Results 211 to 220 of about 608,807 (260)
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Non-kinase targets of protein kinase inhibitors
Nature Reviews Drug Discovery, 2017Kinome-wide profiling platforms have comprehensively identified the relevant kinases that are targeted by numerous protein kinase inhibitors. However, recent projects have begun to discover non-kinase targets of kinase inhibitors. These non-kinase targets can contribute to the desired or undesired activities of inhibitors, or act as silent bystanders ...
Lenka Munoz
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Irreversible Protein Kinase Inhibitors
Current Medicinal Chemistry, 2011Targeting cancer with small molecule irreversible inhibitors of kinases represents an emerging challenge in drug discovery. Irreversible inhibitors bind to kinase active site in a covalent and irreversible form, most frequently by reacting with a nucleophilic cysteine residue, located near the ATP binding pocket.
GARUTI, LAURA +2 more
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Protein kinase inhibitors in melanoma
Expert Opinion on Pharmacotherapy, 2013The most commonly mutated oncogene identified to date in melanoma is BRAF (∼ 50%), an upstream mediator of the mitogen-activated protein kinase (MAPK) pathway. Recently, BRAF-kinase inhibitors as well as MEK-kinase inhibitors were introduced into the clinics.Substantial Phase II and III clinical trials were searched in patients with advanced melanoma ...
Thomas K, Eigentler +2 more
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Paullones as Inhibitors of Protein Kinases
Current Topics in Medicinal Chemistry, 2011Paullones are a class of molecules structurally based on the 7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one parent scaffold. Many of these structures are inhibitors of certain protein kinases, namely cyclin-dependent kinases and glycogen synthase kinase-3. Being well referenced in the literature on the one hand and commercially available on the other
Nadine, Tolle, Conrad, Kunick
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Inhibitors of protein kinases and phosphatases
Trends in Biochemical Sciences, 1994Inhibitors of eukaryotic protein kinases and phosphatases are a chemically diverse array of natural and synthetic compounds, including medicines, potions and poisons. These substances are valuable pharmacological probes and affinity ligands for the kinases and phosphatases of signalling pathways, enhancing our knowledge of the cellular effects of the ...
MacKintosh, Carol, MacKintosh, Robert W.
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Inhibitors of protein tyrosine kinases
Current Opinion in Biotechnology, 1995The description in the past year of several novel protein tyrosine kinase inhibitors, which exhibit dramatic improvements in potency and specificity over earlier agents, will be considered a major turning point in the field. These compounds appear to have the necessary pharmacological properties to finally allow clarification of whether suppression of ...
D W, Fry, A J, Bridges
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Current Oncology Reports, 2002
Protein kinase C (PKC) is a family of serine-threonine protein kinases that are involved in signal transduction pathways that regulate growth factor response, proliferation, and apoptosis. Its central role in these processes, which are closely involved in tumor initiation, progression, and response to antitumor agents, makes it an attractive ...
Helen C, Swannie, Stanley B, Kaye
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Protein kinase C (PKC) is a family of serine-threonine protein kinases that are involved in signal transduction pathways that regulate growth factor response, proliferation, and apoptosis. Its central role in these processes, which are closely involved in tumor initiation, progression, and response to antitumor agents, makes it an attractive ...
Helen C, Swannie, Stanley B, Kaye
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Therapeutic Protein Kinase Inhibitors
Cellular and Molecular Life Sciences, 2008Protein kinase inhibitors represent an important and still emerging class of targeted therapeutic agents. Drug discovery and development strategies have explored numerous approaches to target the inhibition of protein kinase signaling. This review will highlight some of the strategies that have led to the successful clinical development of therapeutic ...
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Drug News & Perspectives, 2005
In humans, the Janus protein tyrosine kinase family (JAKs) contains four members: JAK1, JAK2, JAK3 and TYK2. JAKs phosphorylate signal transducers and activators of transcription (STATs) simultaneously with other phosphorylations required for activation, and there are several cellular mechanisms in place to inhibit JAK/STAT signaling. That one might be
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In humans, the Janus protein tyrosine kinase family (JAKs) contains four members: JAK1, JAK2, JAK3 and TYK2. JAKs phosphorylate signal transducers and activators of transcription (STATs) simultaneously with other phosphorylations required for activation, and there are several cellular mechanisms in place to inhibit JAK/STAT signaling. That one might be
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An inhibitor protein of nuclear protein kinases
Nature, 1979THE cyclical phosphorylation and dephosphorylation of proteins, catalysed by protein kinases and phosphoprotein phosphatases, respectively, are important ways in which cells regulate many of their metabolic activities. Cells seem to have at least two distinct phosphorylation systems, one in the cytoplasm, the other in the nucleus.
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