Search for dissertations about: "Helena Danielson"

Showing result 11 - 15 of 21 swedish dissertations containing the words Helena Danielson.

  1. 11. Fragment-based drug discovery : Novel methods and strategies for identifying and evolving fragment leads

    Author : Edward A. FitzGerald; Helena Danielson; Hanna-Kirsti Schrøder Leiros; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; Biochemistry; Drug Discovery; Biophysics; Fragment-based drug discovery; Epigenetics; Biosensors; Surface Plasmon Resonance; Interaction Analysis; Second-Harmonics; Biokemi; Biochemistry;

    Abstract : The need for new drugs became ever more apparent in the year 2020 when the world was faced with a viral pandemic. How drugs are discovered and their relevance to society became part of daily discussions in workplaces and homes throughout the world. Consequently, efficient strategies for preclinical drug discovery are clearly needed. READ MORE

  2. 12. Biosensor Studies of Ligand Interactions with Structurally Flexible Enzymes : Applications for Antiviral Drug Development

    Author : Matthis Geitmann; U. Helena Danielson; Marc H. V. van Regenmortel; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; Biochemistry; SPR biosensor; HIV-1 reverse transcriptase; HCMV protease; interaction kinetics; drug discovery; non-nucleoside inhibitor; resistance; Biokemi; Biochemistry; Biokemi;

    Abstract : The use of a surface plasmon biosensor fills a missing link in kinetic studies of enzymes, since it measures directly the interaction between biomolecules and allows determination of parameters that are determined only indirectly in activity assays. The present thesis deals with kinetic and dynamic aspects of ligand binding to two viral enzymes: the human cytomegalovirus (HCMV) protease and the human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT). READ MORE

  3. 13. Protease Activity, Inhibition and Ligand Interaction Analysis : Developments and Applications for Drug Discovery

    Author : Thomas Gossas; Helena Danielson; Mikael Widersten; Alexander Wlodawer; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; Biochemistry; proteases; kinetics; biosensors; inhibition; calcium; drug discovery; Biokemi;

    Abstract : The present study has focused on characterising protease-ligand interactions in the context of drug discovery. The proteases that have been studied are human matrix metallopeptidase 12 (MMP-12), HIV-protease and Hepatitis C virus (HCV) NS3/NS4A protease. READ MORE

  4. 14. Sensitivity, Noise and Detection of Enzyme Inhibition in Progress Curves

    Author : Omar Gutierrez Arenas; Helena Danielson; Athel Cornish-Bowden; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; Biochemistry; Progress curves; limit of detection; Z -factor; primary screening; enzyme inhibition; error structure; sensitivity analysis; High-throughput screning; Biokemi;

    Abstract : Starting with the development of an enzymatic assay, where an enzyme in solution hydrolysed a solid-phase bound peptide, a model for the kinetics of enzyme action was introduced. This model allowed the estimation of kinetic parameters and enzyme activity for a system that has the peculiarity of not being saturable with the substrate, but with the enzyme. READ MORE

  5. 15. Exploring Inhibitors of HIV-1 Protease : Interaction Studies with Applications for Drug Discovery

    Author : Maria T. Lindgren; Helena Danielson; Jozsef Tözser; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; Biochemistry; kinetics; biosensors; ADME; drug discovery; SPR; resistance; inhibition; copper; Biokemi; Biochemistry; Biokemi;

    Abstract : A variety of HIV-1 protease inhibitors and their interactions with the enzyme have been characterized in order to identify novel and improved drugs against AIDS. The investigated inhibitors were represented by clinical and non-clinical inhibitors, active site and allosteric inhibitors, transition-state analogues and metal-ions. READ MORE