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

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dc.contributor.authorXiao, T.
dc.contributor.authorLiu, R.
dc.contributor.authorProud, C.
dc.contributor.authorWang, M.
dc.date.issued2016
dc.description.abstractEukaryotic 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.
dc.description.statementofresponsibilityTing Xiao, Rui Liu, Christopher G.Proud, Ming-Wei Wang
dc.identifier.citationActa Pharmaceutica Sinica B, 2016; 6(6):557-563
dc.identifier.doi10.1016/j.apsb.2016.04.002
dc.identifier.issn2211-3835
dc.identifier.issn2211-3843
dc.identifier.orcidProud, C. [0000-0003-0704-6442]
dc.identifier.urihttp://hdl.handle.net/2440/105974
dc.language.isoen
dc.publisherElsevier
dc.rights© 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 license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
dc.source.urihttps://doi.org/10.1016/j.apsb.2016.04.002
dc.subjectHigh-throughput screening
dc.subjectInhibitors
dc.subjectLuminescence
dc.subjectMH-1 peptide
dc.subjecteEF2K
dc.titleA high-throughput screening assay for eukaryotic elongation factor 2 kinase inhibitors
dc.typeJournal article
pubs.publication-statusPublished

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