Kinase inhibitor
TARGETING ONCOGENIC KINASE SIGNALING WITH SMALL MOLECULE KINASE INHIBITOR IMATINIB
... tyrosine kinase activity have been implicated in a number of abnormalities, particularly ...tyrosine kinase inhibitors, imatinib mesylate (Gleevec®; Novartis) has demonstrated magnificent clinical efficacy ...
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Human keratinocytes are efficiently immortalized by a Rho kinase inhibitor
... lifespan in culture that limits their proliferative capacity and clinical use. Here, we report that treatment of primary keratinocytes (originating from 3 different anatomical sites) with Y- 27632, a Rho kinase ...
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Evaluation of the Aurora Kinase Inhibitor, ZM447439, in Canine Malignant Lymphoid Cells in Vitro
... aurora kinase inhibitor (ZM447439), and found that this inhibitor decreases cell viability, increases DNA content change, and leads to apoptosis in canine B- and T-cell lymphoid cell ...aurora ...
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Screening a protein kinase inhibitor library against Plasmodium falciparum
... protein kinase biology in malaria is still being ...protein kinase inhibitor-like scaffolds was screened against the causative parasite, Plasmodium ...protein kinase, or indeed other malaria ...
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Direct activation of PP2A for the treatment of tyrosine kinase inhibitor–resistant lung adenocarcinoma
... tive drug-binding site completely abrogated the anticancer effect of the PP2A activator SMAP DT-061 (17). Therefore, we concluded that the observed anticancer effect is PP2A dependent. In the current study, we included a ...
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Anlotinib: a novel multi-targeting tyrosine kinase inhibitor in clinical development
... tyrosine kinase inhibitor that targets vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR), platelet-derived growth factor receptors (PDGFR), and ...tyrosine ...
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Cyclin dependent kinase inhibitor 2B regulates efferocytosis and atherosclerosis
... Genetic variation at the chromosome 9p21 risk locus promotes cardiovascular disease; however, it is unclear how or which proteins encoded at this locus contribute to disease. We have previously demonstrated that loss of ...
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Salvage pembrolizumab added to kinase inhibitor therapy for the treatment of anaplastic thyroid carcinoma
... Results: Twelve patients were treated with combination kinase inhibitors plus pembrolizumab at the time of progression on their KI therapy. Median age at initiation of pembrolizumab was 60 years (range 47 – 84 ...
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Modulation of apoptosis by the cyclin dependent kinase inhibitor p27Kip1
... ent kinase inhibitor p27 and suggests that under certain conditions p27 is necessary when cells exit the cell cycle to rapidly constrain CDK activity and thereby prevent cell ...
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Primary Cilia Mediate Diverse Kinase Inhibitor Resistance Mechanisms in Cancer.
... FGFR inhibitor BGJ398 significantly reduced the viability of these cells in the presence of trametinib (Figures 5K, S6K, and S6O), providing a potential mechanism for the previously described synergistic effects ...
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A kinase inhibitor screen identifies a dual cdc7/CDK9 inhibitor to sensitise triple negative breast cancer to EGFR targeted therapy
... Kinase inhibitor treatment and drug combination screen Cells were seeded into 96-well plates at the appropriate densities (Additional file 1: Table ...individual kinase inhibitors in dose range as ...
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Raf kinase inhibitor protein1 is a myogenic inhibitor with conserved function in avians and mammals
... Raf Kinase Inhibitor Protein1 (RKIP) is a tumour suppressor that is present in a number of adult ...an inhibitor of both Raf/Mek/Erk and NFĸB signalling when unphosphorylated, but following ...
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Role of Raf-kinase inhibitor protein in colorectal cancer and its regulation by hydroxycamptothecine
... Raf kinase inhibitor protein; NCRCT, non neoplastic colorectal tissue; CRCT, colorectal cancer tissue; MLNT, metastatic lymph node tissue; PEBP, Phosphatidylethanolamine-binding ...
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FRET biosensor-based kinase inhibitor screen for ERK and AKT activity reveals differential kinase dependencies for proliferation in TNBC cells
... various kinase inhibitors on these networks is critical to understand kinase inhibitor efficacy in cancer ...a kinase inhibitor library containing > 350 different kinase ...
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Combination of the ABL kinase inhibitor imatinib with the Janus kinase 2 inhibitor TG101348 for targeting residual BCR-ABL-positive cells
... tyrosine kinase inhibitor (ABL TKI), is a competitive inhibitor that binds to the ATP-binding catalytic site of ABL and decreases kinase domain activity by stabilizing the protein in an active ...
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The cyclin dependent kinase inhibitor p57Kip2 mediates proliferative actions of PTHrP in chondrocytes
... cyclin-dependent kinase inhibitor p57 Kip2 is the opposite of the PTHrP- null phenotype, we hypothesized that PTHrP’s proliferative actions in chondrocytes might be mediated by opposing ...
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HM71224, a selective Bruton’s tyrosine kinase inhibitor, attenuates the development of murine lupus
... inhibitory concentration; IFN- γ : Interferon gamma; IgG: Immunoglobulin G; IgM: Immunoglobulin M; IL-6: Interleukin 6; IN: Interstitial nephritis; LN: Lupus nephritis; MNC: Mononuclear cell; NZB/WF1: New Zealand ...
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Checkpoint kinase inhibitor AZD7762 strongly sensitises urothelial carcinoma cells to gemcitabine
... potent inhibitor of both CHK1 and CHK2 [14], a priori, inhibition of both kinases might contribute to its enhancement of gemcitabine activity on ...CHK1-specific inhibitor Gö6976 [30] also efficiently ...
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Checkpoint kinase inhibitor AZD7762 enhance cisplatin-induced apoptosis in osteosarcoma cells
... AZD7762 reduces cisplatin‑mediated G2/M cell cycle arrest AZD7762 is an inhibitor of Chk1 which regulates the cell cycle. Therefore, we explored whether AZD7762 enhances the inhibition effect of cisplatin on ...
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Anabolic effects of a G protein–coupled receptor kinase inhibitor expressed in osteoblasts
... A GRK inhibitor enhances PTH/PTHrP receptor signaling in cell culture systems. To investigate the role of GRKs in regulat- ing GPCR responsiveness in bone, we initially evaluated the effects of a dominant negative ...
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