Sökning: "Structure-activity relationship"
Visar resultat 1 - 5 av 84 avhandlingar innehållade orden Structure-activity relationship.
1. Lysophosphatidic acid : Physiological effects and structure-activity relationships
Sammanfattning : Lipids havepreviously been considered primarily as building blocks of the cell membrane, but are now also recognized as important cell signaling molecules. Lysophosphatidic acid (LPA) is a glycerophospholipid consisting of a phosphate head group, a linker region, and a lipophilic tail. LÄS MER
2. Internalization mechanisms of cell-penetrating peptides : Structure-activity relationships, cellular distribution and membrane toxicity studies
Sammanfattning : Transport of substances with pharmaceutical potential over the plasma membrane has been pushed a great step forward with the discovery of short cationic polypeptides, known as cell-penetrating peptides (CPP). Since then, the internalization mechanism and cargo delivery properties of CPPs has been extensively studied. LÄS MER
3. Epoxides as Contact Allergens - Formation, Sensitising Potency and Structure-Activity Relationships
Sammanfattning : Chemicals in our environment with which we have repeated skin contact can cause skin sensitisation (contact allergy). To trigger an immune response a compound (hapten) must be able to penetrate the skin, where it needs to be reactive enough to bind to proteins and form immunogenic complexes that are recognised as foreign. LÄS MER
4. Discovery of Small Peptides and Peptidomimetics Targeting the Substance P 1-7 Binding Site : Focus on Design, Synthesis, Structure-Activity Relationships and Drug-Like Properties
Sammanfattning : Biologically active peptides are important for many physiological functions in the human body and therefore serve as interesting starting points in drug discovery processes. In this work the neuropeptide substance P 1–7 (SP1–7, H-Arg-Pro-Lys-Pro-Gln-Gln-Phe-OH), which has been demonstrated to reduce neuropathic pain and attenuate opioid withdrawal symptoms in animal models, has been addressed in a medicinal chemistry program with the overall aim of transforming this bioactive peptide into more drug-like compounds. LÄS MER
5. Cyclic sulfamides as HIV-1 protease inhibitors : Synthesis, X-ray structure analysis and structure-activity relationship
Sammanfattning : Human Immunodeficiency Virus (HIV) is the causative agent of Acquired Immune Deficiency Syndrome (AIDS). Inhibition of HIV-1 protease leads to immature and non-infectious viral particles. The synthesis of a number of cyclic HIV-1 protease inhibitors and the subsequent evaluation in an enzyme assay is presented in this thesis. LÄS MER