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 43 for “"Covalent binding"”.
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Covalent Binding and other Mechanisms of Primaquine Toxicity
<p>A dose-dependent covalent binding of primaquine to mouse liver microsomal protein was found in both in vitro and in vivo studies. The binding in vitro was linear during the first 90 minutes of incubation and dependent on the concentration of mouse liver microsomal protein. The in vitro covalent …
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Untersuchung und Spezifizierung der molekularen Interaktion von Ubiquitin und Sumo mit dem rekombinanten a1-Glyzinrezeptor
The specification of covalent posttranslational modification by sumoylation and ubiquitination of membrane proteins – in this case of the GlyR alpha 1-subunit and its ubiquitin mediated internalisation – is described. The clinical relevance of those mechanisms is wide spread and would in this case …
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Reactivity of Re₂(CH₃COO)₂Cl₄·2H₂O with purine DNA dinucleotides
<p>Covalent binding of dinuclear metal carboxylate compounds to purine DNA nucleobases has been shown to be a source of anticancer activity, and has resulted in intense research to understand the coordination of metal complexes to DNA. This investigation focuses on the formation of dirhenium …
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Ribonucleotide reductase in dividing cells: Purification and inhibition studies with 4-hydroxynonenal
… microsomes was studied. Spin trapping of CCI3', covalent binding of CCl4 to protein and CCl4-dependent MDA formation were used as indices of CCl4 metabolism. Formation of PBN-CCI3' adduct, 14CCl4 covalent binding to protein and CCl4-dependent :MDA production were dependent on temperature range …
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Evaluation of potential photodynamic therapy agents and patient-relevant biomarker combinations for the selective targeting of cancer
… complex, Ru(II)-Rh(III), with DNA. Non-covalent binding of Ru(II)-Rh(III) is strong and involves electrostatic and, potentially, groove binding interactions. Ru(II)-Rh(III) photobinds and photocleaves DNA through an O2-independent, metal-center mediated mechanism that could be beneficial …
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Polyelectrolyte multilayers incorporating photocrosslinking polymers for controlling 2- and 3-dimensional structure
… these polymers in the film and their resultant binding state. Patterning covalent binding through photo-crosslinking in addition to electrostatic binding, can locally override the native tendency to change structure with changes in pH. To achieve this, poly(acrylic acid) was chemically modified …
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Photosynthetic antenna-reaction-center mimicry
… to yield long-lived charge-separated states. Covalent and non covalent binding strategies have been employed in the design and synthesis of these novel artificial antenna-reaction centers. The synthesized molecular systems are characterized using standard spectroscopic techniques. Their …
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Biomolecular interactions and cellular effects of steroidal and metallosupramolecular metallodrugs
… to the project, surveying different DNA-binding modes, explaining their importance in the anticancer properties of metallodrugs and showing an overview of the different strategies used for enhanced delivery of these metallodrugs. In Chapter 2 the synthesis of new steroidal DNA …
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Mixed-Metal Ruthenium-Platinum Polyazine Supermolecules: Synthesis, Characterization and Exploration of DNA Binding
… ruthenium and platinum, which would display covalent binding to DNA. Drawing upon the well-established efficacy of cis-diamminedichloroplatinum(II) (cisplatin) and the DNA-binding properties of select ruthenium polyazine complexes, the approach was to bind the cis-PtIICl2 active site of …
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SALICYLALDEHYDE-TAGGED PEPTIDES FOR THE REVERSIBLE-COVALENT ENGAGEMENT OF PROTEIN LYSINE RESIDUES
Covalent drug discovery has recently re-emerged as a powerful approach for targeting clinically-relevant proteins, offering enhanced potency and selectivity through controlled covalent interactions. In particular, reversible covalent (RC) chemistry combines the strength of covalent binding with the …
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Solid-supported synthesis of peptidoglycan fragments and their biological evaluation
… 1 is a reversible covalent binding inhibitor of R39. These data are supported by an enzymatic study using the thioesterase activity of the R39 peptidase on (R)-S2d. Because of the specific affinity for the R enantiomer of thioesters, the enantioselective synthesis of …
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Insights Into the Dynamic Structure and Inhibitory Mechanism of Plasminogen Activator Inhibitor Type 1
… at several steps, perturbing the initial non-covalent binding, slowing the formation of the acyl-enzyme complex, and compromising the stabilization of the acyl-enzyme intermediate. The work provides a more comprehensive structural model for the active conformation of PAI-1 and illuminates a …
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Assembly and detection of viruses and biological molecules on inorganic surfaces
… and consensus sequences were achieved. Virus binding was characterized using Atomic Force Microscopy, Fluorescene Microscopy and Titration. Using a simple bimolecular model, the binding sequence identified through this work is shown to have a binding constant 100,000 times better than a random …
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Ultrafast infrared spectroscopy investigation of DNA-ligand interactions
… a high-throughput analysis method to study non-covalent binding of small molecules to minor grooves of DNA duplex structures. Minor groove binding to DNA is relevant in the development of potential new therapeutics that target specific DNA sequences to influence a biological process. The …
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Biochemical and computational studies towards selective inhibition of the immunoproteasome
… with 3 inhibitors gaining FDA approval. However, covalent binding and lack of targeted action cause severe toxicity. Upon stimulation by inflammatory cytokines, constitutive proteasome (CP) active sites β1c, β2c and β5c are replaced with corresponding β1i, β2i and β5i subunits; forming the …
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Development of stapled peptide targeted covalent inhibitors and synthesis of novel ADC payloads for applications in cancer therapy
… 1) Development of stapled peptide–targeted covalent inhibitors (SPTCIs) of p53–MDM2 protein–protein interaction (PPI). Herein, the development and synthesis of three novel electrophilic staples and four stapled peptides are described. The stapled peptides bear moieties to covalently target a …
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Immunoassays with chemically modified bacteriophage
… a variety of conditions. The success of the covalent binding of protein to phage particles depends on finding conditions under which a proportion of the phage remains viable and, at the same time, can still be neutralized by anti-protein sera. To this end, different proportions of reactants …
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Towards Multiplexed Nuclear Magnetic Resonance for Environmental Analysis
… NMR can identify unknown pollutants, examine non-covalent binding in soils and, uniquely, study biochemical changes in living organisms. Here, novel approaches are explored to address current challenges and further improve the utility of environmental NMR. The ability to study organisms in vivo …
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Effects of plant flavonoids on the fate of polynuclear aromatic hydrocarbons in rhizosphere soil
… in abiotic control soil. A biologically mediated covalent binding between phenolic moieties may be responsible for the enhanced bound residue formation. Relatively high percentage bound residues were found to be associated with higher clay, soil organic matter, and humus contents in soil. …
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Development of Mass Spectrometric Methods for the Analysis of Components and Complex Interactions in Biological Systems
… spectrometry studies, have shown that a stronger binding affinity equates to a greater efficacy of the drug. For the determination of drug:dye complex binding strength coefficients in solution, two methods have been developed by affinity capillary electrophoresis (ACE), and cation exchange liquid …
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