A high-throughput screening assay for eukaryotic elongation factor 2 kinase inhibitors

doi:10.1016/j.apsb.2016.04.002

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	A high-throughput screening assay for eukaryotic elongation factor 2 kinase inhibitors
	Xiao, Ting 1,4,5; Liu, Rui 2,3; Proud, Christopher G.2,3; Wang, Ming-Wei1,5
刊名	ACTA PHARMACEUTICA SINICA B
	2016-11
卷号	6 期号:6 页码:557-563
关键词	eEF2K Inhibito High-throughput screening Luminescenc MH-1 peptide
ISSN号	2211-3835
DOI	10.1016/j.apsb.2016.04.002
文献子类	Article
英文摘要	Eukaryotic elongation factor 2 kinase (eEF2K) inhibitors may aid in the development of new therapeutic agents to combat cancer. Purified human eEF2K was obtained from an Escherichia coli expression system and a luminescence-based high-throughput screening (HTS) assay was developed using MH-1 peptide as the substrate. The luminescent readouts correlated with the amount of adenosine triphosphate remaining in the kinase reaction. This method was applied to a large-scale screening campaign against a diverse compound library and subsequent confirmation studies. Nine initial hits showing inhibitory activities on eEF2K were identified from 56,000 synthetic compounds during the HTS campaign, of which, five were chosen to test their effects in cancer cell lines. (C) 2016 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND
资助项目	National Health and Family Planning Commission of China[2012ZX09304-011] ; National Health and Family Planning Commission of China[2013ZX09401003-005] ; National Health and Family Planning Commission of China[2013ZX09507001] ; National Health and Family Planning Commission of China[2013ZX09507-002] ; Shanghai Science and Technology Fund[15DZ2291600] ; Thousand Talents Program in China[00000000]
WOS关键词	FACTOR-II ; PHOSPHORYLATION ; TRANSLATION ; DERIVATIVES ; CANCER ; EEF2 ; EF-2
WOS研究方向	Pharmacology & Pharmacy
语种	英语
CSCD记录号	CSCD:5846273
出版者	INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES
WOS记录号	WOS:000390869400006
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/275824]
专题	国家新药筛选中心
通讯作者	Wang, Ming-Wei
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 2.Univ Southampton, Ctr Biol Sci, Life Sci Bldg, Southampton SO16 7LB, Hants, England; 3.South Australian Hlth & Med Res Inst, North Terrace, Adelaide, SA 5000, Australia 4.Nanchang Univ, Dept Pharm, Coll Med, Nanchang 330066, Jiangxi, Peoples R China; 5.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China;
推荐引用方式 GB/T 7714	Xiao, Ting,Liu, Rui,Proud, Christopher G.,et al. A high-throughput screening assay for eukaryotic elongation factor 2 kinase inhibitors[J]. ACTA PHARMACEUTICA SINICA B,2016,6(6):557-563.
APA	Xiao, Ting,Liu, Rui,Proud, Christopher G.,&Wang, Ming-Wei.(2016).A high-throughput screening assay for eukaryotic elongation factor 2 kinase inhibitors.ACTA PHARMACEUTICA SINICA B,6(6),557-563.
MLA	Xiao, Ting,et al."A high-throughput screening assay for eukaryotic elongation factor 2 kinase inhibitors".ACTA PHARMACEUTICA SINICA B 6.6(2016):557-563.