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Information × 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. popup.stage_title Head Tukalo Mykhaylo, Доктор біологічних наук Registration Date 17-12-2012 Organization Institute of Molecular Biology and Genetics of NASU popup.description2 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 popup.authors 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 popup.nrat_date 2020-04-02 Close