Differential inhibition of Staphylococcus aureus PBP2 by glycopeptide antibiotics
Differential inhibition of Staphylococcus aureus PBP2 by glycopeptide antibiotics
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DOI：
10.1021/ja043849e
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发表时间：
2005-03-16
影响因子：
15
通讯作者：
Kahne, D
中科院分区：
文献类型：
--
作者：
Leimkuhler, C;Chen, L;Kahne, D
The glycopeptide antibiotics prevent maturation of the bacterial cell wall by binding to the terminald-alanyl-d-alanine moiety of peptidoglycan precursors, thereby inhibiting the enzymes involved in the final stages of peptidoglycan synthesis. However, there are significant differences in the biological activity of particular glycopeptide derivatives that are not related to their affinity ford-Ala-d-Ala. We compare the ability of vancomycin and a set of clinically relevant glycopeptides to inhibitStaphylococcus aureusPBP2 (penicillin binding protein), the major transglycosylase in a clinically relevant pathogen,S.aureus. We report experiments suggesting that activity differences between glycopeptides against this organism reflect a combination of substrate binding and secondary interactions with key enzymes involved in peptidoglycan synthesis.
