University of Pavia, Department of Genetics and Microbiology, Via Ferrata 1, 27100 Pavia, Italy.
Antimicrob Agents Chemother. 2010 Apr;54(4):1616-8. doi: 10.1128/AAC.01676-09. Epub 2010 Jan 19.
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.
新型抗结核候选药物 2-[2-S-甲基-1,4-二恶烷-8-氮杂螺[4.5]癸-8-基]-8-硝基-6-(三氟甲基)-4H-1,3-苯并噻嗪-4-酮（BTZ043）靶向酶去烯丙基磷酸-β-D-核糖 2'-差向异构酶的 DprE1（Rv3790）亚基。为了监测苯并噻嗪酮（BTZ）耐药性的潜在发展，对来自四家欧洲医院的 240 株敏感和多药耐药结核分枝杆菌临床分离株进行了 dprE1 基因突变检测和 BTZ 敏感性检测。所有 240 株菌株均敏感，从而在 BTZ043 临床试验之前建立了基线。
