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 9 of 9 for “"irreversible inhibitors"”.
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Halo Enol Lactones as Enzyme-Activated Irreversible Inhibitors of Chymotrypsin: Their Synthesis, Kinetics, and Mechanism of Inactivation (Suicide Substrates)
Halo enol lactones can act as enzyme-activated irreversible inhibitors or suicide substrates for (alpha)-chymotrypsin. Acyl transfer to the active site serine generates a halo methyl ketone that remains tethered in the catalytic site during the lifetime of the acyl enzyme, available for reaction …
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Halo Enol Lactones as Enzyme-Activated Irreversible Inhibitors of Alpha-Chymotrypsin: I. The Effect of Lactone Substitution Pattern. Ii. Alpha - Amino-Functionalized Lactones
… compare their effectiveness as enzyme-activated irreversible (suicide) inhibitors for (alpha)-chymotrypsin with the activities of the corresponding (alpha)-substituted lactones. The 4-phenyl-5(E)-(iodomethylidene) tetrahydro-2-furanone, the 4-phenyl-5(E)-(iodomethylidene)dihydro-2-furanone, the …
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Development of animal models in pediatric cancer
… was designed to test a panel of reversible and irreversible inhibitors of cathepsin B and L to induce death of neuroblastoma cells. Efficacy of the compounds depends on their ability to inhibit enzyme activity of cathepsins B and L. Five compounds that differ in mode and rate of inhibition of …
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Design, Synthesis and Evaluation of Covalent Inhibitors for Tissue Transglutaminase and Factor XIIIa
… the discovery of potent and selective covalent inhibitors for each isozyme, namely hTG2 and hFXIIIa. The first project was concentrated on the inhibition of hTG2 activity. Ubiquitously expressed in tissues, hTG2 is a multifunctional enzyme. Its primary activity is the formation of isopeptide …
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Structural Analysis of Cycle Inhibiting Factor from Pathogenic Escherichia Coli
… on a wild-type catalytic triad, whereas irreversible inhibitors of cysteine protease activity do not affect the cytopathic phenotype. Finally, we identify the cell cycle regulatory protein Nedd8 as an interaction partner for Cif. Cif binds Nedd8 in vitro through both the catalytic domain …
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Propoxyphene, Norpropoxyphene, and Proadifen (SKF-525A) Are Mechanism Based Inhibitors of CYP3A4, CYP3A5, and CYP3A in Human Liver Microsomes
… and norpropoxyphene are mechanism-based (irreversible) inhibitors of CYP3A, and to determine if propoxyphene and norpropoxyphene are reversible inhibitors of CYP3A. Mechanismbased inhibition is a type of irreversible inhibition that results from an inhibitor or its metabolite binding to an …
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Mechanisms and Targeting of Neurodevelopmental Regulator Rest In Medulloblastoma Dissemination
… in the context of normal and high REST. However, irreversible inhibition of LSD1 had no effect on cell viability but did exert a REST-dependent reduction of migration. Ingenuity pathway analysis of RNA-sequencing data revealed that irreversible inhibition of LSD1 reduced cell migration signaling …
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The synthesis & optimisation of irreversible ITK inhibitors as a potential new treatment for severe asthma
… inflammatory response in asthmatic patients. ITK inhibitors could represent useful anti-inflammatory agents for severe asthma. This thesis describes the design and development of irreversible ITK inhibitors. It was envisaged that these compounds could provide a better duration of action in vivo …
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A Binary Approach for Selective Recognition of Nucleic Acids and Proteins
… approach was also applied to design covalent inhibitors for HIV-1 reverse transcriptase (RT). In this application, two separate pre-reactive groups were attached to a natural RT ligand, deoxythymidine triphosphate (dTTP). Upon binding of both dTTP analogs in the RT active site, the …