Discovery Sciences, Innovative Medicines and Early Development Biotech Unit, AstraZeneca R&D Gothenburg, Gothenburg, Sweden.
Department of Chemistry and Molecular Biology, University of Gothenburg, Gothenburg, Sweden.
Nat Chem Biol. 2017 Mar;13(3):265-267. doi: 10.1038/nchembio.2270. Epub 2017 Jan 9.
The rapid increase of antibiotic resistance has created an urgent need to develop novel antimicrobial agents. Here we describe the crystal structure of the promising bacterial target phospho-N-acetylmuramoyl-pentapeptide translocase (MraY) in complex with the nucleoside antibiotic tunicamycin. The structure not only reveals the mode of action of several related natural-product antibiotics but also gives an indication on the binding mode of the MraY UDP-MurNAc-pentapeptide and undecaprenyl-phosphate substrates.
抗生素耐药性的迅速增加，催生了对新型抗菌药物的迫切需求。在此，我们描述了具有广阔前景的细菌靶标磷酸-N-乙酰胞壁酰五肽转位酶（MraY）与核苷抗生素乌苯苷结合的复合物晶体结构。该结构不仅揭示了几种相关天然产物抗生素的作用模式，还提示了 MraY UDPMurNAc-五肽和十一异戊烯基焦磷酸底物的结合模式。
