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Showing 1 to 20 of 133 for “"Chemical Biology"”.
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Chemical Biology of Dynein
… and the lack of an inhibitor with the requisite chemical properties, such as compound solubility and stability, for structural studies. The work presented here describes the design and characterization of a class of dynein probes, one of which we use to obtain an inhibitor-bound structure of …
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Chemical biology of matrix metalloproteases
… of a??Click Chemistrya?? in constructing focused chemical libraries, we have been able to apply this strategy to synthesise a 96-membered library of metalloprotease inhibitors followed by in situ screening. Moreover by using the same strategy, we successfully demonstrate that the facile synthesis …
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SORTASE AND CHEMICAL BIOLOGY AS TOOLS TO STUDY UBIQUITINATION
… accessibility to new aspects of ubiquitin biology that were previously inaccessible.
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Chemical Biology Tools to Study Bacterial Cell Surface Glycans
… address this open challenge, we developed novel chemical biology tools to study bacterial cell surface glycans. We have established a new, generalizable strategy for chemoselective glycan modification to enable the study of specific bacterial cell wall glycans. Our method relies on the direct …
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UNDERSTANDING SULFUR BASED REDOX BIOLOGY THROUGH ADVANCEMENTS IN CHEMICAL BIOLOGY
Sulfenic acids are fleeting intermediates formed from the oxidation of cysteine thiols by a number of biologically relevant oxidants. Sulfenic acids are quickly converted to other species including disulfides, thiosulfinates, sulfinic acids, or sulfonic acids, leading to changes in protein …
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Chemical Biology Tools for Biochemical and Functional Analysis of Myosin Phosphatase
… the PPP1R12C–PP1cβ holoenzyme using a suite of chemical biology tools. To overcome challenges posed by PPP1R12C’s intrinsic disorder and the dynamic assembly of the complex, we employed mammalian expression systems and AlphaFold modeling to predict structure and optimize expression. A …
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CHEMICAL BIOLOGY STRATEGIES FOR THE FORMATION AND CLEAVAGE OF CHEMICAL BONDS
… and better understanding of how specific chemical bonds can be either formed or broken gives chemical biologists opportunities to control and regulate these processes with high precision. Therefore, with growing importance of the field of chemical biology, expansion of the toolbox of …
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Wnt signaling in zebrafish fin regeneration : chemical biology using a GSK3β inhibitor
Bone growth can be impaired due to disease, such as osteoporosis. Currently, intermittent parathyroid hormone (PTH) treatment is the only approved therapy in the United States for anabolic bone growth in osteoporosis patients. The anabolic effects of PTH treatment are due, at least in part, to …
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A chemical biology study of human embryonic stem cell pluripotency and differentiation
… High-throughput screening (HTS) of combinatorial chemical libraries is widely used for the search of such bioactive small molecules. My dissertation has focused on using HTS to identify novel small molecules that regulate hESC pluripotency and differentiation. Using a HTS system based on a novel …
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Chemical Biology Approaches to Interrogate Heat Shock Transcription Factor 1 Regulation in Cancer
… basis of HSF1 regulation as well as available biochemical tools to investigate such details are lacking. Based on an in vitro ligand binding approach, the studies presented in this thesis were dedicated to the identification, validation, and characterization of a direct, first-in-class, …
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Using chemical biology as a tool to probe the mechanism of the HDL receptor
The high density lipoprotein (HDL) receptor, scavenger receptor, class B, type I (SR-BI), is a cell surface glycoprotein that controls HDL structure and metabolism by mediating cellular selective uptake of lipids from HDL. The mechanism underlying SR-BI-mediated lipid transfer involves a two-step …
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Chemical Biology, Biochemical and Structural Studies of MDN1, an AAA Protein Required for Ribosome Biogenesis
… of its function. Here, I first combined chemical and biochemical approaches to develop and validate ribozinoindoles (Rbins) as the cell-permeable inhibitors of Mdn1, which are the first potent and selective inhibitors of ribosome biogenesis in eukaryotes. These compounds can be further …
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Development of fluorescent chemical biology tools for the detection and delivery of aldehyde-associated biology
Submission original under an indefinite embargo labeled 'Open Access'. The submission was exported from vireo on 2022-11-11 without embargo terms
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Development of Novel Chemical Biology Tools for Probing Structure-Function Relationships in G Protein-Coupled Receptors
… extracellular signals into intracellular biochemical responses. Understanding with chemical precision how GPCRs function in cellular membranes is an active area of biological research, but despite recent reports of X-ray crystal structures of several GPCRs, some important questions remain …
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From Probes to Cell Surface Labelling: Towards the Development of New Chemical Biology Compounds and Methods
Chemical biology encompasses the study and manipulation of biological system using chemistry, often by virtue of small molecules or unnatural amino acids. Much insight has been gained into the mechanisms of biological processes with regards to protein structure and function, metabolic processes and …
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Probing the chemical biology involved in the haem detoxification pathway of the human malaria parasite, plasmodium falciparum
… in future and to gain deeper insight into the biology underpinning the haem detoxification pathway. To measure changes in the DV lumen volume and uptake, a method using confocal microscopy was optimised and coupled to image analysis techniques. Untreated parasites were allowed to reinvade RBCs …
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Development of novel chemical biology tools to probe malaria parasite physiology and aid in antimalarial drug discovery
… is especially challenging due to the unique biology of malaria parasites, the scarcity of tools for identifying new drug targets, and the poorly understood mechanisms of action of existing antimalarials. Therefore, this work describes the development of two chemical biology tools to address …
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Targeting Virulence as an Approach to Bacterial Pathogenesis: Efforts Towards the Development of Chemical Biology Tools and Anti-Chlamydial Therapeutics
… is a need for the discovery and development of chemical biology tools that can be used to probe the function of chlamydial effectors, and in turn possibly reveal therapeutic targets for antibiotic development. Here we report efforts toward the design, synthesis, and evaluation of small molecules …
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Development of a chemical biology approach for glycoprotein discovery in Caenorhabditis elegans reveals glycosylated isoforms of multiple proteins with mitochondrial function
… function.The first such method is a chemical biology approach for the discovery of glycoproteins in Caenorhabditis elegans (C. elegans). Despite the classic strengths of C. elegans for cell biology and genetics, very few chemical biology approaches are effective in this system. To …
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