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 24 for “"High throughput screens"”.
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Hypercontraction and Drosophila : a model system for the study of human myopathies
… Development of model systems in which to utilize high-throughput screens for novel compounds will help in drug discovery for these diseases. In addition, genetic model systems will allow us to dissect the molecular and cellular pathways activated in response to mutations that affect muscle …
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A liquid-in-glass thermometer with sub-microKelvin resolution, and its application for calorimetry
… optical readout are widely used to implement high throughput screens for drug discovery. However, labeling requires assay customization and does not allow examination of the reactants in their native state. The most direct and universal non-labeling method is calorimetry, but current …
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Kinetic Characterization of the Protein Arginine Deiminase Family: Mechanistic and Inhibition Studies
… activity has led to the development of two novel high-throughput screens for identifying PAD4 inhibitors. In addition, the therapeutic efficacy of Cl-amidine for the treatment of RA has been evaluated in mice. In total, the information collected will aid in the design of future PAD inhibitors that …
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Towards The Total Synthesis Of Withanolide E And Physachenolide C
… of 17β-hydroxy withanolides were identified from high-throughput screens as inhibitors of androgen-induced changes in gene expression of prostate cancer cells. Therefore, these compounds may have important applications as new therapies against prostate cancer. We have devised a synthetic route to …
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Towards The Total Synthesis Of Withanolide E And Physachenolide C
… of 17β-hydroxy withanolides were identified from high-throughput screens as inhibitors of androgen-induced changes in gene expression of prostate cancer cells. Therefore, these compounds may have important applications as new therapies against prostate cancer. We have devised a synthetic route to …
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Towards The Total Synthesis Of Withanolide E And Physachenolide C
… of 17β-hydroxy withanolides were identified from high-throughput screens as inhibitors of androgen-induced changes in gene expression of prostate cancer cells. Therefore, these compounds may have important applications as new therapies against prostate cancer. We have devised a synthetic route to …
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Towards The Total Synthesis Of Withanolide E And Physachenolide C
… of 17β-hydroxy withanolides were identified from high-throughput screens as inhibitors of androgen-induced changes in gene expression of prostate cancer cells. Therefore, these compounds may have important applications as new therapies against prostate cancer. We have devised a synthetic route to …
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Small molecule inhibitors of steroid receptors for breast and prostate cancer
… estrogen receptor (ER) signaling. Moderate-to-high throughput screens of chemical libraries were designed and implemented to identify these inhibitors. The most promising inhibitor of AR transactivation to have emerged from the rigorous screening process was CPIC (1-(3-(2-chlorophenoxy) …
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Defining cell state regulators in cancers using single-cell analysis and CRISPR-Cas9 screening
As high-throughput transcriptional profiling becomes more sophisticated and accessible, our understanding of cancer heterogeneity and its impact on clinical outcomes are being realised. Whilst genomic variation has been extremely useful for cancer stratification and development of targeted …
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Global and chromosome-specific consequences of aneuploidy in Saccharomyces cerevisiae
… biology was previously lacking. We performed high-throughput screens for genes whose deletion has a synthetic fitness cost in aneuploid Saccharomyces cerevisiae cells containing single extra chromosomes. This analysis identified genes that when deleted decrease the fitness of specific disomic …
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Real-Time Bioluminescence Imaging Of Salmonella-Neoplastic Cell Interactions
… cell interactions, I utilized two high-throughput screens. In the first, I designed a bioluminescent transposon-reporter trap to identify specific Salmonella genes activated in the context of cancer cell co-culture conditions. Through this work, I identified five Salmonella genes …
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The Modulation of Life and Death: Small Molecule Activators and Inhibitors of Necrotic and Apoptotic Pathways
… (PARG). Through the development of high-throughput screens, a small molecule activator of procaspase-3 (PAC-1) and an inhibitor of PARG (PIP-1) were identified. PAC-1 was shown to potently induce apoptosis in mammalian cells in a manner directly proportional to the amount of …
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Microfluidic platforms for solid form screening of pharmaceutical parent compounds
… robotic systems have been developed to execute high throughput screens, these robotic tools typically require larger quantities of PC for solid form screening (~ 5 mg of material per condition) than are typically available in the initial phases of the drug development pipeline. Microfluidics has …
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Systems level characterizations of single and combination drug mechanisms of action in vitro and in vivo
… in cancer drug development. At the present time, high throughput screens of natural products and combinatorial synthesis libraries generate more pharmaceutical leads than can be characterized in detail. Lead optimization further generates many derivatives of these cytotoxic hits in an attempt to …
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DEVELOPING SMALL-MOLECULE PROBES AND INHIBITORS FOR ADP-RIBOSE-BINDING PROTEINS
… micromolar range and none of them possess both high activity and satisfactory drug-like properties. The other overlooked ADP-ribose-binding domain is the PAR-binding WWE domains present in multiple E3 ligases that have important cancer implications, but no WWE domain inhibitor or relevant …
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Machine Learning Methods for Discovering Metabolite Structures from Mass Spectra
… spectra. However, the complexity and high dimensionality of spectral data makes it difficult to identify unknown metabolites and their roles, with a large majority of detected metabolites remaining unidentified in public data. This thesis proposes a suite of new computational …
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High-Throughput Discovery of Stimuli of Bacterial Two-Component Systems from the Human Gut Microbiome
… a next-generation sequencing (NGS) approach to high-throughput screening of this library in response to discrete chemical ligands. We demonstrate detection of transcriptional signals from TCSs on a 5-minute time scale. We identify low dynamic range in transcriptional signals, and propose design …
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Characterization of Extremophilic Bacteria for Potential in the Biofuel and Bioprocess Industries
… a diverse subsample of the library (n=207) for high-throughput screens of extracellular cellulase activity, n-butanol tolerance, vanillin utilization, and lignin degradation, as indicated by decolorization of the surrogate Congo red. Many isolates exhibited the capacities screened, including …
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Directed evolution of amino acid dehydrogenases for biocatalysis of chiral amines
… has recently led to the development of ultrahigh-throughput screening platforms that allow sorting of more than 106 variants per hour. So far, these microfluidic droplet sorters have relied exclusively on fluorescent readouts. To further extend the range of applications toward enzymes for …
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Crystallization of active pharmaceutical ingredients using microfluidic platforms and meniscus-guided coating
… of candidate drugs earlier in drug development. High throughput screens yield multiple solid forms of candidate drugs that are later characterized and prioritized for further development. Another focus within the pharmaceutical industry has been to improved manufacturing practices with continuous …
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