Results 31 to 40 of about 564,359 (343)
Molecules, 2022 Schistosomiasis is a neglected tropical disease affecting more than 200 million people worldwide. Chemotherapy relies on one single drug, praziquantel, which is safe but ineffective at killing larval stages of this parasite.
Bernardo Pereira Moreira +6 more
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Roscovitine Targets, Protein Kinases and Pyridoxal Kinase [PDF]
Journal of Biological Chemistry, 2005 (R)-Roscovitine (CYC202) is often referred to as a "selective inhibitor of cyclin-dependent kinases." Besides its use as a biological tool in cell cycle, neuronal functions, and apoptosis studies, it is currently evaluated as a potential drug to treat cancers, neurodegenerative diseases, viral infections, and glomerulonephritis.
Bach, S. +21 more
openaire +7 more sources
Neuronal migration and protein kinases
Frontiers in Neuroscience, 2015 The formation of the six-layered structure of the mammalian cortex via the inside-out pattern of neuronal migration is fundamental to neocortical functions.
Toshio eOhshima
doaj +1 more source
Advance in Reversible Covalent Kinase Inhibitors [PDF]
arXiv, 2021 Reversible covalent kinase inhibitors (RCKIs) are a class of novel kinase inhibitors attracting increasing attention because they simultaneously show the selectivity of covalent kinase inhibitors, yet avoid permanent protein-modification-induced adverse effects.
arxiv
Positional information readout in $Ca^{2+}$ signaling [PDF]
Phys. Rev. Lett. 123, 058102 (2019), 2017 Living cells respond to spatial signals. Signal transmission to the cell interior often involves the release of second messengers like $Ca^{2+}$ . They will eventually trigger a physiological response by activating kinases that in turn activate target proteins through phosphorylation. Here, we investigate theoretically how positional information can be
arxiv +1 more source
Deactivatable Bisubstrate Inhibitors of Protein Kinases
Molecules, 2022 Bivalent ligands, including bisubstrate inhibitors, are conjugates of pharmacophores, which simultaneously target two binding sites of the biomolecule. Such structures offer attainable means for the development of compounds whose ability to bind to the ...
Tanel Sõrmus +4 more
doaj +1 more source
Current Biology, 2000 Vanhaesebroeck B, Alessi, DR: The PI3K-PDK1 connection: more than just a road to PKB.Biochem J 2000, 346:561-576.Scheid MP, Woodgett JR: Protein kinases: six degrees of separation?Curr Biol 2000, 10:R191-R194.Coffer P, Jin J, Woodgett JR: Protein kinase B (c-Akt): a multifunctional mediator of phosphatidylinositol 3-kinase activation.Biochem J 1998 ...
openaire +3 more sources
Calmodulin-dependent protein kinase kinase-β is an alternative upstream kinase for AMP-activated protein kinase [PDF]
Cell Metabolism, 2005 The AMP-activated protein kinase (AMPK) is a critical regulator of energy balance at both the cellular and whole-body levels. Two upstream kinases have been reported to activate AMPK in cell-free assays, i.e., the tumor suppressor LKB1 and calmodulin-dependent protein kinase kinase. However, evidence that this is physiologically relevant currently only
Hawley, Simon A. +7 more
openaire +4 more sources
Inferring the Sign of Kinase-Substrate Interactions by Combining Quantitative Phosphoproteomics with a Literature-Based Mammalian Kinome Network [PDF]
, 2010 Protein phosphorylation is a reversible post-translational modification commonly used by cell signaling networks to transmit information about the extracellular environment into intracellular organelles for the regulation of the activity and sorting of proteins within the cell.
arxiv +1 more source
Using the structural kinome to systematize kinase drug discovery [PDF]
arXiv, 2021 Kinase-targeted drug design is challenging. It requires designing inhibitors that can bind to specific kinases when all kinase catalytic domains share a common folding scaffold that binds ATP. Thus, obtaining the desired selectivity, given the whole human kinome, is a fundamental task during early-stage drug discovery.
arxiv