Negri Ana, Javidnia Prisca, Mu Ran, Zhang Xiaojie, Vendome Jeremie, Gold Ben, Roberts Julia, Barman Dipti, Ioerger Thomas, Sacchettini James C, Jiang Xiuju, Burns-Huang Kristin, Warrier Thulasi, Ling Yan, Warren J David, Oren Deena A, Beuming Thijs, Wang Hongyao, Wu Jie, Li Haitao, Rhee Kyu Y, Nathan Carl F, Liu Gang, Somersan-Karakaya Selin
Schrödinger, Inc. , 120 West 45th Street , New York , New York 10036 , United States.
Department of Medicine, Division of Infectious Diseases , Weill Cornell Medical College , 1300 York Avenue , New York , New York 10065 , United States.
ACS Infect Dis. 2018 May 11;4(5):771-787. doi: 10.1021/acsinfecdis.7b00111. Epub 2018 Feb 21.
The success of Mycobacterium tuberculosis (Mtb) as a pathogen depends on the redundant and complex mechanisms it has evolved for resisting nitrosative and oxidative stresses inflicted by host immunity. Improving our understanding of these defense pathways can reveal vulnerable points in Mtb pathogenesis. In this study, we combined genetic, structural, computational, biochemical, and biophysical approaches to identify a novel enzyme class represented by Rv2466c. We show that Rv2466c is a mycothiol-dependent nitroreductase of Mtb and can reduce the nitro group of a novel mycobactericidal compound using mycothiol as a cofactor. In addition to its function as a nitroreductase, Rv2466c confers partial protection to menadione stress.
结核分枝杆菌(Mtb)作为一种病原体的成功取决于其为抵抗宿主免疫施加的亚硝化和氧化应激而进化出的冗余且复杂的机制。增进我们对这些防御途径的理解可以揭示Mtb发病机制中的薄弱环节。在本研究中,我们结合了遗传学、结构学、计算学、生物化学和生物物理学方法,以鉴定一种以Rv2466c为代表的新型酶类。我们表明,Rv2466c是Mtb的一种依赖于分枝硫醇的硝基还原酶,并且可以使用分枝硫醇作为辅因子来还原一种新型杀分枝杆菌化合物的硝基。除了作为硝基还原酶的功能外,Rv2466c还赋予对甲萘醌应激的部分保护作用。