Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 16 of 16 for “"MEK5"”.
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Design, Synthesis and Evaluation of Diphenylamines as MEK5 Inhibitors
… signal-Regulated Kinase) substrate. The MEK5/ERK5 pathway is involved in cell survival, anti-apoptotic signaling, angiogenesis, and cell motility. It is significantly up-regulated in specific tumor types including breast and prostate cancers. A novel series of compounds utilizing the …
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Dual Inhibition of the PI3K/Akt and MEK5/ERK5 Pathways for the Treatment of Breast Cancer
… crosstalk mechanisms. New evidence suggests that MEK5/ERK5, a member of the MAPK family, is a crucial component in the proliferation and survival of several aggressive cancers. We hypothesize that inhibiting both PI3K/Akt and MEK5/ERK5 pathways will decrease cell viability while maintaining …
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Design, Synthesis, & Biological Evaluation of Novel Het-Aromatic/Aromatic Analogs for the Treatment of HIV, Cancer, & Cognitive Dysfunctions
… survival, metastasis, and chemo-resistance. The MEK5/ERK5 pathway, which is a member of MAPK signaling cascade, is involved in cell survival, anti-apoptotic signaling, angiogenesis, and cell motility. It is found to be significantly upregulated in breast cancers especially triple-negative breast …
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Investigation of a Novel Mitophagy Regulatory Pathway and Chemical Inducer
… for autophagy regulators to identify the MEKK3-MEK5-ERK5 pathway as a potential regulator of mitophagy in the absence of exogenous damage. Here, I provide evidence that genetic or pharmacological inhibition of the MEKK3-MEK5-ERK5 pathway increases mitochondrial content by reducing …
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Analysis of the role of extracellular signal regulated kinase (ERK5) in the differentiation of muscle cells
The MEK5/ ERK5 kinase module is a relatively new discovered mitogen-activated protein kinase (MAPK) signalling pathway with a poorly defined physiological function. Since ERK5 and its upstream activator MEK5 are abundant in skeletal muscle a function of the cascade during muscle differentiation was …
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Age-Related Effects on the Mitogen-Activated Protein Kinase and Phosphatidylinositol 3-Kinase Pathways in Breast Cancer and the Characterization of Novel MEK5 Inhibitors
… (PI3K/Akt) pathway. Further, the role of the MEK5-ERK5 cascade in breast cancer cell proliferation, migration, and invasion was analyzed. In addition, several series of novel MEK5 inhibitors were characterized with regard to both efficacy and selectivity. In vitro assessment revealed distinct …
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Studies on signaling pathways induced by FLT3, an important oncogene in AML
… to inhibit FLT3 and to determine the role of MEK5/ERK5 signaling in FLT3-ITD mediated transformation. Using phosphospecific antibodies, we have identified 3 novel phosphorylation sites in FLT3, Y726, Y793 and Y842, and studied their kinetics and specificity. The additional eight phosphorylated …
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Serine 910 Phosphorylation of Focal Adhesion Kinase Is Critical for Costamere Assembly
… and Src via parallel Raf-1→MEK1/2→ERK1/2 and MEK5→ERK5 signaling pathways. Using co-immunoprecipitation, TIRF-microscopy and FRAP, ET-1 stimulation of NRVM expressing a nonphosphorylatable, S910A-FAK mutant decreased the interaction of paxillin and vinculin within costameres. This interaction …
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Anthrax toxin effects on B lymphocyte function
… (MAPK) kinase family 1-7, with the exception of MEK5. This kinase family is responsible for activating the mitogen-activated protein kinase (MAPK) cascade. This cascade includes extracellular signal-regulated protein kinases (ERK), c-Jun NH2-terminal kinases (JNK) and p38 kinases. The disruption …
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Identification of the ERK5 Kinase as a Key Regulator of Embryonic Stem Cell Pluripotency
… ERK5 kinase activity, upstream activation by MEK5 and a C-terminal transcriptional domain, maintain mESCs in the naïve state, and activation of the ERK5 pathway suppresses transition to primed pluripotency.<br/><br/>I employ quantitative phosphoproteomics to elucidate molecular mechanisms by …
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KLF4 IS A KEY DETERMINANT IN THE DEVELOPMENT AND PROGRESSION OF CEREBRAL CAVERNOUS MALFORMATIONS
… Ccm1 deletion leads to activation of the MEKK3-MEK5-ERK5-MEF2 signaling cascade resulting in a marked upregulation of the transcription factor Krüppel-like factor 4 (KLF4) in ECs in vivo. KLF4 promotes an endogenous production of bone morphogenetic protein 6 (BMP6) in ECs that, in turn, …
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Melatonin-Tamoxifen Drug Conjugates as Breast Cancer Drugs: Pharmacological Evaluation in Phenotypically Diverse Breast Cancer Models and Pharmacokinetic Assessment in Liver Microsome and Female Mouse Models
… mechanisms of action using selective MEK1/2, MEK5, and PI3K inhibitors. C4 and C5 inhibited TamR MCF-7 cells with equal potency and efficacy and both C4 and C5 inhibited TU-BcX-4IC cell viability. Even though both compounds demonstrated similar inhibitory actions against BC cell viability and …
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Rho GTPases in Neuronal Apoptosis and Neurodegeneration
… CGNs evoked apoptosis via repression of unique MEK5/ERK5, p90Rsk, and Akt-dependent pro-survival pathways. Furthermore, selective inactivation of Rac induced the activation and translocation of the pro-apoptotic BH3-only protein Bad to the mitochondria, where it has been demonstrated to induce …
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The effect of cAMP elevation on intracellular signalling pathways in prostate epithelial cells
… Genetic or pharmacological inhibition of the MEK5/ERK5 signalling pathway significantly attenuated the rapid cAMP-mediated changes in LNCaP cell morphology, suggesting this pathway may be a possible target by which to inhibit the onset of neuroendocrine differentiation. To summarise, this …
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The Effect of Resveratrol on Lipopolysaccharide-induced Dopaminergic Deficits and BV-2 Cell Activation
… by LPS, but preliminary data suggest that the MEK5 inhibitor BIX02189 inhibited LPS-induced TNF-α release. Therefore, BIX02189 may be inhibiting a distinct pathway in our model. Overall, these studies suggest that the use of dietary resveratrol supplementation may be protective against …