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 “"Small molecule antagonists"”.
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Type I Interferon-Mediated Killing of Cancer Cells with IAP-Targeted Combination Immunotherapy
SMAC mimetic compounds (SMCs) are small molecule antagonists of the Inhibitor of Apoptosis (IAP) family of proteins. Binding of SMCs to the IAPs results in the sensitization of cancer cells to apoptosis in the presence of death ligands, such as tumour necrosis factor alpha (TNFα). I hypothesize …
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Progression of chondrocyte signaling responses to mechanical stimulation in 3-D gel culture
… function-blocking antibodies and small-molecule antagonists were used to disrupt integrin-matrix interactions during dynamic compression of chondrocytes in 3-D agarose culture. At early days in culture, blocking [alpha]v[beta]3 integrin abolished dynamic compression stimulation of …
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The role of CCR7 axis in facilitating chemoresistance, radioresistance and induction of cell proliferation in cancer
… Furthermore, these effects are abrogated by small molecule antagonists (ICT13069), neutralizing monoclonal antibody, or CCR7 knockdown. Our findings support the hypothesis that antagonising CCR7 receptor will not only inhibit cancer metastasis, as it is well-illustrated in the literature, but …
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Design and Synthesis of Small-Molecule Protein-Protein Interaction Antagonists
… Research on the design and synthesis of small molecules to modulate these proteinprotein interactions can lead to new targets and drugs to modulate their function. In Chapter one, we discuss the design and synthesis of small molecules to probe a proteinprotein interaction in a …
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DEVELOPMENT OF ANTAGONISTS TARGETING CHEMOKINE RECEPTOR CCR5 AND THE CHEMOKINE RECEPTOR CCR5 – MU OPIOID RECEPTOR HETERODIMER
… several disease states and can be targeted using small molecule antagonists. Within this work, CCR5’s role in prostate cancer and HIV/AIDS has been exploited in order to develop potential therapeutics and probes. First, a series of novel compounds was designed by using pharmacophore-based drug …
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Characterisation of novel compounds as antagonists of protease-activated receptor-2 (PAR2)
… been limited by 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 …
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Studies of G Protein-Coupled Receptor Stability and Dimerization Using Novel Fluorescence and Crosslinking Approaches
… denaturation measurements demonstrated that small molecule antagonists substantially stabilize CCR5 and also revealed that the ligands induce distinct receptor conformations, consistent with the hypothesis that GPCRs access numerous conformations during signal transduction rather than …
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Chemical Approaches to Dynein Inhibition
… best suited to study this dynamic motor protein. Small molecules (molecular weight <1000 Daltons) can generally engage their target within minutes. However the first cell-permeable small molecule antagonists of dynein, the ciliobrevins, have only recently been identified. As these compounds have …
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Targeting the formyl peptide receptor 1 for treatment of glioblastoma
… of this project was to identify and synthesise small molecule FPR1 antagonists, and to demonstrate a proof of principle in preclinical in vitro and in vivo models that small molecule FPR1 antagonism can retard expansion of glioma. Methods A number of small molecule FPR1 antagonists were …