Sökning: "Ang II peptidomimetics"

Hittade 4 avhandlingar innehållade orden Ang II peptidomimetics.

  1. 1. Design and synthesis of -turn peptidomimetics : Applications to angiotensin II

    Författare :Susanna Lindman; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmaceutical chemistry; peptide synthesis; turn mimetics; molecular modelling; receptor binding affinity; Farmaceutisk kemi; Pharmaceutical chemistry; Farmaceutisk kemi; Organic Pharmaceutical Chemistry; organisk farmaceutisk kemi;

    Sammanfattning : This study addresses the issue of how to convert peptides into drug-like non-peptides while retaining the biological activity at peptide receptors. Angiotensin II (Asp-Arg-Val-Tyr-Ile-His-Pro-Phe, Ang II) was used as a model peptide. Small bioactive peptides are in most cases conformationally flexible molecules. LÄS MER

  2. 2. Design and Synthesis of AT2 Receptor Selective Angiotensin II Analogues Encompassing β- and γ-Turn Mimetics

    Författare :Ulrika Rosenström; Anders Hallberg; Stephen Hanessian; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmaceutical chemistry; Angiotensin II; AT2; AT1; Benzodiazepine; Peptidomimetics; γ-turn; β-turn; Farmaceutisk kemi; Pharmaceutical chemistry; Farmaceutisk kemi;

    Sammanfattning : Important information on the bioactive conformation of biologically active peptides may be obtained by studies of rigid peptides or well-defined secondary structure mimetics incorporated into pseudopeptides. The structural requirements for the interaction of angiotensin II (Ang II, Asp-Arg-Val-Tyr-Ile-His-Pro-Phe) with its AT1 and AT2 receptors were the subject of this study. LÄS MER

  3. 3. Design and Synthesis of Novel AT2 Receptor Ligands : From Peptides to Drug-Like Molecules

    Författare :Jennie Georgsson; Anders Hallberg; Kevin Burgess; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmaceutical chemistry; angiotensin II; AT1; AT2; AT2 receptor agonist; peptidomimetics; γ-turn mimetics; carbonylation; microwave; molybdenum hexacarbonyl; Farmaceutisk kemi; Pharmaceutical chemistry; Farmaceutisk kemi;

    Sammanfattning : Many peptide receptors are of pharmaceutical interest and there is thus a need for new ligands for such receptors. Unfortunately, peptides are not suitable as orally administrated drugs since they are associated with poor absorption, rapid metabolism and low sub-receptor selectivity. LÄS MER

  4. 4. Design, Synthesis and Biological Evaluation of Selective Nonpeptide AT2 Receptor Agonists and Antagonists

    Författare :Charlotta Wallinder; Anders Hallberg; Mathias Alterman; Anders Karlén; Elizabeth E. Sugg; Uppsala universitet; []
    Nyckelord :AT2 receptor agonist; AT2 receptor antagonist; Ang II peptidomimetics;

    Sammanfattning : The G protein-coupled receptors (GPCRs) are important targets in drug discovery. In several cases, the endogenous ligands that activate the GPCRs of pharmaceutical interest are peptides. LÄS MER