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A Metal-Based Inhibitor of NEDD8-Activating Enzyme
Zhong H.-J.; Yang H.; Chan D.S.-H.; Leung C.-H.; Wang H.-M.; Ma D.-L.
2012
Source PublicationPLoS ONE
ISSN19326203
Volume7Issue:11
AbstractA cyclometallated rhodium(III) complex [Rh(ppy)2(dppz)]+ (1) (where ppy = 2-phenylpyridine and dppz = dipyrido[3,2-a:2′,3′-c]phenazine dipyridophenazine) has been prepared and identified as an inhibitor of NEDD8-activating enzyme (NAE). The complex inhibited NAE activity in cell-free and cell-based assays, and suppressed the CRL-regulated substrate degradation and NF-κB activation in human cancer cells with potency comparable to known NAE inhibitor MLN4924. Molecular modeling analysis suggested that the overall binding mode of 1 within the binding pocket of the APPBP1/UBA3 heterodimer resembled that for MLN4924. Complex 1 is the first metal complex reported to suppress the NEDDylation pathway via inhibition of the NEDD8-activating enzyme. © 2012 Zhong et al.
DOI10.1371/journal.pone.0049574
URLView the original
Language英语
The Source to ArticleScopus
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Cited Times [WOS]:24   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Zhong H.-J.,Yang H.,Chan D.S.-H.,et al. A Metal-Based Inhibitor of NEDD8-Activating Enzyme[J]. PLoS ONE,2012,7(11).
APA Zhong H.-J.,Yang H.,Chan D.S.-H.,Leung C.-H.,Wang H.-M.,&Ma D.-L..(2012).A Metal-Based Inhibitor of NEDD8-Activating Enzyme.PLoS ONE,7(11).
MLA Zhong H.-J.,et al."A Metal-Based Inhibitor of NEDD8-Activating Enzyme".PLoS ONE 7.11(2012).
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