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Type: Journal article
Title: A high-throughput screening assay for eukaryotic elongation factor 2 kinase inhibitors
Author: Xiao, T.
Liu, R.
Proud, C.
Wang, M.
Citation: Acta Pharmaceutica Sinica B, 2016; 6(6):557-563
Publisher: Elsevier
Issue Date: 2016
ISSN: 2211-3835
Statement of
Ting Xiao, Rui Liu, Christopher G.Proud, Ming-Wei Wang
Abstract: 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.
Keywords: High-throughput screening; Inhibitors; Luminescence; MH-1 peptide; eEF2K
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 (
RMID: 0030060409
DOI: 10.1016/j.apsb.2016.04.002
Appears in Collections:Pharmacology publications

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