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 14 of 14 for “"HSP90 inhibitors"”.
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Synthesis Of Substituted Pyrrolo[2,3-D]Pyrimidines As Microtubule-Binding Agents and HSP90 Inhibitors
… agents and heat shock protein 90 (HSP90) inhibitors as anticancer agents are briefly reviewed. The work in this dissertation is centered on the synthesis of substituted pyrrolo[2, 3-d]pyrimidines as potential anticancer agents that act via microtubule inhibition or HSP90 …
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The Pursuit of Unshocking Hsp90 Inhibitors: Development of Gedunin and Cruentaren A as Chemical Leads
Abstract: The 90 kDa heat shock protein (Hsp90) is a molecular chaperone that is critical cellular survival and growth under both typical and stressful conditions. Hsp90 is responsible for the maturation and stability of more than 200 client proteins involved in a diverse assortment of cellular …
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Inhibition of Hsp90 in Streptomyces coelicolor
Inhibition of the chaperone protein Hsp90 in plants and insects has been found to result in drastic changes in phenotype. We investigated the effect of Hsp90 inhibition on the bacteria Streptomyces coelicolor. These changes were studied by growing S. coelicolor in the presence of Hsp90 inhibitors, …
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TO INVESTIGATE THE ROLE OF RNF8 IN REGULATING MITOTIC PROGRESSION IN GLIOMAS
… led to the rational combination of PLK1 and HSP90 inhibitors that elicit an additive effect in reducing GSC proliferation and stemness. Thus, our study has unveiled a novel mechanism of RNF8 in SAC regulation, with relevance to gliomas.
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Evaluating the Therapeutic Effect of an Hsp90 Inhibitor in Mouse Models of Alzheimer’s Disease
… Strategies targeting heat shock protein 90 (Hsp90) inhibition have been widely investigated in the treatment of cancer for over two decades. Its application in the treatment of neurodegenerative diseases however, has emerged more recently in the last decade. The role of the Hsp90 chaperone in …
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APPROACHES OF MODULATION OF THERAPEUTIC TARGETS RELEVANT TO DRUG RESISTANCE
… In recent years, the molecular chaperone Hsp90 has emerged as leading example of such a target-specific therapy. Heat-shock proteins are found at increased levels in many solid tumors and haematological malignancies. Their expression may account for the ability of malignant cells to …
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Discovery of heat shock protein90 inhibitors using structured-based virtual screening
… and behavioural abnormalities. Cholinesterase inhibitors (ChEIs) and N-methyl-D-aspartate receptor (NMDAR) antagonists are current treatment options for mild to moderate AD. These agents are not used to cure the illness, but rather as symptomatic therapy. Heat Shock Protein (HSP90), is one of …
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The Role of Prolactin in the Cellular Response to DNA Damaging Agents
… that one isoform of heat shock protein-90 (HSP90), Hsp90alpha, is a prolactin-Janus kinase-2 (Jak2)-signal transducer and activator of transcription-5 (Stat5) regulated gene in breast cancer cells. We have now observed that prolactin increased the viability of breast cancer cells to DNA …
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Developing Novel Approaches to Improve Response to T Cell Based Cancer Immunotherapy
… a read out of apoptosis. Heat shock protein 90 (HSP90) inhibitors amongst compounds that improved T cell mediated cytotoxicity. We show that treatment with the HSP90 inhibitor ganetespib (Synta) greatly improves T cell mediated cytotoxicity of both human and murine cancer cells lines <em>in …
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Pi3K- and Mtor-Dependent Mechanisms of Lapatinib Resistance and Resulting Therapeutic Opportunities
… pathway, suggesting the use of PI3K and/or mTOR inhibitors in lapatinib-resistant breast cancers. We found that p110α-specific PI3K inhibition effectively overcame lapatinib resistance in LapR cell lines and xenografts with increased p110α activation, while the LapR cell line with …
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Overexpression of Heat Shock Factor 1 Protects against Pathological Proteins in Neurodegenerative Diseases
… Heat shock proteins (HSPs), such as HSP70 and HSP90 are molecular chaperones that maintain protein homeostasis and prevent neuronal death. HSPs are regulated by a stress-induced transcriptional factor, heat shock factor 1 (HSF1). HSF1 is inactive when in complex with HSP90 and becomes active …
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Inhibition of Heat Shock Protein 90 Reduces Inflammatory Signal Transduction in Murine J774 Macrophage Cells and Lessens Disease in Autoimmune MRL/lpr Mice: What in vitro, in vivo, and in silico Models Reveal
Heat shock protein 90 (HSP90) is a molecular chaperone protein that protects proteins from degradation, repairs damaged proteins, and assists proteins in carrying out their functions. HSP90 has hundreds of clients, many of which are inflammatory signaling kinases. The mechanism by which HSP90 …
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HSP70: a therapeutic biomarker for treatment of glioma
… highly inducible molecular chaperones HSP70 and HSP90 are emerging as important anti-cancer targets. Previously, proteomic analysis had demonstrated that post-induction of HSP70 on HSP90 inhibition undermines the efficacy of treatment. The present study has quantified transcriptional levels and …
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Targeting mutant p53 in cSCCs
… compared to normal human keratinocytes (NHK). HSP90 inhibitors, 17-AAG and 17-DMAG, reduce mutant p53 protein levels suggesting that HSP90 plays a role in stabilising mutant p53 in cSCCs.<br/><br/>5. PR-619, a broad range deubiquitinating enzyme (DUB) inhibitor, reduces mutant p53 protein …