Filters
cris logo
-
New search Filters
Select from list
Displayed from Show more
You have reached the maximum number of displayed search results.
All results displayed
No results are available for the search performed
Displayed from
You have reached the maximum number of displayed search results.
All results displayed
Loading results
Obtaining statistical data

Projects / Programmes source: ARIS

Optimization of gyrase inhibitors

Edit
Research activity

Code Science Field Subfield
4.06.00  Biotechnical sciences  Biotechnology   

Code Science Field
T490  Technological sciences  Biotechnology 
B740  Biomedical sciences  Pharmacological sciences, pharmacognosy, pharmacy, toxicology 
B510  Biomedical sciences  Infections 
B120  Biomedical sciences  Molecular biophysics 
B110  Biomedical sciences  Bioinformatics, medical informatics, biomathematics biometrics 
Keywords
antimicrobial drugs, recombinant protein, molecular modeling, DNA gyrase, NMR spectrscopy, microbial biotechnology
Evaluation (rules)
source: COBISS
Evaluation of bibliographic research performance indicators according to ARIS methodology
Citations Citations for bibliographic records in COBIB.SI that are linked to records in citation databases
source: WoS source: Scopus source: COBISS
Researchers (7)
no. Code Name and surname Research area Role Period No. of publications
1.  18675  Robert Bremšak    Researcher  2002 - 2004  0 
2.  07960  MSc Mihael Florjanič  Pharmacy  Researcher  2002 - 2004  0 
3.  17917  PhD Andreja Majerle  Biotechnology  Researcher  2002 - 2004  0 
4.  20159  PhD Marko Oblak  Pharmacy  Researcher  2002 - 2004  0 
5.  07084  PhD Andreja Plaper  Pharmacy  Researcher  2002 - 2004  0 
6.  12060  PhD Primož Pristovšek  Chemistry  Head  2002 - 2004  0 
7.  15768  Miloš Ružič  Pharmacy  Researcher  2002 - 2004  0 
Organisations (2)
no. Code Research organisation City Registration number No. of publications
1.  0104  National Institute of Chemistry  Ljubljana  5051592000  10 
2.  0259  Krka, tovarna zdravil, d.d., Novo mesto (Slovene)  Novo mesto  5043611  0 
Abstract
Increasing bacterial resistance to conventional antibiotics requires development of novel antimicrobial substances. Knowledge of tertiary structures of bacterial proteins - potential drug targets and libraries of organic compounds nowadays enable targeted development of novel antimicrobials. Within the scope of this project we propose to develop novel specific inhibitors of bacterial gyrases. Design of novel compounds will be designed based on molecular modeling and screening results of a number of organic compounds with NMR methods (similar to "SAR by NMR" approach) in the presence of isotopically labeled recombinant gyrase fragment, where compounds with low to moderate affinity to the active site of gyrase are identified and are later combined into novel compounds with increased potency. Assignment of bacterial gyrase B fragment, prepared in the preceding project will be used for analysis of NMR measurements, while inhibition will be tested also with other spectroscopic and biochemical methods. For the purpose of testing specificity of compounds a recombinant human topoisomerase II will be expressed in yeast and purified. Based on molecular modeling of docking into the gyrase with modeling of the corresponding domain of human topo II and organic synthesis we will prepare novel, more selective compounds and test them for their inhibitory activity both in vitro in the enzymatic assay as well as in vivo on microorganisms
Confirmation required
Views history
Favourite