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 50 for “"Competitive Binding"”.
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Testing the Role of Cyclic Nucleotides in Regulating Ion Channels Essential to Pollen Fertility
… visualized using fluorescent biosensors, and a competitive binding assay was designed to gauge CNGC binding affinity for cNMPs. cAMP- and cGMP- specific biosensors showed strong, uniform fluorescence throughout pollen tube; the competitive binding assay was not completed due to laboratory …
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A Break In Communication: The Synthesis, Characterization, DNA Binding and Photocleavage of a Novel Ruthenium Polypyridyl Complex Containing an Electronically Isolated Pyrene Group
… experiments including isothermal and competitive binding titrations in addition to the hydrodynamic technique of viscometry were used to show that [Ru(bpy)2bpy-py]2+ binds to DNA with a binding constant of 8 x 105 and 1x106 M-1 (binding constants calculated using isothermal and …
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Mechanisms of CCR5 Agonist/Antagonist Inhibition of HIV-1 Entry and In Vitro Selection of Virus Resistant to Maraviroc
… of entry. The studies presented here demonstrate competitive binding between the envelope glycoprotein and inhibitor for CCR5 is a major mechanism involved in sensitivity to PSC-RANTES. Although downregulation of coreceptor expression from the cell surface was instigated by PSC-RANTES binding, …
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In Vitro Binding and Transport Regulation by Endothelial Cells: Preliminary Studies looking at FIX and IGF-I
… targeted at understanding the mechanisms of binding and transport across endothelial cells cultured in vitro. Specifically, the first study investigates how the recombinant source of Factor IX (FIX), a blood coagulant protein used in the treatment of Hemophilia B, impacts surface ligand …
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Purification and Characterization of the Prostate Cancer-Associated Antigen: 7E11-C5
… protein (PSP)) were unable to block the binding of MAb 7E11-C5 to its target antigen. Western blot analysis demonstrated that there was no similarity between the 7E11-C5 antigen and these three antigens. The 7E11-C5 antigen was purified 400-fold from LNCaP xenograft tissue extract by …
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Towards decomposition of phosphonates in water using catalytic membranes: paraquat on silica as a proxy
… by the contaminant onto silica surfaces. Competitive binding model predictions are found to be consistent with experimental adsorption data. Addition of an exogenous agent (e.g. H2O2) was also attempted to assist paraquat decomposition; however, investigation of paraquat-H2O2 interaction …
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A Survey of Stapling Methods to Increase the Affinity, Activity and Stability of Ghrelin Analogues
… affinity and α-helicity were measured using competitive binding assays and circular dichroism spectroscopy, respectively. Generally, an increase in alpha-helicity using a flexible staple linker led to an improved affinity towards GHSR. Ghrelin(1-20) analogues with a lactam, triazole, and …
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Nickel Reduces Calcium Dependent Dimerization In Neural Cadherin
… Cell-cell adhesion by cadherins requires the binding of calcium ions to specific sites in the extracellular region. Given the complexity of the cell adhesion microenvironment, we are investigating whether other divalent cations might affect calciumdependent dimerization of neural-(N-) …
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Detection of explosive materials
… non-specialised personnel. This research uses a competitive immunoassay format, which arises from competitive binding between a free form and a bound form of the analyte. Successful detection of explosive material: 2,4,6-trinitrotoluene (TNT) has been demonstrated via a competitive immunoassay …
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Expanding the Spiroligomers Toolbox as Protein-Protein Interaction Inhibitors
… undertaken before each molecule was tested for binding to HDM2, a natural binding partner of p53. A library of molecules was synthesized on solid support that altered the stereochemistry along the spiroligomer as well as the presented functional groups. It was determined that spiroligomers enter …
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Estrogens Containing Alkylating Substituents: The Synthesis and Estrogen Receptor Interactions of Estradiol and Hexestrol Affinity Labels
… reactive than the chloro ones. Their reversible binding to the lamb uterine estrogen receptor was measured by competitive binding assays, and their irreversible reaction with receptor was measured by exchange assays that determine the rate and extent of receptor inactivation. In general, …
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Synthesis and modification of pamam dendrimers as histone replacement molecules
… linear dichroism, dynamic light scattering and competitive binding of ethidium. Experiments designed to investigate modified dendrimer-lipid interactions are also discussed and the results of these are compared to molecular dynamic simulations. The synthesis of novel small molecules based around …
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Electrophilic Affinity Labels and Fluorescent Conjugates for the Estrogen Receptor (Norhexestrol, Aziridine, Hexestrol, Fluorescein, Alkylator)
… terminus which was linked to the bis-phenol binding component of hexestrol by various functionalities: ketone, ester, thioether, or methylene chain. The apparent competitive binding affinity of these derivatives for the estrogen receptor ranges from 1.8-25% of that of estradiol. Most of the …
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Novel genotoxins that target estrogen receptor- and androgen receptor- positive cancers : identification of DNA adducts, pharmacokinetics, and mechanism
… at the 11[beta] position (11[beta]). Competitive binding experiments show that E2-7[alpha] and 11[beta] compete well with the natural ligands for the ER and AR, respectively. Clonal survival studies have shown that hormone receptor expressing malignant cell lines are more sensitive to …
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Graph Representation Learning for Drug Discovery
… a mechanism to assess drug combinations through competitive binding to such targets. Third, we extend the search for new drugs beyond known chemical matter by developing deep generative models that can realize novel compounds with better characteristics. To this end, we propose hierarchical graph …
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Designing Allosteric Inhibitors of Thrombin
… to reduce thrombin activity. There are several binding domains on thrombin including the active site, anion-binding exosites I and II, and the sodium binding site. We hypothesized that thrombin may be better regulated through an allosteric process mediated by small molecules binding to either …
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A STUDY OF THE THERMODYNAMICS OF ANION BINDING TO HUMAN SERUM TRANSFERRIN
… environment of the ion centers of the protein by binding to specific anion sites. The binding of these anions (thiocyanate, perchlorate, adenosinetriphosphate, pyrophosphate, and chloride) is shown to occur pairwise with high positive cooperativity, an observation unique to nonstereospecific …
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Mechanistic Study of The Small Molecule Inhibitor DX-52-1
… protein whose best-known function is its sugar binding ability, as a secondary target of DX-52-1 with functions in cell motility. In addition, we have identified HUK-921, another small molecule with antimigratory activity that has far greater selectivity for galectin-3 over radixin both <em>in …
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Mechanistic studies to evaluate the targeting specificity of novel RGD Micelles to the αVβ3 integrin receptor
… and further evaluated for their RGD-mediated binding specificity to purified <strong>αVβ3</strong> integrin through a competitive binding fluorescence polarization assay (with novel RGD micelles displacing an integrin-bound fluorescent RGD probe by as much as 63.03%). Ultimately, these …
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