Structural insights into characterizing binding sites in EGFR kinase mutants [PDF]
Journal of Chemical Information and Modeling, 2018, 2018 Over the last two decades epidermal growth factor receptor (EGFR) kinase has become an important target to treat non-small cell lung cancer (NSCLC). Currently, three generations of EGFR kinase-targeted small molecule drugs have been FDA approved. They nominally produce a response at the start of treatment and lead to a substantial survival benefit for ...
arxiv +1 more source
Protein-tyrosine phosphorylation in Bacillus subtilis: a 10-year retrospective
Frontiers in Microbiology, 2015 The discovery of tyrosine-phosphorylated proteins in Bacillus subtilis in the year 2003 was followed by a decade of intensive research activity. Here we provide an overview of the lessons learned in that period.
Josef eDeutscher, Ivan eMijakovic
doaj +1 more source
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
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
Differential maturation and chaperone dependence of the paralogous protein kinases DYRK1A and DYRK1B
Scientific Reports, 2022 The HSP90/CDC37 chaperone system not only assists the maturation of many protein kinases but also maintains their structural integrity after folding.
Marco Papenfuss +6 more
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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
Advances in Cancer Therapy: A Comprehensive Review of CDK and EGFR Inhibitors
CellsProtein kinases have essential responsibilities in controlling several cellular processes, and their abnormal regulation is strongly related to the development of cancer.
Mohammed Hawash
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A knowledge graph representation learning approach to predict novel kinase-substrate interactions [PDF]
arXiv, 2022 The human proteome contains a vast network of interacting kinases and substrates. Even though some kinases have proven to be immensely useful as therapeutic targets, a majority are still understudied. In this work, we present a novel knowledge graph representation learning approach to predict novel interaction partners for understudied kinases.
arxiv
Large‐scale phosphorylation mapping reveals the extent of tyrosine phosphorylation in Arabidopsis
Molecular Systems Biology, 2008 Protein phosphorylation regulates a wide range of cellular processes. Here, we report the proteome‐wide mapping of in vivo phosphorylation sites in Arabidopsis by using complementary phosphopeptide enrichment techniques coupled with high‐accuracy mass ...
Naoyuki Sugiyama +6 more
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Recent Advances in Discovery of New Tyrosine Kinase Inhibitors Using Computational Methods
Proceedings, 2019 Tyrosine–protein kinases catalyze chemical reactions that. [...]
Vesna Rastija
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