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Literature summary extracted from

  • Christophe, T.; Jackson, M.; Hee, K.; Fenistein, D.; Contreras-Dominguez, M.; Kim, J.; Genovesio, A.; Carralot, J.; Ewann, F.; Kim, E.; Lee, S.; Kang, S.; Seo, M.; Eun, J.; Skovierova, H.; Pham, H.; Riccardi, G.; Youn, N.; Marsollier, L.; Kempf, M.; Jol
    High content screening identifies decaprenyl-phosphoribose 2' epimerase as a target for intracellular antimycobacterial inhibitors. (2009), PLoS Pathog., 5, e1000645.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
1.1.1.333 analysis developed of an assay method based on the visualization of mycobacterium replication within host cells and application for the search of compounds that are able to chase the pathogen from its hideout Mycobacterium tuberculosis

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.333 N-(2-(4-methoxyphenoxy)ethyl)-3,5-dinitrobenzamide more than a ten-fold decrease in the number of colony-forming units is observed with both human and mouse primary cells at a N-(2-(4-methoxyphenoxy)ethyl)-3,5-dinitrobenzamide concentrations above 5 microM, compound is also highly active against multidrug-resistant and extensively drug-resistant clinical isolates. N-(2-(4-methoxyphenoxy)ethyl)-3,5-dinitrobenzamide shows a clear-cut effect on the synthesis of the arabinan domains of arabinogalactan and lipoarabinomannan, and inhibition of decaprenyl-phospho-arabinose formation in the treated extracts concurrent with the accumulation of decaprenylphospho-ribose. Target of the inhibitors is probably the heteromeric decaprenylphospho-ribose 29 epimerase encoded by the dprE1/dprE2 genes Mycobacterium tuberculosis
1.1.1.333 N-(2-(benzyloxy)ethyl)-3,5-dinitrobenzamide more than a ten-fold decrease in the number of colony-forming units is observed with both human and mouse primary cells at a N-(2-(benzyloxy)ethyl)-3,5-dinitrobenzamide concentrations above 5 microM, compound is also highly active against multidrug-resistant and extensively drug-resistant clinical isolates. N-(2-(benzyloxy)ethyl)-3,5-dinitrobenzamide shows a clear-cut effect on the synthesis of the arabinan domains of arabinogalactan and lipoarabinomannan, and inhibition of decaprenyl-phospho-arabinose formation in the treated extracts concurrent with the accumulation of decaprenylphospho-ribose. Target of the inhibitors is probably the heteromeric decaprenylphospho-ribose 29 epimerase encoded by the dprE1/dprE2 genes Mycobacterium tuberculosis

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.333 Mycobacterium tuberculosis P9WGS9
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1.1.1.333 Mycobacterium tuberculosis H37Rv P9WGS9
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