Sökning: "turn mimetics"

Visar resultat 1 - 5 av 10 avhandlingar innehållade orden turn mimetics.

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

3. 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

4. 3. Synthesis of β-turn and pyridine based peptidomimetics

   Författare :David Blomberg; Jan Kihlberg; Kay Brickmann; Torbjörn Frejd; Umeå universitet; []
   Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Peptidomimetics; beta-turn; beta-strand; pyridine scaffold; Grignard exchange reaction; SNAr reaction; thrombin inhibitor; Leu-enkephalin.; Organic synthesis; Organisk syntes;

   Sammanfattning : Despite the unfavorable pharmacokinetic properties associated with peptides, they are still of great interest in drug development due to a multitude of interesting biological functions. The development of peptidomimetics strives to maintain or improve the biological activity of a peptide concurrently with removing the unwanted properties. LÄS MER

5. 4. Studies towards ß-turn mimetics, synthesis of kedarosamine from threonine, and synthesis of glycopeptides from mucins and gp120

   Författare :Tatjana Vuljanic; Centrum för analys och syntes; []
   Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Tn antigen; glycopeptides; glycosylation; diastereselective reduction; kedarosamine; kedarcidin chromophore; amino acids; peptide T; ß-turn mimetic; Organisk kemi; gp120; Organic chemistry;

   Sammanfattning : The secondary structure of proteins is crucial for proper function of the protein in biological systems. Peptide T, an octapeptide from the envelope glycoprotein gp120 of the HIV virus, has previously been shown to be responsible for binding to the CD4 receptor on T helper/inducer lymphocytes. LÄS MER

7. 5. 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