UM
Structure-based identification of a NEDD8-activating enzyme inhibitor via drug repurposing
Wu, Ke-Jia; Zhong, Hai-Jing; Li, Guodong; Liu, Chenfu; Wang, Hui-Min David; Ma, Dik-Lung; Leung, Chung-Hang
2018-01
Source PublicationEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN0223-5234
Volume143Pages:1021-1027
AbstractNEDD8-activating enzyme (NAE) is an essential player of the NEDD8 conjugation pathway that regulates protein degradation. Meanwhile, drug repurposing is a cost-efficient strategy to identify new therapeutic uses for existing scaffolds. In this report, mitoxantrone (1) was repurposed as an inhibitor of NAE by virtual screening of an FDA-approved drug database. Compound 1 inhibited NAE activity in cell-free and cell-based systems with high selectivity and was competitive with ATP. Furthermore, compound 1 induced apoptosis of colorectal adenocarcinoma cancer cells through inhibiting the degradation of the neddylation substrate p53. (C) 2017 Elsevier Masson SAS. All rights reserved.
KeywordDrug repurposing Mitoxantrone NEDD8 Ubiquitin
DOI10.1016/j.ejmech.2017.11.101
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000428216700084
PublisherELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
The Source to ArticleWOS
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Cited Times [WOS]:16   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Recommended Citation
GB/T 7714
Wu, Ke-Jia,Zhong, Hai-Jing,Li, Guodong,et al. Structure-based identification of a NEDD8-activating enzyme inhibitor via drug repurposing[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2018,143:1021-1027.
APA Wu, Ke-Jia.,Zhong, Hai-Jing.,Li, Guodong.,Liu, Chenfu.,Wang, Hui-Min David.,...&Leung, Chung-Hang.(2018).Structure-based identification of a NEDD8-activating enzyme inhibitor via drug repurposing.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,143,1021-1027.
MLA Wu, Ke-Jia,et al."Structure-based identification of a NEDD8-activating enzyme inhibitor via drug repurposing".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 143(2018):1021-1027.
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