Search for dissertations about: "novel inhibitors"
Showing result 6 - 10 of 443 swedish dissertations containing the words novel inhibitors.
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6. Inhibitors of Human and Malaria Parasite Dihydroorotate Dehydrogenase
Abstract : In the first part of the PhD work, small chemical entities (fragments) found to inhibit human dihydroorotate dehydrogenase (DHODH), were chemically optimized. As part of an ample program at Active Biotech to find new drugs against autoimmune diseases, expanded fragments were repeatedly designed, synthesized and evaluated in a human DHODH assay. READ MORE
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7. Modulating Sirtuin Activity - Design, Synthesis and Evaluation of Sirtuin 2 Inhibitors
Abstract : Sirtuins (SIRTs) are NAD+-dependent lysine deacetylating enzymes targeting histones and a multitude of non-histone proteins. The SIRTs have been related to important cellular processes such as gene expression, cell proliferation, apoptosis and metabolism. They are proposed to be involved in the pathogenesis of e.g. READ MORE
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8. Discovery of Novel Macrocyclic Ligands for Difficult Targets : Applications to Natural Product Derived Keap1 Inhibitors
Abstract : The development of small-molecule ligands for biological targets that possess large, featureless or highly polar binding sites is a challenging task. This thesis is focused on a novel lead generation strategy to identify macrocyclic ligands for difficult-to-drug targets, as well as on the relationship between cell permeability and the conformations of macrocycles. READ MORE
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9. Development and Application of Computational Methods in Antitubercular Drug Design : Identification of Novel Inhibitors of Ribonucleotide Reductase
Abstract : Tuberculosis kills approximately 1.7 million people each year around the world making it one of the most lethal infectious diseases. This thesis concerns the development of two computational tools that can support the early stages of drug discovery, and their use in an anti-tubercular drug discovery program. READ MORE
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10. Towards Anti-Virulence Antimicrobials, Discovery and Development of Sortase A Inhibitors and Investigations of Bacterial Phenotypes
Abstract : Antibiotic resistance is an emerging and serious threat to public health. Immediate actions are required to preserve current antibiotics while intensifying research efforts towards the development of new effective therapeutics. READ MORE