High-throughput screens for eef-2 kinase
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 … WebMay 1, 2014 · eEF-2 kinase dictates cross-talk between autophagy and apoptosis induced by Akt Inhibition, thereby modulating cytotoxicity of novel Akt inhibitor MK-2206. ... High-throughput screens for eEF-2 kinase. J Biomol Screen, 19 (2013), pp. 445-452. Google Scholar. Diggle et al., 1998.
High-throughput screens for eef-2 kinase
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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 WebEnter the email address you signed up with and we'll email you a reset link.
WebIntroduced, 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 ... WebSep 18, 2024 · A high-throughput screen (kinase reaction performed at room temperature) revealed the compound TCMDS-135051 as a highly selective and specific Pf CLK3 kinase inhibitor. This was confirmed in vivo by the finding that parasite strains that developed resistance against TCMDS-135051 acquired mutations in Pf CLK3.
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 high-throughput assay systems may expedite the process. Two high-throughput assays are described for eEF-2K using recombinant, tag-free enzyme purified from bacteria. 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.
WebMay 1, 2014 · The activity of eEF-2, the main eEF involved in the translocation step of elongation, can be inhibited by the eukaryotic elongation factor 2 kinase (eEF2K) (Ma, 2024). eEF2K is an...
WebEvidence 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 … chinese broccoli beef recipe in oyster sauceWebAbstract. 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 … chinese broccoli and oyster sauceWebTwo 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. grand city convention hallchinese broccoli nutrition factsWebJul 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 … chinese broccoli where to buyWebNov 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. chinese brokerWebMay 1, 2016 · Eukaryotic elongation factor 2 kinase (eEF2K) inhibitors may aid in the development of new therapeutic agents to combat cancer. Purified human eEF2K was … grand city gangster-gang crime