Structural Evidence for Rifampicin Monooxygenase Inactivating Rifampicin by Cleaving Its Ansa-Bridge

Li-Kai Liu; Yumin Dai; Heba Abdelwahab; Pablo Sobrado; John J. Tanner

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Structural Evidence for Rifampicin Monooxygenase Inactivating Rifampicin by Cleaving Its Ansa-Bridge

机译：利福平单氧基酶通过切割其ANSA桥灭活利福平的结构证据

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Rifampicin monooxygenase (RIFMO) decreases the potency of rifampicin (RIF) by converting it to oxidative products. Further decomposition of RIF has been observed in bacteria producing RIFMO and contributes to RIFMO-mediated drug resistance. Here we report the first crystal structure of RIFMO in complex with the hydroxylated RIF product. The 2.10 ? resolution structure reveals a breach of the ansa aliphatic chain of RIF between naphthoquinone C2 and amide N1. Our data suggest that RIFMO catalyzes the hydroxylation of RIF at the C2 atom followed by cleavage of the ansa linkage, which leads to inactivation of the antibiotic by preventing key contacts with the RNA polymerase target.

机译：利福平单氧基酶（RIFMO）通过将其转化为氧化产品来降低利福平（RIF）的效力。在产生RifMo的细菌中观察到RIF的进一步分解，有助于利福莫介导的耐药性。在这里，我们在羟基化的RIF产物中报道了RifMo的第一晶体结构。 2.10？分辨率结构揭示了促进萘醌C2和酰胺N1之间的RIF ANSA脂族链。我们的数据表明，RifMo催化RIF在C2原子的羟基化，然后通过防止与RNA聚合酶靶标的键接触来灭活抗生素。

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来源
《Biochemistry》 |2018年第14期|共4页
作者
Li-Kai Liu; Yumin Dai; Heba Abdelwahab; Pablo Sobrado; John J. Tanner;
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Department of Biochemistry and Department of Chemistry University of Missouri—Columbia Columbia Missouri 65211 United States;

Department of Biochemistry Virginia Tech Blacksburg Virginia 24061 United States;

Department of Biochemistry Virginia Tech Blacksburg Virginia 24061 United States;

Department of Biochemistry Virginia Tech Blacksburg Virginia 24061 United States;

Department of Biochemistry and Department of Chemistry University of Missouri—Columbia Columbia Missouri 65211 United States;

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正文语种 eng
中图分类生物化学;
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1. Structural Evidence for Rifampicin Monooxygenase Inactivating Rifampicin by Cleaving Its Ansa-Bridge [J] . Li-Kai Liu, Yumin Dai, Heba Abdelwahab, Biochemistry . 2018,第14期

机译：利福平单氧基酶通过切割其ANSA桥灭活利福平的结构证据
2. Efficient intracellular delivery of rifampicin to alveolar macrophages using rifampicin-loaded PLGA microspheres: effects of molecular weight and composition of PLGA on release of rifampicin [J] . Kimiko Makino, Takehisa Nakajima, Mitsuhiko Shikamura, Colloids and Surfaces, B. Biointerfaces . 2004,第1期

机译：使用载有利福平的PLGA微球有效地将利福平胞内递送至肺泡巨噬细胞：PLGA的分子量和组成对利福平释放的影响
3. The Sensitization Models of Rabbits to Rifampicin and to two kinds of Rifampicin-Protein Conjugates and the Detection of Rifampicin Specific IgG in these Models [J] . 无中国药学（英文版） . 1994,第002期

机译：兔对利福平和两种利福平-蛋白质结合物的敏化模型以及这些模型中利福平特异性IgG的检测
4. Design of dry powder inhaler formulations containing rifampicin with dextran based on the difference in viscosity in the solution [C] . K. Kadota, Y. Yanagawa, T. Tachikawa, Conference on Process Integration, Modelling and Optimisation for Energy Saving and Pollution Reduction . 2018

机译：基于溶液中粘度差异的葡聚糖用葡聚糖含有利福平的干粉吸入器配方的设计
5. Structural insights into the catalytic mechanism of human topoisomerase I and the crystal structure of the human PXR ligand binding domain with the macrolide rifampicin. [D] . Chrencik, Jill. 2004

机译：对人类拓扑异构酶I催化机制的结构见解以及与大环内酯利福平结合的人PXR配体结合结构域的晶体结构。
6. Could high-concentration rifampicin kill rifampicin-resistant M. tuberculosis? Rifampicin MIC test in rifampicin-resistant isolates from patients with osteoarticular tuberculosis [O] . Zehua Zhang, Fei Dai, Fei Luo, 2014

机译：高浓度的利福平可以杀死耐利福平的结核分枝杆菌吗？利福平对骨关节结核患者耐利福平分离株的MIC试验
7. Could high-concentration rifampicin kill rifampicin-resistant ? Rifampicin MIC test in rifampicin-resistant isolates from patients with osteoarticular tuberculosis [O] . 2014

机译：高浓度的利福平能杀死耐利福平的药吗？利福平对骨关节结核患者耐利福平分离株的MIC试验

Structural Evidence for Rifampicin Monooxygenase Inactivating Rifampicin by Cleaving Its Ansa-Bridge

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