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Projects / Programmes source: ARIS

Mimetics of biologically active peptides: Strategies of design and synthesis

Research activity

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 
Keywords
peptidomimetics, peptidomimetics design, synthesis of peptidomimetics, selective inhibitors of thrombin, fibrinogen receptor antagonists, RGD peptides, mimetics of ionogenic amino acids, arginine mimetics, peptidomimetic scaffolds
Evaluation (rules)
source: COBISS
Researchers (12)
no. Code Name and surname Research area Role Period No. of publicationsNo. of publications
1.  08329  PhD Simona Golič Grdadolnik  Chemistry  Researcher  1997 - 1999  298 
2.  01463  PhD Danijel Kikelj  Pharmacy  Head  1999  565 
3.  00839  PhD Aleš Krbavčič  Pharmacy  Researcher  1999  344 
4.  17436  Marija Krbavčič    Researcher  1999 
5.  10005  PhD Gašper Marc  Pharmacy  Researcher  1998 - 1999  36 
6.  17437  Marjeta Mulej    Researcher  1999 
7.  10691  PhD Joško Osredkar  Human reproduction  Researcher  1997 - 1999  1,305 
8.  08519  PhD Marija Sollner Dolenc  Pharmacy  Researcher  1999  651 
9.  01661  PhD Tomaž Šolmajer  Chemistry  Researcher  1997 - 1999  380 
10.  00830  PhD Anton Štalc  Biotechnology  Researcher  1997 - 1999  158 
11.  01878  PhD Uroš Urleb  Pharmacy  Researcher  1997 - 1999  379 
12.  17438  Damijana Zalar    Researcher  1999 
Organisations (3)
no. Code Research organisation City Registration number No. of publicationsNo. of publications
1.  0104  National Institute of Chemistry  Ljubljana  5051592000  21,489 
2.  0258  Lek Pharmaceutical Company d.d.  Ljubljana  1732811  8,400 
3.  0787  University of Ljubljana, Faculty of Pharmacy  Ljubljana  1626973  17,522 
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.
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