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 51 for “"Chemical probes"”.
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Using Chemical Probes to Examine Cellular Activities
<p>Chemical probes are valuable tools for investigating rapid cellular processes, such as anaphase in cell division, by allowing for the modulation of protein activity over the course of minutes. In addition, resistance to chemical probes by mutation can provide insight into inhibitor binding …
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Chemical probes for the study of mitochondrial oxidative stress
… In this thesis three novel classes of chemical probes for the study of oxidative stress are presented. Firstly, progress was made towards a novel mitochondria-targeted hydroxylamine iii based on the 1,1,3,3-tetraethylisoindoline (TEIO) scaffold. This hydroxylamine iii should undergo …
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VHL inhibitors as chemical probes of the hypoxia signalling pathway
… α remain to be elucidated. The development of a chemical probe that unambiguously blocks the VHL:HIF α interaction downstream of HIF α hydroxylation by prolyl hydroxylase domain (PHD) enzymes, would address biological questions about VHL molecular targets and functional consequences of disrupting …
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Chemical Probes and Strategies to Study Mycobacterial Cell Envelope Assembly
… their function. In this work, we discuss chemical approaches to study and manipulate mycobacterial cell envelope biosynthesis. Specifically, we present biosynthetic glycan labeling strategies that leverage the activity of native glycosyltransferases to probe arabinogalactan and …
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Chemical probes for studying cyclooxygenase-2 and nitric oxide in living systems
… molecular imaging relies on the development of chemical or biochemical tools that accumulate at the site of interest or under undergo a selective, observable change following target engagement. Activity-based sensing is a powerful expansion of molecular imaging because it measures chemical …
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Development of Non-covalent Chemical Probes for μ, δ and κ Opioid Receptors
… prescribing practices. The development of new chemical probes will assist in further understanding opioid-receptor interactions and will serve to advance this field of research. As a part of a collaborative Ontario Tech University-Purdue Pharma program, the synthesis of opioid derivatives for …
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MODIFICATION OF XANTHENE AND SILICON ANALOGUES OF XANTHENE FLUOROPHORES FOR CHEMICAL PROBES DEVELOPMENT
… of fluoresceins and development of pH probes based on rhodamines. We have modified the xanthene core of fluorescein by replacing the xanthene oxygen with a dimethylsilyl group which shows 90 nm red-shift relative to fluorescein (λabs/λem =582 nm/598 nm). These fluorophores have …
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Mapping the synapse : synthesis and validation of chemical probes for interrogating PDZ domains
… of sensitive and selective biophysical probes. The peptidyl probes are based on three critical elements: solvatochromic fluorophores, molecular caging, and multivalency. This thesis presents the development of a systematic approach to screen for selective solvatochromic fluorophore-based …
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Structural studies of paired PHD finger-bromodomain chromatin-binding modules: targeting epigenetic readers with chemical probes
The use of chemical probes is a powerful tool that can help to address important biological questions.<br/><br/>The study presented in this thesis aims to target reader domains of chromatin-associated proteins with small molecules, in order to provide information on their ligandability, useful to …
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Computational and synthetic approaches in the design and development of chemical probes for estrogen receptor function
… from collaborators, to design and develop chemical probes of ER function. The underlying mechanisms driving ligand affinity and selectivity remain a key focus in understanding ER function. Correspondingly, we describe the development of imidazo[1,2-a]pyridine ligands to probe the importance …
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Targeting Transcription Factors in Neuroblastoma: Development of Aurora Kinase A/N-Myc Degraders and ID2 Chemical Probes
… discuss our efforts in the development of novel chemical modulators of TFs in neuroblastoma using targeted protein degradation. N-Myc overexpression is the most frequent driver in neuroblastoma. Unique features of N-Myc biology offer innovative approaches for developing chemical modulators of …
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Investigating the expression and function of aldehyde dehydrogenases in prostate cancer. Probing the expression and function of ALDHs using chemical probes, drugs and siRNA
… committed basal (CB) cells. Novel ALDH-affinic probes showed reduced cell viability of primary prostate epithelial cultures as a single agent and also when used in combination with docetaxel. The results indicate the potential of using ALDH-affinic compounds as single agents for therapeutic …
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Investigating the expression and function of aldehyde dehydrogenases in prostate cancer. Probing the expression and function of ALDHs using chemical probes, drugs and siRNA
… committed basal (CB) cells. Novel ALDH-affinic probes showed reduced cell viability of primary prostate epithelial cultures as a single agent and also when used in combination with docetaxel. The results indicate the potential of using ALDH-affinic compounds as single agents for therapeutic …
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Development of chemical probes for intracellular nucleotide delivery, profiling of the metabolic fate(s) of nucleoside monoester phosphoramidates, and a nucleotide mimetic inhibitor of eIF4E
… guanosine monophosphate, as a chemical tool for translational control of protein synthesis. Furthermore, in Chapter 3 we provide another proof-of-concept application of the new pronucleotide strategy for intracellular delivery of 2´-C-β-Methyl guanosine monophosphate as an …
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Efforts toward an enantioselective total synthesis of (–)-oxazolomycin B and simplified chemical probes for proteomics studies; pharmacophore-directed retrosynthesis applied to gracilin A : simplified bioactive derivatives.
The oxazolomycins are bioactive peptide-polyketide hybrid natural products first isolated in 1985 by Uemura and co-workers from Streptomyces bacteria. Their complex structure and wide-ranging bioactivity against various human cancer cell lines, grampositive bacteria, and viruses like HIV, herpes, …
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Dopamine Transporter (DAT) and Metabotropic Glutamate Receptor 5 (MGLU5) Irreversible Probes for Identifying Anti-Psychostimulant Therapeutics
… of this research was to develop irreversible chemical probes based on select DAT inhibitors and mGlu5 NAMs in order to map the corresponding binding sites and poses of these compounds within their major drug targets. The central hypothesis was that these compounds could be derivatized, without …
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