsequent biochemical evaluations revealed that J19-1 activates the Nrf2 pathway by covalently modifying Cys171 of keap1, which inhibits Nrf2 degradation mediated by Keap1-Cul3 complexes. Ultimately, we have demonstrated that J19-1 shows significant cytoprotective effect against cisplatin-induced cytotoxicity in HKC cells.; National High Technology Projects 973 [2015CB856200, 2012CB837400]; NNSFC [21222209, 91313303, 21472010]; SCI(E); ARTICLE; xglei@pku.edu.cn; 6
语种	英语
内容类型	期刊论文
源URL	[http://ir.pku.edu.cn/handle/20.500.11897/438802]
专题	化学与分子工程学院生命科学学院
推荐引用方式 GB/T 7714	Dong, Ting,Liu, Weilong,Shen, Zhirong,et al. Pterisolic Acid B is a Nrf2 Activator by Targeting C171 within Keap1-BTB Domain[J]. SCIENTIFIC REPORTS,2016.
APA	Dong, Ting,Liu, Weilong,Shen, Zhirong,Li, Lin,Chen, She,&Lei, Xiaoguang.(2016).Pterisolic Acid B is a Nrf2 Activator by Targeting C171 within Keap1-BTB Domain.SCIENTIFIC REPORTS.
MLA	Dong, Ting,et al."Pterisolic Acid B is a Nrf2 Activator by Targeting C171 within Keap1-BTB Domain".SCIENTIFIC REPORTS (2016).