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Information × Registration Number 0212U004598, 0110U004647 , R & D reports Title Rational search for inhibitors of aminoacyl-tRNA synthetaes with selective action against causative agent of tuberculosis popup.stage_title Head Tukalo Mykhaylo, Доктор біологічних наук Registration Date 20-01-2012 Organization Institute of Molecular Biology and Genetics of NASU popup.description2 The 3D structural model of M. tuberculosis LeuRS (LeuRSMt) has been build by using homology modelling. As the structural matrix X-ray investigated T. thermophilus LeuRS was used. Stucture of LeuRSMt and selected chemical compounds from the library were prepared for virtual screening. Basing on the results of virtual screening of 34000 compounds, 200 most perspective was selected and biochemical testing by two independent methods was carried out in vitro. In this testing seven compounds (components NN 14, 151, 152, 155, 181, 182 and 199) were identified as the most active LeuRSMt inhibitors (IC50 2,5 to 11,0 mcМ). These compounds will becomes the base for construct a new antitubercular drugs which will be not toxic for the human. For biological testing the target-specific E. coli tester strains has been engineered, and started direct identification of chemical components with pharmacological potential and anti-tubercular activity that are inactive against human LeuRS. Product Description popup.authors Бджола Володимир Григорович Бояршин Костянтин Сергійович Голуб А ндрій Григорович Гудзера Ольга Йосипівнв Кpикливий Iван Андрійович Коваленко Оксана Петрівна Яремчук Ганна Дмитрівна Ярмолюк Сергій Миколайович popup.nrat_date 2020-04-02 Close