Sökning: "β-turn"

Visar resultat 1 - 5 av 7 avhandlingar innehållade ordet β-turn.

1. 1. 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

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. Design, Synthesis, and Evaluation of Functionalized Chroman-4-one and Chromone Derivatives. Somatostatin receptor agonists and Sirt2 inhibitors

   Författare :Maria Fridén-Saxin; Göteborgs universitet; []
   Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Chroman-4-ones; Chromones; Inhibitors; Molecular Modeling; Peptidomimetic; Samarium; Sirtuin; Sirt2; Somatostatin; Structure-Activity Relationships; Tubulin; β-Turn;

   Sammanfattning : Peptides are involved in many physiological processes such as regulation of blood-pressure, food intake, pain transmission and blood-glucose levels. They consist of amino acids that are connected through amide bonds which make peptides hydrophilic and conformationally flexible. LÄS MER

5. 4. Towards the Development of Photoswitchable β-Hairpin Mimetics

   Författare :Máté Erdélyi; Adolf Gogoll; Anders Karlén; John A. Robinson; Uppsala universitet; []
   Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Organic chemistry; β-hairpin; peptidomimetics; Sonogashira; NMR; photochemistry; microwave; peptide; palladium; Organisk kemi; Organic chemistry; Organisk kemi;

   Sammanfattning : Peptide secondary structure mimetics are important tools in medicinal chemistry, as they provide analogues of endogeneous peptides with new physicochemical and pharmacological properties. The β-hairpin motif has been shown to be involved in numerous physiological processes, among others in regulation of eucariotic gene transcription. LÄS MER

7. 5. 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