Kinase inhibition
Mirk kinase inhibition blocks the in vivo growth of pancreatic cancer cells
... Mirk kinase inhibitor and the untreated controls ...Mirk kinase activity in the pancreatic cancer cells enabled more sonic hedgehog signaling and thus more stromal ...Also, inhibition of Mirk might ...
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Mirk kinase inhibition targets ovarian cancer ascites
... active kinase in these ...Mirk kinase inhibition in spheroids made from established cell lines and in patient-derived ascites cancer cell spheroids reduced spheroid volume, disrupted spheroid ...
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Fyn kinase inhibition as a novel therapy for Alzheimer’s disease
... Alzheimer ’ s disease (AD) is a devastating neurodegenerative disorder, afflicting more than one-third of people over the age of 85. While many therapies for AD are in late-stage clinical testing, rational drug design ...
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Synergism of FAK and tyrosine kinase inhibition in Ph+ B-ALL
... VS-4718 is a potent, selective, and orally bioavailable FAK inhibitor currently under evaluation in subjects with various solid tumors in a phase I clinical trial (ClinicalTrials.gov NCT01849744); however, efficacy in ...
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Src kinase inhibition promotes the chondrocyte phenotype
... family kinase Lyn exhibits a dynamic expression pattern in the chondrogenic cell line ATDC5 and in a mixed population of embryonic mouse chondrocytes in high-density monolayer ...culture. Inhibition of Src ...
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Effects of Src-kinase inhibition in cancer-induced bone pain
... Src is a non-receptor protein tyrosine kinase that plays a multitude of roles in cell signaling. 20 It is mainly present in osteoclasts, 21 platelets, 22 and neurons 23 and is part of the N-methyl-D-aspartate ...
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Spleen tyrosine kinase inhibition in the treatment of autoimmune, allergic and autoinflammatory diseases
... Th e RA clinical trial noted a prompt clinical improve- ment in patients receiving background treatment. Can Syk inhibitors be used in monotherapy? Does prolonged treatment preserve the clinical benefi t, and if so, for ...
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Acquired MET Expression Confers Resistance to EGFR Inhibition In a Mouse Model of Glioblastoma Multiforme
... factor inhibition has never been described and it remains to be observed in GBM patients who underwent EGFR TKI ...EGFR kinase inhibition is a dynamic process involving rapid and drastic changes in ...
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Cycloartanes with Anticancer Activity Demonstrate Promising inhibition of the Mrckα and Mrckβ Kinases
... apoptosis, kinase inhibition and antiangiogenic activity amongst other possible mechanisms ...MRCKα kinase has motivated us to search for other cycloartanes with MRCKα/β inhibitory activity in an ...
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In-silico and Molecular Analysis of Reticulon 4asNovel therapeutic option for axonal regeneration
... histological analysis, signifying that axon maturation is made easy by Rho-kinase inhibition These findings suggest that Ras homolog gene family, member/Rhoassociated protein kinase A Rh[r] ...
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Inhibition of c-Jun NH2-terminal kinase or extracellular signal-regulated kinase improves lung injury
... JNK inhibition by SP600125, in both ischemia and reperfusion periods, almost com- pletely suppressed TNFα release into BAL fluid [34] and IL-1-induced MMP expression in synoviocytes and in joint arthritis ...that ...
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Proteasomal degradation of sphingosine kinase 1 and inhibition of dihydroceramide desaturase by the sphingosine kinase inhibitors, SKi or ABC294640, induces growth arrest in androgen-independent LNCaP-AI prostate cancer cells
... Recently, the SK2 selective inhibitor, ABC294640 was demonstrated to induce proteasomal degradation of c-Myc and myeloid cell leukemia 1 (Mcl-1) in multiple myeloma cells [14]. We had previously demonstrated that the ...
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ITK inhibition induced in vitro and in vivo anti-tumor activity through downregulating TCR signaling pathway in malignant T cell lymphoma
... genetic inhibition of ITK, the selective ITK inhibitor BMS-509744 also demonstrated similarly the antitumor and pro-apoptotic activities in vitro and in ...
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Autophagy inhibition improves the cytotoxic effects of receptor tyrosine kinase inhibitors
... activity of these drugs [5]. Indeed, a number of anti-can- cer compounds can induce cyto-protective autophagy [6]. Beside conventional chemotherapics, protective role of autophagy was also described during the use of ...
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INHIBITION OF SPLEEN TYROSINE KINASE (SYK) IN SILICO BY THIAZOLE DERIVATIVES
... tyrosine kinase is JAK STAT pathway. Activation of spleen tyrosine kinase (SYK) was shown to be the earliest detectable signaling response to cross-linking of the high affinity IgE receptor (FceRI) ...
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Modulation of Trophoblast Cell Death by Oxygen and EGF
... In summary, this study demonstrates that first trimester extravillous-like trophoblast possess apoptotic machinery that can be induced by alter- ation in oxygen tension or inhibition of PI3K path- way via the ...
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The drug-resistance to gefitinib in PTEN low expression cancer cells is reversed by irradiation in vitro
... EGFR kinase inhibitors is unlikely to be effective in PTEN-deficient tumors, even if they harbor activating EGFR ...EGFR kinase inhibitors, and there is no suitable means for reversal of drug resistance in ...
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Inhibition of the release of arachidonic acid prevents the development of sarcolemmal membrane defects in cultured rat myocardial cells during adenosine triphosphate depletion
... depletion. Inhibition of phospholipid degradation by U26,384 prevented the development of sarcolemmal membrane defects and the release of creatine kinase from the cultured myocardial cells during ATP ...
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Tyrosine kinase inhibitor suppresses coronary arteriosclerotic changes and vasospastic responses induced by chronic treatment with interleukin 1 beta in pigs in vivo
... tyrosine kinase inhibitor, ST 638, on those responses induced by IL-1 beta in our swine ...tyrosine kinase activation may play an important role in mediating the effects of IL-1 beta, while also suggesting ...
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Multi-tyrosine kinase inhibitors in preclinical studies for pediatric CNS AT/RT: Evidence for synergy with Topoisomerase-I inhibition
... the input of MTK inhibition in this process, we evaluated the effect on NF-B in response to irinotecan as a single agent and then in combination with sorafenib. Using BT12 cells, we examined the presence of ...
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