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 18 of 18 for “"Protein Kinase Inhibitors"”.
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Doxorubicin combined with phytochemicals as pro-apoptotic agents and protein kinase inhibitors for the treatment of acute myeloid leukaemia
… most common form of adult leukaemia with several kinase mutations. The FLT3-ITD mutation is a common kinase mutation observed in (20-30%) of AML patients and this mutation is also the most involved in the prognosis of AML. It confers poor treatment outcome in patients despite intensive …
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Design, synthesis, and structure-activity relationship studies of dual Plasmodium falciparum phosphatidylinositol 4-kinase and cGMP-dependent protein kinase inhibitors
… efforts. Considering the success of human kinase inhibitors as anti-cancer drugs and the identification of Plasmodium kinases as promising targets for malaria chemotherapy, this study aimed to optimize anti-plasmodium phosphatidylinositol 4-kinase (PI4K) and the cGMP-dependent protein …
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Development of Integrated Machine Learning and Data Science Approaches for the Prediction of Cancer Mutation and Autonomous Drug Discovery of Anti-Cancer Therapeutic Agents
… science approaches to design new drugs to target protein kinase inhibitors. We show that these techniques exhibit strong promise in aiding cancer research and drug discovery.</p>
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Interrelationships among estrogen, insulin-like growth factor-I and cyclic adenosine monophosphate in the regulation of uterine progesterone and estrogen receptors
… factors mediate regulation of these receptor proteins. Exposure of uterine cells maintained in primary culture to estradiol, IGF-I, or to agents which raised intracellular cAMP levels stimulated significant increases in progesterone receptor (PR) content. Stimulation of PR levels by these …
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The cyclic AMP-activated sodium current in the molluscan neuron: A kinetic analysis of regulation by diffusion, phosphodiesterase and calcium ion
… response to cyclic AMP injection is resistant to protein kinase inhibitors, and is very likely mediated by direct cyclic AMP binding to the channel receptor. The slow I$\sb{\rm Na,cAMP}$ is regulated by diffusion-hydrolysis kinetics: it varied in latency to current onset, latency to peak …
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Micro-analysis of adenylate cyclase and cyclic AMP-dependent protein kinase activities in human mammary tumors
… profiles of adenylate cyclase and cAMP-dependent protein kinase within a series of malignant and benign human mammary tumors. The methods allow for determination of enzyme activity in histologically-confirmed neoplastic areas within individual tumors which permits comparisons to be made with …
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Regulation of Maize (Zea mays L.) Starch Synthase IIa by Protein Phosphorylation
… studies indicate that in cereal endosperm, protein phosphorylation plays a major role in regulating the formation of functional multi-enzyme complexes between SSs and SBEs during starch biosynthesis and that SSIIa forms the core of such a functional protein complex, with SSI and SBEIIb. The …
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Regulation of the FGF14:Nav Interactome by a GSK-3 Centered Pathway
… which interact with accessory and regulatory proteins including ankyrin-G, β-IV-spectrin, neurofascin, and intracellular fibroblast growth factors (iFGFs, FGF11-14). Dysregulation of the sodium channel complex is associated with a panorama of psychiatric disorders in both animal models as well …
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CHARACTERIZATION OF HUMORAL RESPONSE TO EPSTEIN-BARR VIRUS (EBV) INFECTION AND PROTEIN KINASES INVOLVED IN VIRAL REPLICATION
… and 140,000 deaths each year worldwide. Cellular protein kinases have been reported to play a role in the viral life cycle, but their influence on different stages of EBV life cycle has not been studied extensively. Therefore, in the first part of my dissertation, I investigated the involvement of …
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Autoinhibition and Chloride Sensing in the WNK1 Kinase
Protein kinases control diverse cellular pathways and have are the subject of intensive study regarding how they maintain specificity toward sub- strates. The research presented here focuses on a 230kDa serine/threonine protein kinase known as WNK1 (with no lysine {k}). The protein was first cloned …
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QUANTITATIVE PROTEOMIC APPROACHES TO STUDY DRUG MECHANISM OF ACTION
In recent years an increased number of covalent protein kinase inhibitors has been approved for cancer therapy and many more are undertaking clinical trials. Covalent binding is usually obtained by introducing in these drugs an electrophilic warhead able to bind specific nucleophilic sites in the …
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Protein O-Kinases in the Archaeon Sulfolobus solfataricus
For many years, it has been understood that protein phosphorylation-dephosphorylation constitutes one of the most ubiquitous mechanisms for controlling the functional properties of proteins. Although originally believed to be a eukaryotic phenomenon, protein phosphorylation is now known to occur in …
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Studies Toward the Syntheses of Antiarrythmic, Anti-Virulence, and Anticancer Small Molecules
… fibrillation, b) the development of potent inhibitors of QseC mediated virulence gene expression, and c) studies toward a biomimetic total synthesis of nigricanoside A. Antiarrhythmic analogs of 17(R),18(S)-epoxyeicosatetraenoic acid (17(R),18(S)-EEQ): Arrhythmias such as atrial and …
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Design and Applications of Split-Luciferase Systems in Vitro and in Cellulo
Split-protein reassembly methods allow for the detection of a variety of macromolecular interactions in vitro, in cellulo and in vivo. Spilt-protein reporters, such as split-firefly luciferase (Fluc), depend upon the conditional reassembly of the genetically fragmented enzyme. The two fragments of …
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Targeting Cyclin Dependent Kinases 4/6 Activity in Pancreatic Ductal Adenocarcinoma
Pages vi-xiii are incorrectly numbered as pages v-xii.
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TSLP-induced Mechanisms and Potential Therapies for CRLF2 B-cell Acute Lymphoblastic Leukemia
… gene, leading to overexpression of the CRLF2 protein- a component of the receptor signaling complex for the cytokine Thymic Stromal LymphoPoietin (TSLP) on the surface of B-ALL cells. TSLP has been shown to induce proliferation of human and mouse B-cell precursors via activation of the …
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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 …