Search for dissertations about: "fragment screening"

Showing result 1 - 5 of 42 swedish dissertations containing the words fragment screening.

  2. 1. Introducing weak affinity chromatography to drug discovery with focus on fragment screening

    Author : Minh-Dao Duong-Thi; Sten Ohlson; Brian Dymock; Linnéuniversitetet; []
    Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; affinity LC-MS; fragment-based drug discovery; fragment screening; high throughput; mass spectrometry; stereoisomer; enantiomer; thrombin; weak affinity chromatography; WAC; WAC-MS.; Biomedical Sciences; Biomedicinsk vetenskap; Biokemi; Biochemistry;

    Abstract : Fragment-based drug discovery is an emerging process that has gained popularity in recent years. The process starts from small molecules called fragments. One major step in fragment-based drug discovery is fragment screening, which is a strategy to screen libraries of small molecules to find hits. READ MORE

  4. 2. 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

  5. 3. Towards a New Generation of Anti-HIV Drugs : Interaction Kinetic Analysis of Enzyme Inhibitors Using SPR-biosensors

    Author : Malin Elinder; U. Helena Danielson; Maurizio Botta; Uppsala universitet; []
    Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; drug discovery; fragment; screening; reverse transcriptase; microbicides; interaction analysis; NNRTIs; Biochemistry; Biokemi; Biokemi; Biochemistry;

    Abstract : As of today, there are 25 drugs approved for the treatment of HIV and AIDS. Nevertheless, HIV continues to infect and kill millions of people every year. Despite intensive research efforts, both a vaccine and a cure remain elusive and the long term efficacy of existing drugs is limited by the development of resistant HIV strains. 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. Fragment Based Drug Discovery with Surface Plasmon Resonance Technology

    Author : Helena Nordström; Helena Danielson; Gregg Siegal; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; Fragment based drug discovery; SPR biosensor; matrix metalloproteinase-12; HIV-1 protease; resistance;

    Abstract : Fragment based drug discovery (FBDD) has been applied to two protease drug targets, MMP-12 and HIV-1 protease. The primary screening and characterization of hit fragments were performed with surface plasmon resonance -technology. Further evaluation of the interaction was done by inhibition studies and in one case with X-ray crystallography. READ MORE