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Matrix Viscoelasticity Regulates Dendritic Cell Migration and Immune Priming
Advanced Materials, EarlyView.Matrix viscoelasticity is a key mechanical feature of the tumor microenvironment but remains poorly understood in immune regulation. Here, we develop a tunable collagen platform to decouple viscoelasticity from stiffness and show that slow‐relaxing matrices constrain dendritic cell migration by limiting actomyosin‐driven matrix remodeling, thereby ...
Wei‐Hung Jung +6 more
wiley +1 more source
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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
exaly +3 more sources
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
openaire +4 more sources
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
openaire +2 more sources
Inhibitors of protein kinase C
Cellular Signalling, 1994P C, Gordge, W J, Ryves
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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 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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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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