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 14 of 14 for “"activity-based protein profiling"”.
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Kinetic Characterization, Inhibition, and Activity-Based Protein Profiling of Protein Arginine Methyltransferase 1
<p>Protein arginine methyltransferases (PRMTs) are SAM-dependent enzymes that catalyze the mono- and di-methylation of peptidyl arginine residues. Although all PRMTs produce mono-methyl arginine (MMA), type I PRMTs go on to form asymmetrically dimethylated arginine (ADMA), while type II enzymes …
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Activity-Based Protein Profiling Reveals Changes to the Regulation of Enzymatic Activity by the Hepatitis C Virus
… are built, maintained, and controlled by the activity of enzymes. Understanding how enzymes contribute to the regulation of various pathways and processes allows us to gain a deeper understanding of the entirety of the biological system. As changes in enzyme activity are often essential for …
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Synthesis of activity-based protein profiling probes for malaria and hypertension disease models & potential novel ACE inhibitors with an attenuated zinc binding group
Angiotensin-converting enzyme (ACE) and P. falciparum A M1 (PfA-M1) are both zinc metalloproteases implicated in hypertension and malaria, respectively. Hypertension affects approximately 26 % of the world’s population while each year over 300 million cases of malaria occur worldwide resulting in …
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Design and Synthesis of an E3 ligase Activity-Based Probe and its Application for the Discovery of a New Class of E3 Ligase
… yet there are currently no effective tools for profiling their activity. Herein, a new class of E3 activity-based probe (ABP) is presented which is built by re-engineering ubiquitin (Ub)-charged E2 conjugating enzymes. The utility of these probes has been demonstrated by the rapid dissection of …
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PROTEOMICS INSIGHTS INTO MOLECULAR MECHANISMS OF TRIPTOLIDE AGAINST COLORECTAL CANCER
… cytoskeleton, cell migration, cell adhesion, protein synthesis and induce alteration of transcription factors in colorectal cancer cell line HCT 116. In my first project, protein alterations of HCT 116 cells treated with triptolide were profiled at a global level, by using Isobaric Tags for …
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Ligand-Driven Development of Pd-Catalyzed Nondirected C–H Activation of Arenes
… Using a dual-ligand palladium catalyst system based on an N-acylsulfonamide (NASA) ligand and a pyrazine-derived ligand, the methodology enables broad substrate scope and direct access to alkyne-tagged scaffolds suitable for copper-catalyzed azide-alkyne cycloaddition (CuAAC) derivatization and …
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Chemical and biochemical studies of ubiquitin conjugation machinery
The post-translational modification of proteins is a major mechanism employed in eukaryotic cells to expand the functional diversity of the proteome. Covalent modification of amino acid side chains confers new or altered functionality to the modified protein by creating new recognition surfaces on …
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Insights into the substrate specificities, interactions and regulatory mechanisms of bacterial glycoconjugate biosynthesis enzymes
… production in the cell. However, the protein-protein interactions that comprise these complexes are poorly understood. In Chapter 3, I explore interactions among a subfamily of monoPGTs known as large (Lg) PGTs in near-native membrane mimetic systems. In this work, I characterize LgPGT …
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Discovery and characterization of a novel Deubiquitinase ZUP1
… (DUBs) regulate the post-translational protein modification<br/>ubiquitylation, which is involved in various cellular processes including protein<br/>degradation, an array of signalling pathways and the DNA damage response.<br/>The recent discovery of a fifth family of cysteine protease …
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Proteome-wide Functional Profiling of Serine Hydrolases in the Human Malaria Parasite
… targets. In this study, we have employed activity-based protein profiling (ABPP) and liquid chromatography-tandem mass spectrometry (LC-MS/MS) to functionally characterize SHs. In our effort to profile plasmodial SHs using ABPP, we have identified a human erythrocyte SH, acylpeptide …
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Proteomic Approaches For Profiling Cofactor-Dependent Proteins In Mycobacterium Tuberculosis
… the necessary chemical moieties to enable activity-based protein profiling experiments. In Chapter 2, we developed a probe that contains an N-hydroxy alanine warhead, which acts as a mechanism-based inhibitor of PLP-dependent enzymes, a linear diazirine for UV-crosslinking, and an alkyne …
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Chemical Tools for Exploring Metabolite Interactions with Nuclear Receptors and Beyond
… characterization of specific metabolite–protein interactions remains a major challenge in chemical biology and drug development. The functionalization of native metabolites and synthetic small molecules with bio-orthogonal detection tags (alkyne, azide, and others) has afforded chemical …
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Functional Characterization of Serine Hydrolases Mediating Lipid Metabolism and Protein Depalmitoylation in Asexual Stage Plasmodium Falciparum
… that PfABHD17A may exhibit depalmitoylase activity in vitro. LPLs are important for asexual stage parasites acquiring FAs from the host. The P. falciparum genome includes 17 putative LPLs while LPLs responsible for hydrolyzing FA from lysophosphatidylcholine (LPC) in the asexual stage are …
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An Activity-Based Proteomics Approach for Identifying Ajoene's S-thiolation Protein Targets in Blood and Cancer Cells
… cytotoxicity have shown that it modifies proteins by S-thioallylating redox-sensitive cysteine residues through a thioldisulfide exchange reaction. Further investigations into this exchange have been the primary aim of this PhD thesis using a biotinylation protocol for trapping out the …