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题名: Caffeic acid phenethyl ester (CAPE) revisited: Covalent modulation of XPO1/CRM1 activities and implication for its mechanism of action
作者: Wu, Sijin1;  Zhang, Keren1;  Qin, Hongqiang2;  Niu, Mingshan1;  Zhao, Weijie3;  Ye, Mingliang2;  Zou, Hanfa2;  Yang, Yongliang1
关键词: caffeic acid phenethyl ester ;  covalent binding ;  nuclear export ;  XPO1 ;  CRM1
刊名: CHEMICAL BIOLOGY & DRUG DESIGN
发表日期: 2017-05-01
DOI: 10.1111/cbdd.12905
卷: 89, 期:5, 页:655-662
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Biochemistry & Molecular Biology ;  Chemistry, Medicinal
研究领域[WOS]: Biochemistry & Molecular Biology ;  Pharmacology & Pharmacy
英文摘要: Caffeic acid phenethyl ester (CAPE) is the bioactive constituent of propolis from honeybee hives and is well known for its anti-inflammatory, anticarcinogenic, antioxidant, and immunomodulatory properties. Herein, we revisited the cellular mechanism underlying the diverse biological effects of CAPE. We demonstrated that XPO1/CRM1, a major nuclear export receptor, is a cellular target of CAPE. Through nuclear export functional assay, we observed a clear shift of XPO1 cargo proteins from a cytoplasmic localization to nucleus when treated with CAPE. In particular, we showed that CAPE could specifically target the non-catalytic and conserved Cys(528) of XPO1 through the means of mass spectrometric analysis. In addition, we demonstrated that the mutation of Cys(528) residue in XPO1 could rescue the nuclear export defects caused by CAPE. Furthermore, we performed position-restraint molecular dynamics simulation to show that the Michael acceptor moiety of CAPE is the warhead to enable covalent binding with Cys(528) residue of XPO1. The covalent modulation of nuclear export by CAPE may explain its diverse biological effects. Our findings may have general implications for further investigation of CAPE and its structural analogs.
关键词[WOS]: NUCLEAR EXPORT INHIBITORS ;  FACTOR-KAPPA-B ;  LEPTOMYCIN-B ;  NUCLEOCYTOPLASMIC TRANSPORT ;  TRANSCRIPTION FACTOR ;  DRUG-RESISTANCE ;  CELLS ;  CANCER ;  DERIVATIVES ;  SUPPRESSES
语种: 英语
WOS记录号: WOS:000399734600001
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/152017
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Dalian Univ Technol, Sch Life Sci & Biotechnol, Ctr Mol Med, Dalian, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, Natl Chromatog R&A Ctr, Dalian, Peoples R China
3.Dalian Univ Technol, Sch Pharmacol, Dalian, Peoples R China

Recommended Citation:
Wu, Sijin,Zhang, Keren,Qin, Hongqiang,et al. Caffeic acid phenethyl ester (CAPE) revisited: Covalent modulation of XPO1/CRM1 activities and implication for its mechanism of action[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2017,89(5):655-662.
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