Registration Number
0212U008469,
0110U006120
, R & D reports
Title
Development for technology target-specific search of aminoacyl-tRNA synthetases inhibitors with selective action against specific human infections.
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Head
Tukalo Mykhaylo, Доктор біологічних наук
Registration Date
17-12-2012
Organization
Institute of Molecular Biology and Genetics of NASU
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LeuRSMT overproducer has been constructed by transforming pET 28a plasmid, which contains the gene of leucyl-tRNA synthetase from M. tuberculosis, to E. coli Rosetta (DE3) cells. The method of isolation and purification of recombinant LeyRSMT has been developed. The recombinant leucyl-tRNA synthetase M. tuberculosis with purity of over 95% has been obtained in amount of 60 mg. Using two independent methods (ATP-pyrophosphate exchange and aminoacylation of tRNA) for in vitro assay the effect of 200 most promising compounds, selected with the receptor-based virtual screening, on enzymatic activities of LeuRSMT was studied. Three compounds N 151, 152 and 199 have shown most significant inhibition effect on activity of M. tuberculosis leucyl-tRNA synthetase. These compounds will form the basis for further structural optimization using molecular dynamics and X-Ray crystallography techniques. The target-specific testing strains of E.coli, which should allow to perform direct identification of chemical compounds with potential antimicrobial properties and inactive to human leucyl- tRNA synthetase have been constructed.5481
Product Description
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Бджола Володимир Григорович
Бояршин Костянтин Сергійович
Волинець Галина Петрівна
Гудзера Ольга Йосипівна
Дудченко Тарас Миколайович
Кpикливий Iван Андрійович
Коваленко Оксана Петрівна
Яpемчук Ганна Дмитрівна
Ярмолюк Сергій Миколайович
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2020-04-02
