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 17 of 17 for “"17-AAG"”.
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17-AAG and sihsp90α combinational therapy as a novel anti-cancer approach
… of glioma. This study utilized a Hsp90-inhibitor 17-AAG and hsp90α-specific siRNA (sihsp90α), either as single agent or in combination, to inhibit Hsp90 function in glioblastoma. Hsp90α mRNA and protein expression levels post treatment were evaluated using qRT-PCR and confocal microscopy. To …
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Mechanism-Based Strategies to Enhance The Actions of A
… and hydrolysis of ATP. The geldanamycin analog, 17-AAG, binds to the ATP pocket of HSP90 leading to the degradation of client proteins. However, treatment with 17-AAG results in the elevation of the levels of antiapoptotic proteins HSP70 and HSP27, which may lead to cell death resistance. The …
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Evaluating the Therapeutic Effect of an Hsp90 Inhibitor in Mouse Models of Alzheimer’s Disease
… we utilized a widely used Hsp90 inhibitor, 17-AAG (17-allylamino-17- desmethoxygeldanamycin), to show that 17-AAG not only induces a heat shock-like response, </p> <p>but also regulates (likely at the transcriptional level as modeled by qRT-PCR) select proteins enriched in the synapse, such …
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Molecular Mechanisms by Which HSP90 Inhibition in the Spinal Cord Enhances Opioid Receptor Signaling
… when HSP90 is inhibited in spinal cord using 17-AAG, ERK MAPK signaling, and subsequent opioid anti-nociception is enhanced. Quantitative proteomic analysis on the spinal cords of CD-1 mice treated with 17-AAG revealed that both 5' AMP-activated protein kinase subunit beta-1 (AMPK) and …
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Pharmacological modulation and manipulation of cancer drug resistance
… Two of these agents (indomethacin and 17-AAG) partially down-regulated the expression of P-gp in the A549-Taxol cell line but did not overcome P-gp-mediated resistance when combined with docetaxel simultaneously or in pre-treated proliferation assays. Three agents (lapatinib, sulindac …
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Charakterisierung von Schlüsselproteinen der Signaltransduktion (EGF-R, c-erbB2, Hsp90) in humanen Tumorxenografts mittels Gewebemikroarray
… wurden entwickelt. Das Geldanamycin Derivat 17-AAG (17-allylamino-geldanamycin) befindet sich in klinischer Phase Studien in England und den USA. Es hemmt die Interaktion des Hsp90 mit anderen Proteinen. <br> <br>In der vorliegenden Arbeit wurden Schlüsselproteine der Signaltransduktion …
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HSP70: a therapeutic biomarker for treatment of glioma
… in glioma cells U87-MG using VER-155008 and 17-AAG, respectively. Improved efficacy of HSP70 and HSP90 inhibitors was evaluated using a chemosensitivity assay. MicroRNAs (miRNAs) are highly conserved small non-coding RNA molecules (21-24 nucleotides) that regulate simultaneously the …
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THE INHIBITOR-OF-APOPTOSIS PROTEIN SURVIVIN INCREASES P34CDC2 PHOSPHORYLATION AND ENHANCES CELL SURVIVAL AND PROLIFERATION BY PROTECTING THE WEE1 KINASE FROM DEGRADATION BY CASPASE-3
… and Cdc2, we treated cells with AICAR and 17-AAG that inhibit Hsp90, which is known to be required for Survivin stability. Treatment of BaF3 cells expressing wt-Survivin with AICAR and 17-AAG decreased Cdc2-Tyr15 phosphorylation compared to vehicle-treated control cells. Taken together, …
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Novel Cancer Therapeutics, the Generation of ROS, and Cell Survival
… studies show that the geldanamycin derivative, 17-allylamino-17-demethoxygeldanamycin (17-AAG), interacts with the secondary bile acid, deoxycholic acid (DCA), to kill primary rat hepatocytes and HuH7 human hepatoma cells. An effect abolished by the addition of the ROS-quenchers, NAC and Trolox. …
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Synovial sarcoma : translating gene expression into patient care
… studies that demonstrate the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin (17-AAG) inhibits proliferation of synovial sarcoma by inducing apoptosis and that this is associated with degradation of multiple receptor tyrosine kinases and disruption of the SYT-SSX-β-catenin interaction. …
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Biodegradable Polymeric Biomaterials in Different Forms for Long-acting Contraception and Drug Delivery to the Eye and Brain
… and blood-brain barrier (BBB) permeability of 17-N-allylamino-17-demethoxygeldanamycin (17-AAG) to treat Alzheimer’s disease. The nanoparticles sustained the release of 17-AAG for at least one week in vitro and showed increased permeability (2-fold) of the 17-AAG across BBB in vivo in mice, and …
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Onkogenomische Aspekte Zytokin-assoziierter Signaltransduktion
… Chaperon HSP90 durch das Geldanamycin-Derivat 17-AAG oder RNA-Interferenz gegen HSP90 zu einer Hemmung des Jak-STAT-Signalwegs einhergehend mit einer reduzierten Proliferation der cHL-Zellen führt. Im zweiten Teil der Arbeit konnten durch Genexpressionsanalysen Zielgene von STAT6 im cHL …
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Pi3K- and Mtor-Dependent Mechanisms of Lapatinib Resistance and Resulting Therapeutic Opportunities
… kinase inhibitor AZD8055 or the Hsp90 inhibitor 17-AAG. Together these data strongly suggest the use of PI3K/mTOR inhibitors or Hsp90 inhibitors to prevent or delay lapatinib resistance. Further, we found that p110α-specific PI3K inhibition in combination with lapatinib was both effective against …
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Formulation Devlopment Of Mesoporous Silica Nanoparticles As An Injectable Delivery System
… loading of hydrophobic molecules such as PTX and 17-AAG depends on the polarity of solvent, with less polar solvents improving drug loading. We have successfully co-loaded PTX and 17-AAG into the same particles. We observed that PEGylation decreases loading of hydrophobic molecules. We hypothesize …
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Novel Monte Carlo Approaches to Identify Aberrant Pathways in Cancer
… cells compared with non-resistant cells when 17-AAG (a drug that inhibits HSP90AA1) is applied. We believe that this dissertation work not only offers novel computational tools towards understanding complicated biological problems, but more importantly, it provides a valuable paradigm where …
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APPROACHES OF MODULATION OF THERAPEUTIC TARGETS RELEVANT TO DRUG RESISTANCE
… the tumors than in the plasma, as in the case of 17-AAG and its active metabolite. However, side effects and poor formulability of 17-AAG restricted its potential of clinical application and motivated many groups to synthesize new compounds. The aim of this project is to identify new Hsp90 …
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Targeting mutant p53 in cSCCs
… 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 levels in a range of …