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 101 for “"small molecule inhibitor"”.
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Mechanistic Study of The Small Molecule Inhibitor DX-52-1
… and cancer cell invasion and metastasis. Small organic molecules inhibiting cell migration can be used as both research probes and therapeutic agents. DX-52-1, a semisynthetic derivative of the natural product quinocarmycin (also known as quinocarcin), inhibits the migration of Madin-Darby …
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Structural analysis of LMO2 for the development of a small molecule inhibitor
… LMO2 for structure based drug development of small molecules that will target LMO2 protein-protein interactions. LMO2 could not be purified alone as removal of the fusion tag resulted in severe precipitation of the free LMO2. Consequently, LMO2 was co-expressed with an antibody single domain …
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Characterization of Selective Inhibition of Adenylyl Cyclase Activity By Small Molecule Inhibitor Nky80
… cyclase (AC), via synthesis of the signaling molecule cyclic AMP (cAMP), are involved in many isoform specific physiological functions. Decreasing AC5 activity has been shown to have potential therapeutic benefit, including reduced stress on the heart, pain relief, and attenuation of morphine …
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Investigating a novel small molecule inhibitor of nuclear import as an anti-cancer approach
… model, we showed that its inhibition using small-interfering RNA (siRNA) resulted in cancer cell death via apoptosis while sparing normal cells, suggesting it has potential as a target for anti-cancer therapy. An in silico screen for Kpnβ1 inhibitors identified several small molecules that …
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CHARACTERISATION OF A NOVEL SMALL MOLECULE INHIBITOR FOR IMMUNE ACTIVATION IN TRIPLE NEGATIVE BREAST CANCER
… Our group has previously identified a novel small molecule inhibitor, CHL-4, whose anti-tumour effects function through Lyn kinase, a member of the Src family kinases. This current study characterised a novel immunomodulatory role for CHL-4, which is able to increase gene and protein …
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Investigating the effect of a small molecule, Inhibitor of Nuclear Import (INI-43) as a pan-cancer treatment
… a nuclear import protein that transports cargo molecules from the cytoplasm into the nucleus and plays an important role in other cellular processes such as mitosis and mitotic spindle assembly, DNA replication and cell cycle progression. Previous studies in our laboratory have reported that …
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Structural investigation of 1,8-dinitro-4,5-dihydroxyanthraquinone and implications for docking as a small molecule inhibitor into the protease of West Nile virus
… drug would decrease the disease burden. The small molecule, 1,8-dinitro-4,5-dihydroxyanthraquinone has shown to bind the proteases of the dengue and West Nile viruses while also reducing their titers in cell-based assays. Structure-based analog design will likely be performed in the near …
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Identification and characterization of a small molecule inhibitor of IMP-1 that decreases expression of IMP-1 target mRNAs and inhibits proliferation of IMP-1 positive cancer cells
… high throughput screen of approximately 150,000 small molecules. Reported here is BTYNB, the first small molecule inhibitor of IMP-1, BTYNB decreases levels of IMP-1 target mRNAs, inhibits proliferation of IMP-1 positive cancer cells, and functions through the unique mechanism of decreasing …
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In Vitro and in Vivo Pharmacodynamic Characterization of the Novel Plasma Kallikrein Inhibitor Pf-04886847
… study was to develop and characterize a novel small molecule inhibitor of plasma kallikrein and to evaluate its potential usefulness in the treatment of kallikrein-mediated inflammatory and thrombotic disorders. Using in vitro biochemical assays, PF-04886847 was identified as a potent and …
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Development of peptide-based 19F MRI agents and BPTF-bromodomain inhibitors
… In a second project, the development of a small molecule inhibitor of an epigenetic protein target is described. AU1, the first reported small molecule inhibitor of the bromodomain of a protein called BPTF, was discovered in the Pomerantz lab in 2015. As BPTF is a relatively understudied …
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FUNCTIONAL ANALYSIS OF ANAPLASTIC LYMPHOMA KINASE DURING EMBRYONIC NEUROGENESIS IN ZEBRAFISH
… in alk by, Morpholino knock-down and a small molecule inhibitor compromised neuronal differentiation and neuron survival in the CNS, but left progenitor formation intact. Also Midkine, a putative ligand for Alk and receptor protein tyrosine phosphatase zeta (RPTPz), a known Alk …
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METHODS OF AREA-SELECTIVE ATOMIC LAYER DEPOSITION OF A METAL OXIDE USING SMALL MOLECULE INHIBITORS AND COMPETITIVE ADSORPTION
… on Cu were studied. Blocking performance using a small molecule inhibitor (DMATMS) applied through pre-soak and/or cyclically in situ vs. a self-assembled monolayer (ODTS) prepared ex situ was assessed using different precursor (TMA, BDMADA-Al), co-reactant (H2O, t-BuOH), and process temperature …
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Identification of the Phosphatase NUDT5 as a Target for the Treatment of Triple Negative Breast Cancer
… remain as conventional chemotherapy and PARP inhibitors (only applicable for a subset of BRCA-mutated TNBC patients). Consequently, our focus has been on the exploration of innovative targeted therapies for TNBC. This study investigated the novel phosphatase, NUDT5, as a potential therapeutic …
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Preclinical evaluation of a novel telomerase inhibitor in malignant cells of the hematopoietic system
… most cancer cells. Recently, a non-nucleosidic small molecule inhibitor, BIBR1532, has been identified which is highly selective for the inhibition of telomerase resulting in telomere dysfunction and delayed growth arrest in tumor cells. Here we examined the effects of BIBR1532 in different …
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Small molecule inhibition of immunoregulatory protein-protein interactions
… (PPIs) between cells, receptors, and secreted molecules. Generating and maintaining an appropriate immune response and regulation requires coordination across many cell types and components, while dysregulation of these interactions can lead to disease. A major obstacle in small molecule …
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Synthesis, biological activity and mechanism of atypical carotenoid antilipoperoxidants
… remains enigmatic. We posited that a potent small molecule inhibitor of lipid peroxidation could be a useful probe to understand the role of lipid peroxidation in human disease. Carotenoids are an extensively studied class of polyene containing small molecules with antilipoperoxidant …
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Targeting MERTK on tumour cells and macrophages: a potential intervention for sporadic and NF2-related meningioma and schwannoma tumours
… or the vascular endothelial growth factor inhibitor bevacizumab. The main objective of this thesis was to investigate targeting of the receptor tyrosine kinase MERTK as a potential pharmacological intervention in schwannomas and meningiomas. Immunofluorescence and flow cytometry …
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Modulating the expression and activity of the nuclear import protein, Karyopherin β1, in cancer cells
… from our laboratory using a newly identified small molecule, Inhibitor of Nuclear Import-43 (INI-43), showed that INI-43 significantly reduced the proliferation of cancer cells of different tissue origins and interfered with the nuclear import function of Kpnβ1. In order to investigate the …
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The effect of inhibiting KPNB1-mediated nuclear import on cancer cell biology and inflammatory transcription factor signalling
… and to characterise the in vivo effect of the small molecule inhibitor of nuclear import, INI-43, on tumour formation. Using siRNA and a small molecule inhibitor, INI-43, to inhibit KPNB1 we found that cervical cancer cell migration and invasion was significantly reduced. The reduced motility …
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Effect of a novel contraceptive compound on vaginal health
… to block the semen liquefaction process using a small molecule inhibitor called triazole B1. B1 acts to block the activity of prostate specific antigen, the serine protease responsible for initiating the liquefaction process by cleaving the protein SEMG-1. B1 is intended to be used as a local …
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