Search for dissertations about: "Fragment-Based Lead Discovery"

Showing result 1 - 5 of 7 swedish dissertations containing the words Fragment-Based Lead Discovery.

  2. 1. Accelerating the discovery of drugs for Neglected Tropical Diseases using biophysical methods

    Author : Giulia Opassi; Helena Danielson; Jenny Sandmark; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; NATURVETENSKAP; NATURAL SCIENCES; Neglected Tropical Diseases; Drug Discovery; Biochemistry; Biophysics; Kinetic; Fragment Based Lead Discovery; Assay Development;

    Abstract : Even though they account for 10% of the global disease burden and besides the new record of funding in 2018, tropical diseases are still neglected by the majority of pharmaceutical companies and public funding. The reason can be mostly found in the fact that for these diseases a conventional drug discovery process is often too expensive. READ MORE

  4. 2. Discovery and evaluation of direct acting antivirals against hepatitis C virus

    Author : Eldar Abdurakhmanov; Helena Danielson; David Frick; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; Direct acting antivirals; Hepatitis C; NS3-4A protease; NS5B polymerase; structure-based drug discovery; fragment-based drug discovery; surface plasmon resonance; Biokemi; Biochemistry;

    Abstract : Until recently, the standard therapy for hepatitis C treatment has been interferon and ribavirin. Such treatment has only 50% efficacy and is not well tolerated. The emergence of new drugs has increased the treatment efficacy to 90%. READ MORE

  5. 3. Molecular simulations of G protein-coupled receptors : A journey into structure-based ligand design and receptor function

    Author : Pierre Matricon; Jens Carlsson; Bjørn Olav Brandsdal; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; G Protein-Coupled Receptor; Molecular Dynamics Simulations; Free Energy Perturbation; Ligand Binding; Fragment-Based Lead Discovery; Molecular Docking Screens; Homology Modeling; GPCR Activation Mechanism; Biology with specialization in Molecular Biotechnology; Biologi med inriktning mot molekylär bioteknik;

    Abstract : The superfamily of G protein-coupled receptors (GPCRs) contains a large number of important drug targets. These cell surface receptors recognize extracellular signaling molecules, which stimulates intracellular pathways that play major roles in human physiology. READ MORE

  6. 4. Progress of Weak Affinity Chromatography as a Tool in Drug Development

    Author : Elinor Meiby; Sten Ohlson; Manfred Raida; Linnéuniversitetet; []
    Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; NATURVETENSKAP; NATURAL SCIENCES; NATURVETENSKAP; NATURAL SCIENCES; weak affinity chromatography; fragment based drug discovery; fragment screening; thrombin; trypsin; cyclin G-associated kinase; Hsp90; Pin1; cyclooxygenase; lipodisks; Biokemi; Biochemistry;

    Abstract : Weak Affinity Chromatography (WAC) is a technology that was developed to analyse weak (KD > 10-5 M) although selective interactions between biomolecules. The focus of this thesis was to develop this method for various applications in the drug development process.Fragment Based Drug Discovery is a new approach in finding new small molecular drugs. READ MORE

  7. 5. Reducing Attrition via Improved Strategies for Pre-clinical Drug Discovery : SPR-biosensor Aided Interaction Studies

    Author : Johan Winquist; Helena Danielson; Roderick E. Hubbard; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; Biokemi; Biochemistry;

    Abstract : The efficacy of a drug is tightly intertwined with its interaction mechanism with the drug target. The mechanism is dependent on the physicochemical and structural characteristics of both target and drug molecule.Drug discovery is plagued by a high attrition rate, whereas in the clinic, a major issue is drug resistance. READ MORE