Projects / Programmes
Mimetics of biologically active peptides: Strategies of design and synthesis
Code |
Science |
Field |
Subfield |
1.09.00 |
Natural sciences and mathematics |
Pharmacy |
|
Code |
Science |
Field |
B740 |
Biomedical sciences |
Pharmacological sciences, pharmacognosy, pharmacy, toxicology |
P310 |
Natural sciences and mathematics |
Proteins, enzymology |
peptidomimetics, peptidomimetics design, synthesis of peptidomimetics, selective inhibitors of thrombin, fibrinogen receptor antagonists, RGD peptides, mimetics of ionogenic amino acids, arginine mimetics, peptidomimetic scaffolds
Researchers (12)
Organisations (3)
Abstract
The aim of this projest is design and synthesis of mimetics of amino acid sequences comprising two to four amino acid residues with high proportion of ionogenic amino acids, i.e. arginine, lysine, aspartic acid or glutamic acid in which one of the remaining non-ionogenic acids is preferably proline (e.g. Arg-Gly-Asp, Lys-Pro-Arg, Lys-Pro-Arg-Arg, Arg-Pro-Lys, Lys-Pro-Arg, Arg-Lys-Asp, Pro-Arg etc.). These motifs in amino acids sequences are crucial for binding of several biologically important small peptides e.g. tuftsin, thymopentin, RGD peptides, thrombin active site inhibitors, bradykinin, neurotensin and substance P to their respective receptors. The mimetics resulting from this project will comprise a scaffold bearing several properly positioned ionogenic groups and will be biologically evaluated as such or will be used as templates for construction of peptidomimetics on the basis of the aforementioned and more complex peptides. The concept of mimicking more than one neighboring ionogenic amino acids with a single template which can be additionally combined with other moieties to afford a peptidomimetic represents a new approach to peptidomimetics design. It is expected that application of this novel concept in peptidomimetics research may lead to new ligands for integrins and new thrombin active site inhibitors with antithrombotic activity.