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Information × Registration Number 0220U104726, 0120U000079 , R & D reports Title Multitarget drug discovery against Staphylococcus aureus and development of fluorescent assay to evaluate antibiofilm activity for identified antibacterial agents popup.stage_title Head Volynets Halyna P., Кандидат біологічних наук Registration Date 26-12-2020 Organization Institute of Molecular Biology and Genetics of NAS of Ukraine popup.description2 During the Project realization, the gene of Staphylococcus aureus threonyl-tRNA synthetase was cloned and the conditions for expression of the soluble form of this enzyme in E. coli strains were selected. Recombinant S. aureus threonyl-tRNA synthetase and seryl-tRNA synthetase were obtained in preparative amounts. Molecular docking of a collection containing 124830 ligands was performed and 128 compounds were selected for testing of their inhibitory activity toward S. aureus threonyl-tRNA synthetase and seryl-tRNA synthetase using aminoacylation assay. According to compound screening results at a concentration of 100 µM, 22 compounds inhibiting S. aureus threonyl-tRNA synthetase by 30-55% and 4 compounds that inhibit S. aureus seryl-tRNA synthetase were identified. It was found that only two compounds inhibit both enzymes simultaneously. It was revealed that compound 2-[1-(4-methoxy-phenyl)-2-nitro-ethylsulfanyl]-phenylamine, which possesses dual-target inhibitory activity toward S. aureus threonyl-tRNA synthetase and seryl-tRNA synthetase inhibits growth of methicillin-resistant S. aureus strain ATCC43300 by 89% at the concentration of 32 mg/l. Three fluorescent dyes – Dye 21, Dye 23 and Dye 16, for visualization of the amyloid component of S. aureus 25923 biofilm have been developed. Product Description popup.authors popup.nrat_date 2020-12-26 Close