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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Pharmacological LRRK2 kinase inhibition induces LRRK2 protein destabilization and proteasomal degradation [PDF]
, 2016 Leucine-rich repeat kinase 2 (LRRK2) kinase activity is increased in several pathogenic mutations, including the most common mutation, G2019S, and is known to play a role in Parkinson’s disease (PD) pathobiology.
Baekelandt, V. +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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Intracellular mechanisms underlying the nicotinic enhancement of LTP in the rat dentate gyrus [PDF]
, 2008 We have previously shown that activation of nicotinic acetylcholine receptors (nAChRs) enhanced long-term potentiation (LTP) in the rat dentate gyrus in vitro via activation of α7 nAChR. In the present studies, mechanisms underlying the acute and chronic
Abel +81 more
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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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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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Compounds from Natural Sources as Protein Kinase Inhibitors. [PDF]
Biomolecules, 2020 The advantage of natural compounds is their lower number of side-effects when compared to most synthetic substances. Therefore, over the past several decades, the interest in naturally occurring compounds is increasing in the search for new potent drugs.
Baier A, Szyszka R.
europepmc +2 more sources
Computerized Protein Modeling and Molecular Docking Analysis of Human Proto Oncogene Tyrosine Protein Kinase YES for Discovery of Novel Lead Molecules [PDF]
, 2010 Human proto-oncogene tyrosine-protein kinase YES (YES) is a non receptor kinase belongs to Src family. This gene lies in close proximity to thymidylate synthase gene on chromosome 18, and a corresponding pseudogene has been found on chromosome 22.
Amineni Umamaheswari +2 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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Synergistic antitumour activity of RAF265 and ZSTK474 on human TT medullary thyroid cancer cells [PDF]
, 2015 Medullary thyroid cancer (MTC) is an aggressive malignancy responsible for up to 14% of all thyroid cancer-related deaths. It is characterized by point mutations in the rearranged during transfection (RET) proto-oncogene.
Barollo, Susi +11 more
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