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 “"thermal shift"”.
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Structural and Inhibitor Binding Studies of Tyrosyl-DNA Phosphodiesterase 1
… binding assays were investigated. These include thermal shift assay and intrinsic protein fluorescence spectroscopy. The results obtained by thermal shift assay were found to be highly variable. It was therefore decided that the thermal shift assay may not be suitable to study ligand binding …
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Viscoelastic characterization of polyurea based polymers
… were obtained in the form of Prony series. The thermal shift factor for bulk relaxation was fitted with the Arrhenius equation while for shear relaxation, the trend was fitted with the WLF equation. The nonlinear response at ambient conditions was predicted using the modified free volume model …
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Synthesis and Design of ClpP Activators as Novel Antibiotics
… related to metabolism and clearance, including thermal shift and surface plasmon resonance assays. Results. Synthesized and tested 33 novel compounds, comprising a total of 80 synthetic steps. Conclusion. The three-part conclusion from the dissertation is that: Heterocycles and bulky side chains …
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Characterization of the Viscoelastic Fracture of Solvated Semi-Interpenetrating Polymer Network Silicone Hydrogels
… relevant master curves and corresponding thermal shift factors of such properties as shear relaxation modulus, dynamic moduli, and the loss factor. Concurrently, the cohesive fracture properties were studied by utilizing a "semi-infinite" strip geometry under constrained tension in which …
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Targeting PfUCHL3 Using Chemically Constrained Peptides
… peptides for PfUCHL3. Through the use of thermal shift assays the inhibitory peptide’s were shown to stabilise the proteins structure upon binding and increase the melting temperature. Work is currently underway to determine the cell permeability properties of the peptides and their …
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Functional and mechanistic studies of human mitochondrial carriers
… aim of determining the substrate binding site by thermal shift analysis. The results obtained provided a proof of principle. Finally, the kinetic mechanism of mitochondrial carriers, which was claimed to be sequential, was revisited. This was the only extant evidence in favour of a dimer model. …
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Characterization and Lifetime Performance Modeling of Acrylic Foam Tape for Structural Glazing Applications
… from a dynamic mechanical analyzer (DMA). The thermal shift factors obtained from these constitutive tests were successfully applied to the creep rupture and ramp-to-fail data collected at 23°C, 40°C, and 60°C (73°F, 104°F, and 140°F), resulting in master curves of ramp-to-fail strength and …
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Structural basis for the function of the transcriptional regulator KstR from Mycobacterium tuberculosis
… techniques (i.e. electrophoretic mobility shift assay, surface plasmon resonance and intrinsic fluorescence quenching assay). Protein-DNA binding assays have demonstrated that the 21-amino-acid extension at the N-terminus of KstR imposes a positive but non-essential role for KstR-DNA …
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Identification and Optimization of Small Molecule Binders for ALK2, USP5, and DCAF1
… engagement with an EC50 of 10 µM by cellular thermal shift assay. Moreover, we described a second SAR effort to optimize compound 19 with the intent of generating a chemical probe to investigate the biology of DCAF1 in cells. Lastly, we outlined the optimization of an alternative chemical …
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Performance Evaluation and Durability Studies of Adhesive Bonds
… and time-temperature-superposition principle, thermal shift factors were obtained and successfully used to characterize the creep rupture master curves for specific joint configurations, leading to insights into delayed failures corresponding to three years through experiments carried out in …
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MASS SPECTROMETRIC STRATEGIES TO IDENTIFY BIOACTIVE COMPONENTS FROM NATURAL EXTRACTS WITH ANTI-INFLAMMATORY ACTIVITIES
… of a MS-CETSA (Mass Spectrometry – Cellular Thermal Shift Assay) methodology to probe the direct target of a bergamot leaves polyphenols extract.
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Biophysical and Biochemical Screening Approaches for Antimicrobial Drug Discovery Targeting S. aureus ClpP
… Chapter two discusses optimization of thermal shift assay as primary screening assay for ClpP and its utility toward screening of fragment collections and buffer conditions. Chapter three discussed the development of a site specific Fluorescence Polarization based FP probe based on ADEP …
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Antibiotic Drug Discovery Targeting Bacterial Metabolism
… chapter describes the adaptation of the cellular thermal shift assay to explore target engagement in the Gram-negative cell system. Drug entry and accumulation are especially challenging to achieve in Gram-negative cells due to their unique dual membrane system and associated efflux machinery. …
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Development of peptide inhibitors as molecular therapeutics against tandem-repeat proteins
… Cdc20 in mammalian cell lysates using a Cellular Thermal Shift Assay (CETSA). Lastly, I determined the co-crystal structures of three of the highest affinity D-box peptides bound to Cdc20, providing high-resolution insights into the binding interface, which should aid in the further development of …
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Regulating the stabilities of NOD1 and NOD2, two innate immune receptors, with sugars and chaperones
… enzyme O-GlcNAc transferase (OGT). A cellular thermal shift assay (CETSA) typically used to detect protein-ligand binding was adapted in order to monitor the stability changes caused by O-GlcNAcylation, and it was found that wild type NOD1 and NOD2 were stabilized when modified by OGT. Lastly, …
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Targeting Transcription Factors in Neuroblastoma: Development of Aurora Kinase A/N-Myc Degraders and ID2 Chemical Probes
… Appendix A reports the development of a cellular thermal shift assay for evaluating the target engagement of small-molecule compounds with Cyclin Kinase 1/2.
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Exploring Kinases of Metabolism and Signaling in the Malaria Parasite Plasmodium
… Future studies to further optimize a cellular thermal shift assay coupled with mass spectrometry may confirm on-target binding of takinib and HS220 in Plasmodium parasites. Finally, a model of PfPK9 was generated to guide hypotheses about takinib-binding and enable structural comparison with …
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Novel Optical Materials for Passive Photonic Applications
… as it is the material properties (optical, thermal, mechanical, electrical, ...) in addition to their processing and compatibilities with standard processes that enable us the creation of entirely new devices or improve the performance of currently available optical devices. In this …
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Probing the druggability of the Notch1 ankyrin domain using a fragment-based approach
… fragment-library exploited a fluorescent-based thermal shift assay that identified 36 fragment hits. Some of the fragments were kinetically characterised by Surface Plasmon Resonance (SPR) and their affinities were found to be in the millimolar range. Several attempts at soaking vii and …
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Mikrobinių lipolizinių fermentų imobilizavimas ir imobilizuotų preparatų analizė /
… out by determining the stabilizing pH values by thermal shift assay and the optimum reaction temperature by spectrophotometric determination. The enzyme immobilization was based on adsorption. The lipolytic activity of the preparations and their supernatants and the concentration of the protein …
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