Sökning: "Fragment based drug discovery"

Visar resultat 1 - 5 av 18 avhandlingar innehållade orden Fragment based drug discovery.

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

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

   Sammanfattning : 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. LÄS MER

3. 2. Fragment Based Drug Discovery with Surface Plasmon Resonance Technology

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

   Sammanfattning : 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. LÄS MER

4. 3. Introducing weak affinity chromatography to drug discovery with focus on fragment screening

   Författare :Minh-Dao Duong-Thi; Sten Ohlson; Brian Dymock; Linnéuniversitetet; []
   Nyckelord :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;

   Sammanfattning : 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. LÄS MER

5. 4. Revealing Secrets of Synaptic Protein Interactions : A Biosensor based Strategy

   Författare :Christian Seeger; U Helena Danielson; Sarah Lummis; Uppsala universitet; []
   Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Surface plasmon resonance; biosensor; AMPA receptor; GABAA receptor; ligand-gated ion channel; A-kinase anchoring protein; caldendrin; calmodulin; HIV; fragment based drug discovery; Biokemi; Biochemistry; Neuroscience; Neurovetenskap;

   Sammanfattning : Protein interactions are the basis of synaptic function, and studying these interactions on a molecular level is crucial for understanding basic brain function, as well as mechanisms underlying neurological disorders. In this thesis, kinetic and mechanistic characterization of synaptic protein interactions was performed by using surface plasmon resonance biosensor technology. LÄS MER

7. 5. Discovery and evaluation of direct acting antivirals against hepatitis C virus

   Författare :Eldar Abdurakhmanov; Helena Danielson; David Frick; Uppsala universitet; []
   Nyckelord :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;

   Sammanfattning : 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%. LÄS MER