Sökning: "bioactive conformation"

Visar resultat 1 - 5 av 16 avhandlingar innehållade orden bioactive conformation.

  1. 1. The solution conformations of macrocycles. Applications in the exploration of weak interactions and in drug development

    Författare :Emma Danelius; Göteborgs universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Macrocycles; cyclic peptides; NMR; solution conformational analysis; NAMFIS; β-hairpin; weak interactions; halogen bonding; protein-protein interaction; bioactive conformation; macrolides; cell permeable conformation.;

    Sammanfattning : Understanding the solution conformation and dynamics of molecules with biological relevance, as well as the impact of their conformation stabilizing weak interactions, is for example important for drug design. Macrocycles have attractive pharmaceutical properties, and are of special interest as drug leads for targets with large, flat and featureless binding sites like protein-protein interfaces. LÄS MER

  3. 2. Synthesis of Aldehyde-Functionalized Building Blocks and Their Use for the Cyclization of Peptides : Applications to Angiotensin II

    Författare :Petra Johannesson; Rob M. J. Liskamp; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmaceutical chemistry; Synthesis; Aldehyde; Cyclization; Peptide; Angiotensin II; Ang II; Bioactive Conformation; Solid Phase Peptide Synthesis; Dimethyl Acetal; Farmaceutisk kemi; Syntes; Aldehyd; Cyklisering; Peptid; Bioaktiv konformation; Fast-fas peptidsyntes; Dimetylacetal; 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 with retained biological activities at peptide receptors. Angiotensin II (Asp-Arg-Val-Tyr-Ile-His-Pro-Phe, Ang II) was used as a model peptide. LÄS MER

  4. 3. 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

  5. 4. 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

  7. 5. 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