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. 2010 Apr;54(4):1616-8.
doi: 10.1128/AAC.01676-09. Epub 2010 Jan 19.

Clinical isolates of Mycobacterium tuberculosis in four European hospitals are uniformly susceptible to benzothiazinones

Maria Rosalia Pasca  1 , Giulia Degiacomi, Ana Luisa de Jesus Lopes Ribeiro, Francesca Zara, Patrizia De Mori, Beate Heym, Maurizio Mirrione, Roberto Brerra, Laura Pagani, Leopoldo Pucillo, Panajota Troupioti, Vadim Makarov, Stewart T Cole, Giovanna Riccardi
Affiliations

Clinical isolates of Mycobacterium tuberculosis in four European hospitals are uniformly susceptible to benzothiazinones

Maria Rosalia Pasca et al. Antimicrob Agents Chemother. 2010 Apr.

Abstract

The new antitubercular drug candidate 2-[2-S-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one (BTZ043) targets the DprE1 (Rv3790) subunit of the enzyme decaprenylphosphoryl-beta-d-ribose 2'-epimerase. To monitor the potential development of benzothiazinone (BTZ) resistance, a total of 240 sensitive and multidrug-resistant Mycobacterium tuberculosis clinical isolates from four European hospitals were surveyed for the presence of mutations in the dprE1 gene and for BTZ susceptibility. All 240 strains were susceptible, thus establishing the baseline prior to the introduction of BTZ043 in clinical trials.

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References

    1. Andersson, D. I.2006. The biological cost of mutational antibiotic resistance: any practical conclusions? Curr. Opin. Microbiol. 9:461-465. - PubMed
    1. Christophe, T., M. Jackson, H. K. Jeon, D. Fenistein, M. Contreras-Dominguez, J. Kim, A. Genovesio, J. P. Carralot, F. Ewann, E. H. Kim, S. Y. Lee, S. Kang, M. J. Seo, E. J. Park, H. Škovierová, H. Pham, G. Riccardi, J. Nam, L. Marsollier, M. Kempf, M. L. Joly-Guillou, T. Oh, W. K. Shin, Z. No, U. Nehrbass, R. Brosch, S. T. Cole, and P. Brodin.2009. High content screening identifies decaprenyl-phosphoribose 2′ epimerase as a target for intracellular antimycobacterial inhibitors. PLoS Pathog. 5:e1000645. - PMC - PubMed
    1. Makarov, V., G. Manina, K. Mikusova, U. Möllmann, O. Ryabova, B. Saint-Joanis, N. Dhar, M. R. Pasca, S. Buroni, A. P. Lucarelli, A. Milano, E. De Rossi, M. Belanova, A. Bobovska, P. Dianiskova, J. Kordulakova, C. Sala, E. Fullam, P. Schneider, J. D. McKinney, P. Brodin, T. Christophe, S. Waddell, P. Butcher, J. Albrethsen, I. Rosenkrands, R. Brosch, V. Nandi, S. Bharath, S. Gaonkar, R. K. Shandil, V. Balasubramanian, T. Balganesh, S. Tyagi, J. Grosset, G. Riccardi, and S. T. Cole.2009. Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis. Science 324:801-804. - PMC - PubMed
    1. Riccardi, G., M. R. Pasca, and S. Buroni.2009. Mycobacterium tuberculosis: drug resistance and future perspectives. Future Microbiol. 4:597-614. - PubMed
    1. Sassetti, C. M., D. H. Boyd, and E. J. Rubin.2003. Genes required for mycobacterial growth defined by high density mutagenesis. Mol. Microbiol. 48:77-84. - PubMed

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