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Projects / Programmes source: ARIS

Characterization of ligand-receptor interactions

Research activity

Code Science Field Subfield
1.09.00  Natural sciences and mathematics  Pharmacy   

Code Science Field
B000  Biomedical sciences   
P000  Natural sciences and mathematics   
Keywords
non-covalent interactions, NMR spectroscopy, laser tweezers, screening, fragment-based design
Evaluation (rules)
source: COBISS
Researchers (5)
no. Code Name and surname Research area Role Period No. of publicationsNo. of publications
1.  25434  PhD Urban Bren  Chemistry  Researcher  2008 - 2009  359 
2.  29497  PhD Nikola Minovski  Pharmacy  Junior researcher  2008 - 2011  115 
3.  19576  PhD Gregor Mlinšek  Cardiovascular system  Researcher  2008 - 2009  170 
4.  25493  PhD Andrej Perdih  Pharmacy  Researcher  2008 - 2010  262 
5.  01661  PhD Tomaž Šolmajer  Chemistry  Head  2008 - 2011  380 
Organisations (1)
no. Code Research organisation City Registration number No. of publicationsNo. of publications
1.  0104  National Institute of Chemistry  Ljubljana  5051592000  21,489 
Abstract
Experimental methodology for investigation of ligand-receptor interactions based on high-resolution nuclear magnetic resonance (NMR) and molecular force spectroscopy will be implemented and developed. In particular generally appearing problems of large molecular weight of the protein target and low solubility of ligands in aqueous solution will be considered. Development of experimental methodology will be focused on determination of experimental parameters, which allow identification of ligand binding to protein targets and quantitative determination of non-covalent interactions in formation of ligand-receptor complexes. Precise identification of ligand binding is crucial for effective screening approaches. Knowledge of nature and energetics of non-covalent interactions between the ligand and receptor functional groups offers essential information for rational drug design and improvement of theoretical algorithms for investigation of drug-receptor complexes.
Significance for science
New molecular targets and development of novel antibiotics directed at these targets are a challenge for a scientist in the field of biomedicine on one hand and on the other hand a pressing need of medicine for introduction of novel drugs into therapy because of unmet medical needs and fast development of bacterial resistance towards current antimicrobial drugs. The contribution to the development of science will be validation and characterization of DNA gyrase as molecular target for the development of novel antimicrobials and importance of this targets in pathology of various bacterial infections. The most important result will be the discovery of novel antibiotics and enzyme inhibitors and knowledge about their mode of action. Also, important new knowledge will result from experimental determination of structure of the ligand –enzyme complex which will enable insight into underlying molecular mechanisms. The results of our work will be published in highly ranked journals and we will report on our research at international conferences.
Significance for the country
The research activity directed towards development of a novel chemical entity to the end of preclinical research has been completed successfully in this laboratory for biological systems in which various enzymatic targets and chemical classes of inhibitor molecules were studied. There is also a continuously growing interest of the world pharmaceutical industry to promote an intense collaboration with innovative groups in academia. Such collaboration is the basis for formation of high-tech biotechnological companies what has been a priority for the Slovenian economic development of the 21st century. Functional knowledge obtained and developed by young researchers of the project team will be a foundation on which these high-tech biotechnological companies can be organized. The resulting products which can be commercialized are an important contribution towards the economic exploitation of existing infrastructure of academic research institutions. Novel knowledge obtained by this project will contribute to further development of the field of pharmacy, biotechnology and biomedicine in Slovenia.
Most important scientific results Annual report 2008, 2009, final report, complete report on dLib.si
Most important socioeconomically and culturally relevant results Annual report 2008, 2009, final report, complete report on dLib.si
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