Sökning: "AT2"

Visar resultat 1 - 5 av 21 avhandlingar innehållade ordet AT2.

  1. 1. Computational Modeling of the AT2 Receptor and AT2 Receptor Ligands : Investigating Ligand Binding, Structure–Activity Relationships, and Receptor-Bound Models

    Författare :Christian Sköld; Anders Karlén; Anders Hallberg; Torbjörn Lundstedt; Tommy Liljefors; Uppsala universitet; []
    Nyckelord :Pharmaceutical chemistry; Angiotensin II; AT1; AT2; SAR; bioactive conformation; turn mimetic; peptidomimetic; DISCO; homology model; 3D-QSAR; CoMFA; Farmaceutisk kemi;

    Sammanfattning : Rational conversion of biologically active peptides to nonpeptide compounds with retained activity is an appealing approach in drug development. One important objective of the work presented in this thesis was to use computational modeling to aid in such a conversion of the peptide angiotensin II (Ang II, Asp-Arg-Val-Tyr-Ile-His-Pro-Phe). LÄS MER

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

    Författare :Jennie Georgsson; Anders Hallberg; Kevin Burgess; Uppsala universitet; []
    Nyckelord :MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; 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

  3. 3. 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 :MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; 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

  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

  5. 5. On angiotensin II receptor type 2 receptors in the small intestine

    Författare :Sara Ewert; Göteborgs universitet; Göteborgs universitet; Gothenburg University; Göteborgs universitet; Gothenburg University; []
    Nyckelord :renin-angiotensin; angiotensin; small intestine; mucosa; epithelium; AT1; AT2; bradykinin; BK2 receptor; nitric oxide; iNOS; smooth muscle; contractility;

    Sammanfattning : The endocrine renin-angiotensin system (RAS) is important in the regulation of extracellular fluid volume and systemic blood pressure in strenuous conditions such as hypovolemia. Also present locally in peripheral tissues, all components of RAS are expressed and have been shown to modulate development, cell growth and inflammation. LÄS MER