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 18 of 18 for “"druggable target"”.
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Overactive NF-KB signaling as a druggable target and evaluation of parthenolide an NF-KB inhibitor in canine cancer
… transcription factors that have 400+ genetic targets, and are involved in many vital cellular processes, including innate immunity, inflammatory responses, development, cellular growth, and survival. Not surprisingly, overactivation of NF-kB is a feature of many chronic disease processes, …
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INHIBITING THE NUCLEAR RECEPTOR ESRRA RESCUES CORE PATHOLOGIES IN CELLULAR AND ANIMAL MODELS OF BATTEN DISEASE
… that ESRRA may represent a novel therapeutic target for multiple BDs. Transcriptomic analysis revealed that pharmacological inhibition of ESRRA with XCT-790 triggers a beneficial metabolic reprogramming by further suppressing defective mitochondrial respiration, activating the PPARG pathway, …
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Development of Glyco-RNA Technologies & Elucidating the Roles of miRs in Head and Neck Cancer Metastasis
… which this process arises from and find druggable targets. Our findings uncover miR-206 as a differentially regulated miR in metastatic tumors. We then predict and validate its downstream target TAGLN2 to regulate metastatic potential. These discoveries are important as they highlight …
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Synthesis Of Natural Product-Based Sphingosine Derivatives
… of sphingosine to S1P and has been examined as a druggable target for the treatment of hyper-proliferative diseases, inflammation, cancer and other pathological conditions. Natural products that consist of an azetidine ring represents an interesting class of conformationally constrained scaffolds …
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CROSSTALK BETWEEN TUMOUR VASCULATURE AND OVARIAN CANCER STEM CELLS: THE ROLE OF L1CAM.
… TME and OCSC, therefore, offers a source of new targets and mechanisms to overcome the limitations of current treatments. We identified L1CAM, an adhesion glycoprotein, expressed both in tumour endothelium and epithelial cancer cells, as a mediator of the interaction between the vascular TME …
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Small molecules with anti-trypanosomal and anti-leishmanial activity
… activity and a good selectivity profile. Further target identification studies on the effect of these new inhibitors using in vitro assays confirmed inhibition of GPI anchor biosynthesis as a mode of action. This provides further evidence that the GPI anchor is a druggable target for the …
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Investigating the genome of Anaplastic Lymphoma Kinase-positive Anaplastic Large Cell Lymphoma
… disease pathology and to uncover novel targets for therapy, Whole-Exome Sequencing (WES) of ALK+ ALCL was performed, as well as Gene-Set Enrichment Analysis. This revealed that the Notch pathway was the most enriched in mutations. In particular, variant T349P of Notch1, which confers a …
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Towards systems pharmacology models of druggable targets and disease mechanisms
… cost effective decisions on drug viability and target druggability and therefore attempt to reduce this time-consuming and costly attrition. Using text mining and text classification I present a growing landscape of systems pharmacology models in literature growing from humble roots because of …
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Protein-based Degrader Strategies against Oncogenic RAS
Targeted therapies have emerged as a promising cancer treatment strategy by inhibiting proteins specific to cancer cells while preserving healthy cells. RAS proteins play a crucial role in cancer development and are associated with increased tumor growth and invasion. Mutations in RAS genes, …
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Molecular cloning, recombinant protein expression and structural characterization of a universal stress G4LZI3 protein from Schistosoma mansoni
… have such shared features can be very useful targets for disease intervention. Universal stress proteins (USPs) act as natural biological defence mechanisms in living organisms. They are overexpressed in stress conditions and assist in overcoming stressors through various mechanisms. USPs has …
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An in vitro chemogenomic screening system to identify the molecular targets of antimalarial drug candidates
… promising hit compounds, but elucidating the targets of these compounds, often a necessary step in the hit-to-lead development process, has been slow. This is because target identification has rested primarily on one technique, *in vitro* evolution and whole genome sequencing (IVIEWGA), which …
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Structural Characterization of the Switch domain regions of Schistosoma mansoni druggable Adenylate cyclase-stimulating Gα-protein
… of S. mansoni has been identified as a promising druggable target against the parasite. The broad focus of this study was to explore the solubility, stability and druggability of the Gα protein from the switch domain regions of S. mansoni. In-silico analysis of the switch domain regions using …
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Investigating fibroblast growth factor and its role in canine osteosarcoma
… is even more compelling if the stimulus is a druggable target. Fibroblast growth factors (FGFs) interact with fibroblast growth factor receptors (FGFRs) to initiate cell signaling that is important in embryonic development, wound healing, and angiogenesis. FGF2, also termed basic FGF (bFGF), …
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Functional identification of molecular oncotargets associated with the resistance to ALK inhibition in neuroblastoma via genome-wide CRISPR-Cas9 screens
… Lymphoma Kinase (ALK) as the only directly ‘druggable’ target with a significant mutation rate (9%). ALK is a receptor tyrosine kinase whose dysregulation has been implicated as the driver lesion in a variety of cancer types, including Non-Small Cell Lung Cancer (NSCLC) and various paediatric …
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Role of Neuraminidase-mediated Desialylation in Microglial Activation
… that blockage of sialidase may be a novel druggable target for neurodegenerative disease research. The effect of microglia- induced desialylation in trans was also investigated by desialylating neurons by sialidase or conditioned medium from LPS-treated microglial cultures, and it was found …
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Synthesis, pharmacological and physicochemical profiling of antimalarial and antischistosomal N-aryl 3-trifluoromethyl pyrido [1,2-α] benzimidazoles
… development of novel drugs with the ability to target multiple parasite stages and be efficacious against resistant parasite strains to achieve effective control and treatment of malaria and schistosomiasis. Originating from a World Health Organisation-Tropical Disease Research initiative, a …
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Probing the chemical biology involved in the haem detoxification pathway of the human malaria parasite, plasmodium falciparum
… (CQ), amodiaquine (AQ) and piperaquine (PPQ) target this process, the pathway has received tremendous recognition within the drug discovery and development arena as a valuable, druggable target. However, the pathway involves multiple processes that are equally important and present as …
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ASSESSMENT OF RELEVANT MOLECULAR TARGETS WITH THERAPEUTIC SIGNIFICANCE IN CANINE NEOPLASMS.
… have highlighted the need for effective, targeted therapies. While targeted therapies such as tyrosine kinase inhibitors, monoclonal antibodies, antibody-drug conjugates, and immunocytokines have transformed human oncology, their application in veterinary medicine remains limited by scant …