Sökning: "thrombin inhibitor"

Visar resultat 1 - 5 av 47 avhandlingar innehållade orden thrombin inhibitor.

  1. 1. A New Look into Protein C Inhibitor : Posttranslational Modifications and their Functions

    Författare :Wei Sun; Sophia Schedin Weiss; Hakon Leffler; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Protein C inhibitor; posttranslational modifications; N-glycan; O-glycan; mass spectrometry; factor Xa; thrombin; prostate specific antigen; Biochemistry; Biokemi; Biokemi; Biochemistry;

    Sammanfattning : The influences of posttranslational modifications on the functions of the versatile serpin protein C inhibitor (PCI) were studied. PCI is a serine protease inhibitor that is expressed in many tissues and secreted to various fluids in human, including blood plasma, seminal plasma, and urine. LÄS MER

  2. 2. Structure-Based Design and Synthesis of Protease Inhibitors Using Cycloalkenes as Proline Bioisosteres and Combinatorial Syntheses of a Targeted Library

    Författare :Fredrik Thorstensson; Ingemar Kvarnström; Charles Hedgecock; Linköpings universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; organic chemistry; organic synthesis; combinatorial synthesis; metathesis; olefin metathesis; thrombin; HCV; NS3; protease; proline isosteres; inhibitor; Organic synthesis; Organisk syntes;

    Sammanfattning : Structure-based drug design and combinatorial chemistry play important roles in the search for new drugs, and both these elements of medicinal chemistry were included in the present studies. This thesis outlines the synthesis of protease inhibitors against thrombin and the HCV NS3 protease, as well as the synthesis of a combinatorial library using solid phase chemistry. LÄS MER

  3. 3. In vivo Pharmacokinetics of Two New Thrombin Inhibitor Prodrugs : Emphasis on Intestinal and Hepatobiliary Disposition and the Influence of Interacting Drugs

    Författare :Elin Matsson; Hans Lennernäs; Lars Knutson; Ulf Eriksson; Kim Brouwer; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Direct thrombin inhibitors; prodrugs; ximelagatran; AZD0837; erythromycin; ketoconazole; drug-drug interactions; hepatobiliary transport; biliary clearance; ATP-binding cassette; ABC transporters; solute carriers; SLC transporters; CYP3A4; Biopharmacy; Biofarmaci; Biopharmaceutics; Biofarmaci;

    Sammanfattning : Biliary excretion is an important elimination route for many drugs and metabolites. For such compounds, it is important to know the extent of excretion and drug exposure in the bile, e.g., for the risk assessment of drug interactions, liver toxicity and the effects of genetic variants. LÄS MER

  4. 4. Design, Synthesis and Characterization of Small Molecule Inhibitors and Small Molecule : Peptide Conjugates as Protein Actors

    Författare :Jonas Nilsson; Lars Baltzer; Ingemar Kvarnström; Thomas Olsson; Linköpings universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Synthetic receptor; Peptide inhibitor conjugate; Peptide protein surface interactions; General Lead Discovery Library; Combinatorial Chemistry; Solid Phase Chemistry; Targeted Library; Thrombin inhibitor; Fluorescence; Surface Plasmon Resonance; Organic chemistry; Organisk kemi;

    Sammanfattning : This thesis describes different aspects of protein interactions. Initially the function of peptides and their conjugates with small molecule inhibitors on the surface of Human Carbonic Anhydrase isoenzyme II (HCAII) is evaluated. LÄS MER

  5. 5. Early assessment of efficacy and safety of novel anticoagulants as exemplified by direct thrombin inhibitors. Non-clinical pharmacodynamic studies in vitro and in vivo

    Författare :Margareta Elg; Göteborgs universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; animals; antidote; bleeding; inhibition constant; inogatran; association rate constant; melagatran; thrombin inhibitor; thrombosis; fibrinolysis;

    Sammanfattning : The drawbacks of today's anticoagulants are parenteral use (heparins), a narrow interval between efficacy and bleeding, and the high variability of effect with a consequent need for frequent monitoring (coumarins). The aim of the current studies was to evaluate properties important for efficacy and safety of novel anticoagulants, as exemplified by direct thrombin inhibitors, with non-clinical methods. LÄS MER