Search for dissertations about: "γ-turn"

Found 4 swedish dissertations containing the word γ-turn.

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

    Author : Ulrika Rosenström; Anders Hallberg; Stephen Hanessian; Uppsala universitet; []
    Keywords : 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;

    Abstract : 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. READ MORE

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

    Author : Jennie Georgsson; Anders Hallberg; Kevin Burgess; Uppsala universitet; []
    Keywords : 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;

    Abstract : 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. READ MORE

  3. 3. 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

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

    Author : Susanna Lindman; Uppsala universitet; []
    Keywords : 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;

    Abstract : 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. READ MORE