Department of Biology and Biotechnology "Lazzaro Spallanzani", University of Pavia, via Ferrata 1, 27100, Pavia, Italy,
Appl Microbiol Biotechnol. 2013 Oct;97(20):8841-8. doi: 10.1007/s00253-013-5218-x. Epub 2013 Sep 14.
The re-emergence of tuberculosis in recent years led the World Health Organization (WHO) to launch the Stop TB Strategy program. Beside repurposing the existing drugs and exploring novel molecular combinations, an essential step to face the burden of tuberculosis will be to develop new drugs by identifying vulnerable bacterial targets. Recent studies have focused on decaprenylphosphoryl-D-ribose oxidase (DprE1) of Mycobacterium tuberculosis, an essential enzyme involved in cell wall metabolism, for which new promising molecules have proved efficacy as antitubercular agents. This review summarizes the state of the art concerning DprE1 in terms of structure, enzymatic activity and inhibitors. This enzyme is emerging as one of the most vulnerable target in M. tuberculosis.
近年来，结核病的再次出现促使世界卫生组织（WHO）启动了“遏制结核病战略”计划。除了重新利用现有药物和探索新的分子组合外，通过确定易受攻击的细菌靶标来开发新药，将是应对结核病负担的重要步骤。最近的研究集中在分枝杆菌中的脱磷酸-D-核糖基磷酸烯醇丙酮酸氧化酶（DprE1）上，这是一种参与细胞壁代谢的必需酶，新的有前途的分子已被证明具有抗结核作用。本文综述了 DprE1 的结构、酶活性和抑制剂方面的最新进展。该酶正成为结核分枝杆菌中最脆弱的靶标之一。
