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首页> 外文期刊>Acta crystallographica.Section D. Biological crystallography >Structure of the complex between teicoplanin and a bacterial cell-wall peptide: Use of a carrier-protein approach
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Structure of the complex between teicoplanin and a bacterial cell-wall peptide: Use of a carrier-protein approach

机译：teicoplanin和之间的复杂的结构细菌细胞壁肽:使用载体蛋白的方法

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摘要

Multidrug-resistant bacterial infections are commonly treated with glycopeptide antibiotics such as teicoplanin. This drug inhibits bacterial cell-wall biosynthesis by binding and sequestering a cell-wall precursor: a d-alanine-containing peptide. A carrier-protein strategy was used to crystallize the complex of teicoplanin and its target peptide by fusing the cell-wall peptide to either MBP or ubiquitin via native chemical ligation and subsequently crystallizing the protein-peptide-antibiotic complex. The 2.05? resolution MBP-peptide-teicoplanin structure shows that teicoplanin recognizes its ligand through a combination of five hydrogen bonds and multiple van der Waals interactions. Comparison of this teicoplanin structure with that of unliganded teicoplanin reveals a flexibility in the antibiotic peptide backbone that has significant implications for ligand recognition. Diffraction experiments revealed an X-ray-induced dechlorination of the sixth amino acid of the antibiotic; it is shown that teicoplanin is significantly more radiation-sensitive than other similar antibiotics and that ligand binding increases radiosensitivity. Insights derived from this new teicoplanin structure may contribute to the development of next-generation antibacterials designed to overcome bacterial resistance.
机译：多重抗药性细菌感染通常与糖肽抗生素治疗比如teicoplanin。通过绑定和细胞壁生物合成隔离一个细胞壁前体:d-alanine-containing肽。策略是用于复杂的结晶teicoplanin及其目标肽的融合细胞壁肽MBP或泛素通过本机化学结扎和随后结晶的protein-peptide-antibiotic复杂。MBP-peptide-teicoplanin结构表明,teicoplanin承认其配体通过五个氢键和多个组合范德瓦耳斯相互作用。与unliganded teicoplanin结构teicoplanin揭示的灵活性抗菌肽具有重要的支柱对配体识别的影响。实验显示一个X-ray-induced第六个氨基酸的脱氯抗生素;明显比其他辐射灵敏类似抗生素和配体绑定增加辐射敏感度。这个新的teicoplanin结构可能导致新一代抗菌药物的发展为了克服细菌耐药性。

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