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脂质II作为抗生素的作用靶点。

Lipid II as a target for antibiotics.

作者信息

Breukink Eefjan, de Kruijff Ben

机构信息

Department of Biochemistry of Membranes, Bijvoet Center for Biomolecular Research, Utrecht University, The Netherlands.

出版信息

Nat Rev Drug Discov. 2006 Apr;5(4):321-32. doi: 10.1038/nrd2004.

Abstract

Lipid II is a membrane-anchored cell-wall precursor that is essential for bacterial cell-wall biosynthesis. The effectiveness of targeting Lipid II as an antibacterial strategy is highlighted by the fact that it is the target for at least four different classes of antibiotic, including the clinically important glycopeptide antibiotic vancomycin. However, the growing problem of bacterial resistance to many current drugs, including vancomycin, has led to increasing interest in the therapeutic potential of other classes of compound that target Lipid II. Here, we review progress in understanding of the antibacterial activities of these compounds, which include lantibiotics, mannopeptimycins and ramoplanin, and consider factors that will be important in exploiting their potential as new treatments for bacterial infections.

摘要

脂联素II是一种膜锚定的细胞壁前体,对细菌细胞壁生物合成至关重要。将脂联素II作为抗菌策略的有效性体现在它是至少四类不同抗生素的靶点,包括临床上重要的糖肽类抗生素万古霉素。然而,细菌对包括万古霉素在内的许多现有药物的耐药性问题日益严重,这使得人们对其他靶向脂联素II的化合物的治疗潜力越来越感兴趣。在这里,我们综述了对这些化合物抗菌活性的理解进展,这些化合物包括羊毛硫抗生素、甘露糖肽霉素和瑞莫拉宁,并考虑了在开发其作为细菌感染新疗法的潜力方面将很重要的因素。

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