Targeting the mycobacterial envelope for tuberculosis drug development.
Targeting the mycobacterial envelope for tuberculosis drug development.
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DOI：
10.1586/eri.12.91
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发表时间：
2012-09
影响因子：
5.7
通讯作者：
Ronning DR
中科院分区：
文献类型：
--
作者：
Favrot L;Ronning DR
引起结核病的细菌，结核分枝杆菌，有一个相当独特的外膜，主要由脂类组成，含有被称为霉菌酸的长链和分支脂肪酸。这些脂质形成一种渗透屏障，阻止许多环境溶质进入，从而使这些细菌抗酸，并能够在极其恶劣的环境中生存。抗结核药物必须穿透这一层才能达到他们的目标。这篇综述强调了药物开发的努力，这些努力增加了缓慢增长的结核病药物流水线，确定了以药物为靶点的新的酶活性，并增加了对分枝杆菌外膜和细胞壁核心组装的重要生物合成途径的了解。此外，这篇综述的一部分着眼于旨在削弱这一屏障的发现努力，以降低分枝杆菌的毒力，降低宿主的适应性，或通过破坏渗透屏障来增强当前药物库的疗效。
The bacterium that causes tuberculosis, Mycobacterium tuberculosis, possesses a rather unique outer membrane composed largely of lipids that possess long-chain and branched fatty acids, called mycolic acids. These lipids form a permeability barrier that prevents entry of many environmental solutes, thereby making these bacteria acid-fast and able to survive extremely hostile surroundings. Antitubercular drugs must penetrate this layer to reach their target. This review highlights drug development efforts that have added to the slowly growing tuberculosis drug pipeline, identified new enzyme activities to target with drugs and increased the understanding of important biosynthetic pathways for mycobacterial outer membrane and cell wall core assembly. In addition, a portion of this review looks at discovery efforts aimed at weakening this barrier to decrease mycobacterial virulence, decrease fitness in the host or enhance the efficacy of the current drug repertoire by disrupting the permeability barrier.
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