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 20 of 203 for “"kinase inhibitor"”.
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SCRIBBLE: A POTENTIAL DUAL KINASE INHIBITOR
Extracellular signal-regulated kinases (ERKs) modulate cellular activities in response to extracellular stimuli and play important biological roles. Thus, perturbed kinase pathways induce pathological conditions, such as tumor development. Rit, a novel member of the Ras family GTPases, activase …
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Regulation of the cyclin-dependent kinase inhibitor p21 by TBX3
… that TBX3 may repress the cyclin-dependent kinase inhibitor p21WAF1, which has a role in a myriad of processes including cell cycle arrest, senescence, apoptosis, differentiation and DNA replication and repair. The current study therefore aimed to explore this possibility and to reveal a …
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Radiosensitization of Head & Neck Carcinoma Cells by Linifanib, A Receptor Tyrosine Kinase Inhibitor
… Linifanib (ABT-869), a multi-receptor tyrosine kinase inhibitor of VEGF and platelet derived growth factor (PDGF) receptor families, on radio-sensitization of HNSCC. The results show that Linifanib (ABT-869) can induce an antitumor effect and radio-sensitize HNSCC cells via inhibition of STAT3 …
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Functional characterization of the cyclin-dependent kinase inhibitor p21 by gene targeting in the mouse
Thesis (Ph. D.)--Massachusetts Institute of Technology, Dept. of Biology, 1998.
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RAF-1 kinase inhibitor protein-mediated cholecystokinin-2 receptor desensitization and extracellular signal-regulated kinase activation
Raf-1 kinase inhibitor protein (RKIP) is initially known as a suppressor for Raf-1-mediated ERK activation. Moreover, recent findings indicate that RKIP also has a role in G-protein-coupled receptor (GPCR) desensitization. Protein kinase C (PKC)-mediated phosphorylation at Serine 153 (S153) on RKIP …
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SCF SKP2B - AND KPC1-DEPENDENT DEGRADATION OF CYCLIN-DEPENDENT KINASE INHIBITOR KRP1 AND CELL CYCLE REGULATION IN ARABIDOPSIS THALIANA
In animals and fungi, cyclin-dependent kinase inhibitors play a key role in cell cycle regulation by inhibiting the activities of cyclin-dependent kinase/cyclin complexes. However, little is known about the role of this group of proteins in plant cell cycle regulation. To gain insight into the …
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Multiple Levels of Regulation of Cyclin-dependent Kinase Inhibitor 1A (p21/WAF-1) by the <i>DDX5 </i>Gene
The p68 protein, an archetypical member of the DEAD box family of RNA helicases, exhibits both ATPase and RNA helicase dependent/independent activities. To date the p68 protein has been implicated in most parts of RNA metabolism including ribosome biogenesis, transcription, RNA decay, miRNA …
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Prognostic markers associated with tyrosine kinase inhibitor treatment response and maintenance of treatment free remission in chronic myeloid leukaemia
… with the introduction of highly active tyrosine kinase inhibitors (TKIs). However, treatment responses are highly heterogeneous. The aim of this thesis is to identify prognostic markers that may help individualise treatment and optimise outcome by stratifying patients into risk groups. Selective …
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Development of Machine Learning Models for Generation and Activity Prediction of the Protein Tyrosine Kinase Inhibitors
… approaches for generation and scoring of novel kinase inhibitor molecules. We utilized a binary Random Forest classification model to develop a Machine Learning based scoring function to evaluate the generated molecules on Kinase Inhibition Likelihood. By training the model on several chemical …
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Targeting integrin alpha 5 and focal adhesion kinase to overcome azacitidine resistance in higher risk myelodysplastic syndromes
… alpha 5 blocking antibody or a focal adhesion kinase inhibitor could overcome azacitidine resistance. After establishing an effective dose of the focal adhesion kinase inhibitor, GSK2256098, I demonstrated that these doses were not toxic to healthy haematopoietic stem and progenitor cells …
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P27 Expression in Endothelin-1 Stimulated Mitogenesis
… is mediated through the cyclin dependent kinase inhibitor p27. BCEC were isolated from bovine eyes and grown in DMEM-10% serum in a 5% C02, 37° C incubator. Confluent cultures of BCEC were incubated for 24 hours with lOOnM Endothelin-1, luM BQ123 and BQ123 +100nM Endothelin-1 and some left …
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SIGNALING MECHANISMS IN SEPSIS-INDUCED IMMUNE DYSFUNCTION
… in the circulation. It was noted that Rho-kinase inhibitor reduced sepsis-induced pulmonary recruitment of neutrophils and tissue injury via regulation of CXC chemokines formation in the lung. Moreover, inhibition of Rho-kinase signaling decreased sepsis-induced T-cell apoptosis as well as …
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Genistein-Induced Potentiation Effect on Glucose-Stimulated Insulin Secretion (GSIS) in INS-1 β-cells
… isolated from soy bean seed and having tyrosin kinase inhibition activity, had a potentiation effect on GSIS (glucose-stimulated insulin secretion) in pancreatic INS-1 beta cells. Although the potentiation effect was glucose-dependent, the signal involved in potentiation effect were not …
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Pi3K- and Mtor-Dependent Mechanisms of Lapatinib Resistance and Resulting Therapeutic Opportunities
… cases and are frequently responsive to the HER2 kinase inhibitor lapatinib, but generally for only short duration. We aimed to understand how breast cancers with HER2 amplification become resistant to lapatinib, in order to identify potential therapies that can overcome lapatinib resistance. To …
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An optical proteomic profile of the HER2 family in breast tumours and the effect of exposure to tyrosine kinase inhibitors
… of HER2-targeted therapy with the tyrosine kinase inhibitor (TKI) lapatinib, in vitro, and elucidation of the ensuing conformational changes may help understand the molecular activity of lapatinib and elucidate mechanisms of resistance. Clinical translation of this knowledge may help to …
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Tyrosine 370 Phosphorylation of Atm Positively Regulates Dna Damage Response
… ATM Y370F mutant or pretreatment with an EGFR kinase inhibitor gefitinib blocks EGFR and ATM association, hinders CHK2 activation and subsequent foci formation, and increases radio-sensitivity. Thus, we reveal a critical mechanism by which EGFR directly regulates ATM activation in DNA damage …
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Development and application of novel analytical methods for molecularly targeted cancer therapeutics
… developed for the quantification of 1) tyrosine kinase inhibitor anti-cancer drugs to examine the interaction of these agents with drug resistance mechanisms, and 2) the multiple myeloma drug thalidomide as a pilot study to identify potential correlations between serum drug levels and …
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Cellular Mechanism of Arglabin-Dimethylaminohydrochloride Cytotoxicity
… was to determine the farnesyltransferase (FTase) inhibitory activity of arglabin-DMA and to investigate the effects of arglabin-DMA on three proteins: Ras, Rho and cyclin kinase inhibitor p21/WAF1/CIP1.</p> <p><em>In vitro</em> FTase assays were used to study the effect of arglabin-DMA on FTase …
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