Results 11 to 20 of about 2,078,021 (401)
The Kinase Specificity of Protein Kinase Inhibitor Peptide [PDF]
Frontiers in Pharmacology, 2021 G-protein-coupled-receptor (GPCR) signaling is exquisitely controlled to achieve spatial and temporal specificity. The endogenous protein kinase inhibitor peptide (PKI) confines the spatial and temporal spread of the activity of protein kinase A (PKA), which integrates inputs from three major types of GPCRs.
Yao Chen, Yao Chen, Bernardo L. Sabatini
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Novel protein kinase signaling systems regulating lifespan identified by small molecule library screening using Drosophila. [PDF]
PLoS ONE, 2012 Protein kinase signaling cascades control most aspects of cellular function. The ATP binding domains of signaling protein kinases are the targets of most available inhibitors. These domains are highly conserved from mammals to flies.
Stephen R Spindler +4 more
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Bivalent inhibitors of protein kinases [PDF]
Critical Reviews in Biochemistry and Molecular Biology, 2014 Protein kinases are key players in a large number of cellular signaling pathways. Dysregulated kinase activity has been implicated in a number of diseases, and members of this enzyme family are of therapeutic interest. However, due to the fact that most inhibitors interact with the highly conserved ATP-binding sites of kinases, it is a significant ...
Carrie M. Gower +2 more
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Biomolecules, 2022 Protein kinases are major drug targets. Most kinase inhibitors are directed against the adenosine triphosphate (ATP) cofactor binding site, which is largely conserved across the human kinome.
Christian Feldmann, Jürgen Bajorath
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Fast in-vitro screening of FLT3-ITD inhibitors using silkworm-baculovirus protein expression system.
PLoS ONE, 2022 We report expression and purification of a FLT3 protein with ITD mutation (FLT3-ITD) with a steady tyrosine kinase activity using a silkworm-baculovirus system, and its application as a fast screening system of tyrosine kinase inhibitors.
Naoki Yamamoto +3 more
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Frontiers in Chemistry, 2023 Receptor-Interacting serine/threonine-Protein Kinase 1 (RIPK1) emerged as an important driver of inflammation and, consequently, inflammatory pathologies.
Camilla Scarpellini +11 more
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Protein kinase inhibitors for amyotrophic lateral sclerosis therapy
British Journal of Pharmacology, 2020 Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disorder that causes the progressive loss of motoneurons and, unfortunately, there is no effective treatment for this disease.
V. Palomo +4 more
semanticscholar +1 more source
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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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 biological target could be modulated by an external trigger.
Tanel Sõrmus +4 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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