Structure-based repurposing of FDA-approved drugs as inhibitors of NEDD8-activating enzyme

doi:10.1016/j.biochi.2014.03.005

UM > Institute of Chinese Medical Sciences

Residential College	false
Status	已發表Published
	Structure-based repurposing of FDA-approved drugs as inhibitors of NEDD8-activating enzyme
	Zhong H.-J.4; Liu L.-J.4; Chan D.S.-H.2; Wang H.-M.1; Chan P.W.H.3; Ma D.-L.2; Leung C.-H.4
	2014
Source Publication	Biochimie
ISSN	61831638 03009084
Volume	102 Issue:1 Pages:211-215
Abstract	We report the discovery of an inhibitor of NEDD8-activating enzyme (NAE) by an integrated virtual screening approach. Piperacillin 1 inhibited NAE activity in cell-free and cell-based systems with high selectivity. Furthermore, piperacillin 1 was able to inhibit the degradation of the NAE downstream protein substrate p27. Our molecular modeling and kinetic studies suggested that this compound may act as a non-covalent ATP-competitive inhibitor of NAE.
Keyword	Inhibitor Nedd8-activating Enzyme Repurposing Structure-based Virtual Screening
DOI	10.1016/j.biochi.2014.03.005
URL	View the original
Indexed By	SCIE
Language	英語English
WOS Research Area	Biochemistry & Molecular Biology
WOS Subject	Biochemistry & Molecular Biology
WOS ID	WOS:000338623600024
Scopus ID	2-s2.0-84901791098
Fulltext Access	View Full-Text via DOI View Full-Text via Web of Science View Full-Text via Scopus
Citation statistics
Document Type	Journal article
Collection	Institute of Chinese Medical Sciences
Corresponding Author	Ma D.-L.; Leung C.-H.
Affiliation	1.Department of Fragrance and Cosmetic Science, Graduate Institute of Natural Products, Kaohsiung Medical University, Taiwan, ROC 2.Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China 3.Division of Chemistry and Biological Chemistry, School of Physical and Mathematical Sciences, Nanyang Technological University,Singapore 637371, Singapore 4.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China
First Author Affilication	Institute of Chinese Medical Sciences
Corresponding Author Affilication	Institute of Chinese Medical Sciences
Recommended Citation GB/T 7714	Zhong H.-J.,Liu L.-J.,Chan D.S.-H.,et al. Structure-based repurposing of FDA-approved drugs as inhibitors of NEDD8-activating enzyme[J]. Biochimie, 2014, 102(1), 211-215.
APA	Zhong H.-J.., Liu L.-J.., Chan D.S.-H.., Wang H.-M.., Chan P.W.H.., Ma D.-L.., & Leung C.-H. (2014). Structure-based repurposing of FDA-approved drugs as inhibitors of NEDD8-activating enzyme. Biochimie, 102(1), 211-215.
MLA	Zhong H.-J.,et al."Structure-based repurposing of FDA-approved drugs as inhibitors of NEDD8-activating enzyme".Biochimie 102.1(2014):211-215.

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