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 513 for “"antagonists"”.
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Novel Agonists and Antagonists of Platelet Receptors
Platelets are central for the primary haemostatis. The platelet has surface bound receptors that are vital for the platelet activation. One of these receptors, the purinergic ADP-activated G-protein coupled receptor (GPCR) P2Y12 is a key receptor for platelet activation, and thus for thrombus …
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Engineering of bacterial exotoxin and endotoxin antagonists
Limited Restriction Lifted for Item 89522 on 2017-09-30T09:15:35Z.
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Directed Evolution of T Cell Receptor Antagonists
In Chapter 4, further engineering of TCR stability mutants to produce increased affinity binding for SAg is described. An optimized TCR fragment (containing nine mutations) was isolated after mutagenesis and selection, and was found to have approximately 1000-fold improved affinity for SAg. A …
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Configurationally restricted bis-tetraazamacrocyclic complexes: chemokine receptor antagonists
The chemokine receptor CXCR4 is a trans-membrane protein which has been implicated in many physiological and pathological processes including cancer, rheumatoid arthritis and most significantly HIV replication. CXCR4 plays a vital role in embryonic development but is not essential at the …
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Synthesis and Characterisation of Dual CCR7/CXCR4 Antagonists
… identified a series of sulfonamides as CCR7 antagonists. This project aims to extend on those studies and to develop a dual CCR7 and CXCR4 antagonist to reduce metastasis in cancer. Novel potent biaryl sulfonamide CCR7 antagonists were synthesised and assessed by calcium flux assay. Several …
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Ligand-receptor interactions of Gonadotropin-releasing hormone antagonists
The interactions of selected GnRH agonists and antagonists with the GnRH receptor were investigated using site directed mutagenesis and photoaffinity cross/inking of the receptor with a labelled GnRH analog. With the aim of identifying residues involved in ligand binding, the relative affinities of …
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Synthesis and Development of Potential CB1 Receptor Neutral Antagonists
<p>Cannabis and its derivatives have been used for both medicinal and recreational purposes. The study of this plant led to the discovery of over 60 cannabinoids, found exclusively in cannabis, that contribute to the behavioral effects of cannabis use, the most common is …
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Engineering Soluble, High Affinity Receptor Antagonists for Bacterial Exotoxins
Chapter four describes the engineering of murine Vbeta8.2 for picomolar affinity to staphylococcal enterotoxin B (SEB). As the known contact regions had already been heavily mutagenized, additional engineering of the Vbeta was performed through extension of the CDR1 loop. Soluble forms of the …
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Design and Synthesis of Small-Molecule Protein-Protein Interaction Antagonists
… of the compound. In Chapter two, small-molecule antagonists targeting uPA-uPAR protein-protein interaction are presented. A total of 500 commercially-available compounds were previously identified by virtual screening and tested by a FP assay. Three classes of compounds were found with biological …
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Effects of Single and Dual Orexin Receptor Antagonists on Trigeminal Nociception
… orexin peptides. Single and dual orexin receptor antagonists have been synthesized to selectively block the activity of these orexinergic receptors. I hypothesized that a single orexin receptor antagonist blocking orexin receptor 2 would have the same inhibitory effect as a dual orexin receptor …
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Profiling the activity of GPR55 antagonists against recombinant and endogenous GPR55
… selective pharmacological tools. However, novel antagonists have recently been developed, allowing for the determination of GPR55-selective effects. The objective of the present study was to utilise molecular imaging techniques to evaluate the effectiveness of two previously published novel GPR55 …
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Characterisation of Novel Autophagy and Necroptosis Antagonists Encoded by Human Cytomegalovirus
Human cytomegalovirus (HCMV) is a ubiquitous herpesvirus that causes significant morbidity and mortality in immunocompromised individuals. To support its intracellular survival, HCMV has evolved diverse strategies to manipulate key host pathways and evade intrinsic immune defences. In this thesis, …
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Allies or Antagonists: Alberta Elementary Teachers’ Current Perceptions of School Psychologists
Using a mixed-methods design, the present study investigates Alberta elementary teachers’ perceptions of school psychologists, specifically examining their knowledge about school psychologists and school psychological services, teachers’ experience and use of these services, and their satisfaction …
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The synthesis and evaluation of small organic molecules as cholecystokinin antagonists
… discussion on the many types of CCK receptor antagonists is included. For the drug discovery process, a number of synthetic approaches have been investigated and alternative chemical approaches developed. 1,4-Benzodiazepine analogues were prepared, with substitutents In the 1,2 & 3- position …
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Identification of Novel CCR4 Antagonists Through Inhibition of CCL22-Induced Cell Migration
… In this study, I investigated 78 potential CCR4 antagonists using an in vitro transmigration assay, focusing on the inhibition of CCL22-mediated migration. RAW 264.7 cell lines, as well as CCR4-transfected HEK293T cells, were used in our studies. Our findings demonstrated increased migration of …
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Characterisation of novel compounds as antagonists of protease-activated receptor-2 (PAR2)
… the lack of potent and selective small-molecule antagonists. Recently, a number of new putative antagonists including GB88 and AZ8838 have been proposed to be effective in cells and in vivo. However, given the relative lack of information about these compounds this thesis examined the …
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The synthesis and biochemical and pharmacological evaluation of gamma-aminobutyric acid antagonists
… with the examination of a number of GABA antagonists in two in vitro assay systems. A series of cage-structured compounds including bicyolic phosphate esters (2,6,7,-Trioxa-l-phosphabicyclo (2,2,2,) octan-l-oxides with suitable 4-substituents) have been shown to be potent a GABA …
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Effects of selective neurotensin receptor antagonists on responding for brain stimulation reward
… of systemic administration of two selective NT antagonists, SR-48692 and SR-142948a, on responding for medial mesencephalic electrical stimulation. The curve-shift method adapted to operant responding for brain stimulation reward was used to assess reward and performance changes following …
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Development of screening assays to test novel integrin antagonists in allergic inflammation
… (HTS) for identification of novel integrin antagonists for the treatment of ocular allergy and to better understand the mechanisms of action of integrin-mediated levocabastine antiallergic action. Results: This thesis provides evidence that adopting scintillation proximity assay (SPA) …
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BIOLOGICAL AND TRANSDUCTIONAL EFFECTS OF ALLOSTERIC ANTAGONISTS ON THE ACTIVITY OF CHEMOATTRACTANT RECEPTORS
… This model of concerted type of allosteric antagonists raises the possibility to stabilize slightly different active receptor conformations, which might interact preferentially with distinct tranducer molecules or signaling pathway. Moreover, this class of antagonists would offer untapped …
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