Pharmacological approaches to understanding protein kinase signaling networks
Frontiers in Pharmacology, 2023 Protein kinases play vital roles in controlling cell behavior, and an array of kinase inhibitors are used successfully for treatment of disease. Typical drug development pipelines involve biological studies to validate a protein kinase target, followed ...
Elloise H. Stephenson +1 more
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Marine-derived protein kinase inhibitors for neuroinflammatory diseases
BioMedical Engineering OnLine, 2018 Neuroinflammation is primarily characterized by overexpression of proinflammatory mediators produced by glial activation or immune cell infiltration. Several kinases have been shown to be critical mediators in neuroinflammation. One of the largest groups
Chong Ning +6 more
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Folia Biologica, 2006 Since protein kinases have been found to be implicated in many diseases, first of all malignancies, they are considered as promising therapeutic targets. Many protein kinase inhibitors have been designed by now. These molecules have a low molecular weight and most of them bind to protein kinases competing with ATP for the ATP-binding site. Some protein
I, Shchemelinin, L, Sefc, E, Necas
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PLoS ONE, 2010 Predicting off-targets by computational methods is getting increasing importance in early drug discovery stages. We herewith present a computational method based on binding site three-dimensional comparisons, which prompted us to investigate the cross ...
Enrico Defranchi +5 more
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Profile of the GSK published protein kinase inhibitor set across ATP-dependent and-independent luciferases: implications for reporter-gene assays. [PDF]
PLoS ONE, 2013 A library of 367 protein kinase inhibitors, the GSK Published Kinase Inhibitor Set (PKIS), which has been annotated for protein kinase family activity and is available for public screening efforts, was assayed against the commonly used luciferase ...
Patricia Dranchak +6 more
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Protein Kinase Inhibitors and Oxidative Stress Modulate In Vivo Phosphorylation of <i>Trypanosoma cruzi</i> DNA Polymerase β. [PDF]
PharmaceuticsBackground/Objectives: Protein kinases play crucial roles in signal transduction pathways that regulate growth and differentiation in Trypanosoma cruzi. These protein kinases are attractive targets to develop new drugs to treat Chagas disease.
Maldonado E +9 more
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Scientific Reports, 2022 Therapeutic resistance to kinase inhibitors constitutes a major unresolved clinical challenge in cancer and especially in glioblastoma. Multi-kinase inhibitors may be used for simultaneous targeting of multiple target kinases and thereby potentially ...
Oxana V. Denisova +10 more
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Cytoprotective effect of the elongation factor-2 kinase-mediated autophagy in breast cancer cells subjected to growth factor inhibition. [PDF]
PLoS ONE, 2010 Autophagy is a highly conserved and regulated cellular process employed by living cells to degrade proteins and organelles as a response to metabolic stress. We have previously reported that eukaryotic elongation factor-2 kinase (eEF-2 kinase, also known
Yan Cheng +5 more
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Requirement for the eIF4E binding proteins for the synergistic down-regulation of protein synthesis by hypertonic conditions and mTOR inhibition. [PDF]
PLoS ONE, 2013 The protein kinase mammalian target of rapamycin (mTOR) regulates the phosphorylation and activity of several proteins that have the potential to control translation, including p70S6 kinase and the eIF4E binding proteins 4E-BP1 and 4E-BP2.
Michael J Clemens +2 more
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Analysis of the phosphoproteome of CK2α(–/–)/Δα′ C2C12 myoblasts compared to the wild-type cells
Open Biology, 2023 CK2 is a Ser/Thr protein kinase composed of two catalytic (α/α′) subunits and a non-catalytic β-subunit dimer, whose activity is often abnormally high in cancer cells.
Christian Borgo +8 more
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