Search for dissertations about: "Macrocyclic inhibitors"

Showing result 11 - 15 of 16 swedish dissertations containing the words Macrocyclic inhibitors.

  1. 11. Design and Synthesis of Inhibitors Targeting the Hepatitis C Virus NS3 Serine Protease and the Aspartic Protease BACE-1

    Author : Marcus Bäck; Ingemar Kvarnström; Stephen Hanessian; Linköpings universitet; []
    Keywords : NATURAL SCIENCES; NATURVETENSKAP;

    Abstract : This thesis describes the synthesis of molecules designed to inhibit the hepatitis C virus (HCV) NS3 serine protease and the human aspartic protease BACE-1, and it also reports the structure-activity relationships between potential inhibitors and the targeted enzymes. In addition, consideration is given to the class of enzymes known as proteases, as well as the question of why such enzymes can be regarded as suitable targets for developing drugs to combat diseases in general. READ MORE

  2. 12. Advanced NMR techniques for structural elucidation in medicinal chemistry

    Author : Hermina Wieske; Máté Erdélyi; Mikael Akke; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES;

    Abstract : The nuclear Overhauser effect (NOE) is an NMR phenomenon that can reveal spatial proximity between two atoms. It has found applications in organic chemistry and structural biology including natural product chemistry, organic synthesis, medicinal chemistry, macromolecular structure elucidation and protein-ligand interactions. READ MORE

  3. 13. The solution conformations of macrocycles. Applications in the exploration of weak interactions and in drug development

    Author : Emma Danelius; Göteborgs universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; Macrocycles; cyclic peptides; NMR; solution conformational analysis; NAMFIS; β-hairpin; weak interactions; halogen bonding; protein-protein interaction; bioactive conformation; macrolides; cell permeable conformation.;

    Abstract : Understanding the solution conformation and dynamics of molecules with biological relevance, as well as the impact of their conformation stabilizing weak interactions, is for example important for drug design. Macrocycles have attractive pharmaceutical properties, and are of special interest as drug leads for targets with large, flat and featureless binding sites like protein-protein interfaces. READ MORE

  4. 14. Interaction kinetic analysis in drug design, enzymology and protein research

    Author : Vladimir O Talibov; U. Helena Danielson; Glyn Williams; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; Biokemi; Biochemistry;

    Abstract : The work presented here is focused on the phenomenon of molecular recognition – the mutual ability of biological molecules to recognize each other through their chemical signatures. Here, the kinetic aspects of recognition were evaluated, as interaction kinetics reveal valuable dimensions in the description of molecular events in biological systems. READ MORE

  5. 15. Design and Synthesis of Angiotensin IV Peptidomimetics Targeting the Insulin-Regulated Aminopeptidase (IRAP)

    Author : Hanna Andersson; Anders Hallberg; Anders Karlén; Federico Corelli; Uppsala universitet; []
    Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; angiotensin IV; AT4; insulin-regulated aminopeptidase IRAP ; inhibitor; peptidomimetics; γ-turn mimetic; macrocycle; Pharmaceutical chemistry; Läkemedelskemi; Medicinal Chemistry; Läkemedelskemi;

    Abstract : Peptidomimetics derived from the bioactive hexapeptide angiotensin IV (Ang IV, Val1-Tyr2-Ile3-His4-Pro5-Phe6) have been designed and synthesized. These peptidomimetics are aimed at inhibiting the insulin-regulated amino peptidase (IRAP), also known as the AT4 receptor. READ MORE