Delcour Anne H
Department of Biology, University of Houston, 369 Science and Research Building II, Houston, TX 77204-5001, USA.
Biochim Biophys Acta. 2009 May;1794(5):808-16. doi: 10.1016/j.bbapap.2008.11.005. Epub 2008 Nov 27.
To date most antibiotics are targeted at intracellular processes, and must be able to penetrate the bacterial cell envelope. In particular, the outer membrane of gram-negative bacteria provides a formidable barrier that must be overcome. There are essentially two pathways that antibiotics can take through the outer membrane: a lipid-mediated pathway for hydrophobic antibiotics, and general diffusion porins for hydrophilic antibiotics. The lipid and protein compositions of the outer membrane have a strong impact on the sensitivity of bacteria to many types of antibiotics, and drug resistance involving modifications of these macromolecules is common. This review will describe the molecular mechanisms for permeation of antibiotics through the outer membrane, and the strategies that bacteria have deployed to resist antibiotics by modifications of these pathways.
迄今为止,大多数抗生素作用于细胞内过程,且必须能够穿透细菌细胞壁。特别是革兰氏阴性菌的外膜构成了一个必须克服的巨大屏障。抗生素穿透外膜基本上有两条途径:疏水性抗生素通过脂质介导途径,亲水性抗生素通过一般扩散孔蛋白。外膜的脂质和蛋白质组成对细菌对多种抗生素的敏感性有很大影响,涉及这些大分子修饰的耐药性很常见。本综述将描述抗生素透过外膜的分子机制,以及细菌通过修饰这些途径来抵抗抗生素的策略。