Registration Number
0218U003037,
0115U001404
, R & D reports
Title
Development of the system of fast screening of DNA-binding compounds for the search of inhibitors of nucleic acids biosynthesis enzymes as potential antitumor and antimicrobial agents
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Head
Dubey Igor, Доктор хімічних наук
Registration Date
12-01-2018
Organization
Institute of Molecular Biology and Genetics of NASU
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Biological activity of duplex and quadruplex (G4) DNA ligands found at the previous stage and new compounds was studied in enzymatic test systems in vitro based on topoisomerasde I and telomerase, respectively. Inhibitors of both enzymes were found, including active compounds with IC50 in the range 1.1-1.8 uM. The dependence between the structure of compounds, level of binding tovarious forms of DNA and inhibition efficiency was analyzed. Positive correlation between ligand affinity to duplex and G4-DNA and activity with corresponding enzymes was established.
Product Description
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Ільченко Микола Миколайович
Алексеєва Інна Володимирівна
Дубей Лариса Василівна
Костіна Валентина Григорівна
Криворотенко Дмитро Валентинович
Кузів Ярослав Богданович
Негруцька Валентина Володимирівна
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2020-04-02