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Protein kinase inhibitors for acute leukemia [PDF]
Biomarker Research, 2018 Conventional treatments for acute leukemia include chemotherapy, radiation therapy, and intensive combined treatments (including bone marrow transplant or stem cell transplants). Novel treatment approaches are in active development.
Yuan Ling +3 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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PKIDB: A Curated, Annotated and Updated Database of Protein Kinase Inhibitors in Clinical Trials
Molecules, 2018 The number of protein kinase inhibitors (PKIs) approved worldwide continues to grow steadily, with 39 drugs approved in the period between 2001 and January 2018.
Fabrice Carles +3 more
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Targeting the trypanosome kinetochore with CLK1 protein kinase inhibitors. [PDF]
Nat Microbiol, 2020 The kinetochore is a macromolecular structure that assembles on the centromeres of chromosomes and provides the major attachment point for spindle microtubules during mitosis.
Saldivia M +22 more
europepmc +2 more sources
Differentiating pulmonary hypertension associated with protein kinase inhibitors [PDF]
Pulmonary Circulation, 2022 Protein kinase inhibitors (PKIs) have been implicated in pulmonary vascular toxicities including risk factors for at least three of the five World Health Organization groups of pulmonary hypertension (PH).
Joshua A. Jacobs +2 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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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.
Andrea Baier, Ryszard Szyszka
doaj +2 more sources
Never Gonna Give You Up – Current Developments in Covalent Protein Kinase Inhibitors
CHIMIA, 2022 Covalent inhibitors have recently seen a revival in medicinal chemistry. Inhibitors addressing non-catalytic cysteine residues with weakly reactive electrophiles have been very successfully employed to target protein kinases, one of the major druggable ...
Laura Hillebrand, Matthias Gehringer
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Discovery of moiety preference by Shapley value in protein kinase family using random forest models
BMC Bioinformatics, 2022 Background Human protein kinases play important roles in cancers, are highly co-regulated by kinase families rather than a single kinase, and complementarily regulate signaling pathways.
Yu-Wei Huang +7 more
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Advances in RIPK1 kinase inhibitors
Frontiers in Pharmacology, 2022 Programmed necrosis is a new modulated cell death mode with necrotizing morphological characteristics. Receptor interacting protein 1 (RIPK1) is a critical mediator of the programmed necrosis pathway that is involved in stroke, myocardial infarction ...
Lu Chen +13 more
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