High-throughput screens for eef-2 kinase
WebJul 15, 2014 · Eukaryotic elongation factor-2 kinase (eEF2K), encoded by the EEF2K gene, is well-known to be a Ca 2+ /calmodulin (CaM)-dependent kinase which can negatively modulate protein synthesis. It is highly conserved among eukaryotes from mammals to invertebrates, of which human and mouse may have 99 % overall amino acid identity. WebJan 24, 2014 · Using this high-throughput assay, we screened more than 7000 compounds and discovered additional small molecules that inhibit the ATM kinase and further validated these hits by secondary assays. Introduction
High-throughput screens for eef-2 kinase
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WebeEF-2 kinase is a highly conserved protein kinase in the calmodulin -mediated signaling pathway that links multiple up-stream signals to the regulation of protein synthesis. It phosphorylates eukaryotic elongation factor 2 ( EEF2) and thus inhibits the EEF2 function. [6] [8] Activation [ edit]
WebSep 27, 2013 · eEF-2 kinase is a potential therapeutic target for breast cancer, gliomas, and depression. No potent inhibitors of eEF-2K have been reported, and thus development of … WebMay 20, 2024 · Background: Eukaryotic elongation factor 2 kinase (eEF2K) regulates the elongation stage of protein synthesis by phosphorylating eEF2, a process related to various diseases including cancer and cardiovascular and neurodegenerative diseases. In this study, we describe the identification of novel eEF2K inhibitors using high-throughput screening …
WebSep 27, 2013 · eEF-2 kinase is a potential therapeutic target for breast cancer, gliomas, and depression. No potent inhibitors of eEF-2K have been reported, and thus development of … WebHere, we describe the purification of the protein kinase, eEF-2K, and the utilization of three biochemical assays in the course of identifying small molecules that block its enzymatic …
WebTwo high-throughput assays are described for eEF-2K using recombinant, tag-free enzyme purified from bacteria. The first is a fluorescence-based assay that uses the phosphorylation of a Sox-based peptide substrate by eEF-2K, which results in a 5-fold increase in fluorescence emission, allowing for continuous monitoring of the kinase activity.
WebWe report here the development and optimization of a simple 384-well colorimetric assay to measure H(2)O(2) generated by the redox cycling of compounds incubated with reducing agents in high-throughput screening (HTS) assay buffers. The phenol red-horseradish peroxidase (HRP) assay readily detected H(2)O(2) either added exogenously or generated … cryptographic errorWebIntroduced, optimized and conducted an in vitro high-throughput drug screen assay for compounds with activity against liver stage malaria. Discovered and confirmed several compounds active against ... cryptographic exceptionWebSep 27, 2013 · This website requires cookies, and the limited processing of your personal data in order to function. By using the site you are agreeing to this as outlined in our … dusit thani manila phone numberWebEvidence that elongation factor 2 kinase (eEF-2K) has potential as a target for anticancer therapy and possibly for the treatment of depression is emerging. Here the steady-state … cryptographic exception padding is invalidWebOct 26, 2015 · High-Throughput Screens for eEF-2 Kinase. Article. Sep 2013; Ramakrishna Edupuganti; Ashwini K Devkota; Mangalika Warthaka; Kevin Dalby; eEF-2 kinase is a potential therapeutic target for breast ... cryptographic erasureWebNov 26, 2007 · Kinases are important drug discovery targets for a wide variety of therapeutic indications; consequently, the measurement of kinase activity remains a common high-throughput screening (HTS) application. Recently, enzyme-coupled luciferase-kinase (LK) format assays have been introduced. cryptographic erase vs secure eraseWebJul 13, 2024 · In the same study, the identification of a selective but weak inhibitor of eEF2K (IC 50 = 0.28 μM) called A-484954 through a high-throughput screen was also reported … dusit thani maldives stw