The future for early-stage tuberculosis drug discovery.
The future for early-stage tuberculosis drug discovery.
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DOI：
10.2217/fmb.14.125
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发表时间：
2015
影响因子：
3.1
通讯作者：
Parish T
中科院分区：
文献类型：
--
作者：
Zuniga ES;Early J;Parish T
由于治疗方案漫长而复杂，以及日益严重的耐药问题，迫切需要新的、更好的药物来治疗结核病。过去几年，药物发现工作有所增加，更加关注现代高通量筛选技术。基于靶标的方法与药物鉴定的传统经验方法的结合，得到了最近才通过更新的遗传工具实现的基于靶标的表型筛选的使用的补充。使用这些方法，已经发现了许多有前途的化合物系列。然而，将它们开发成药物仍存在重大问题。本综述重点介绍了结核病药物发现的最新进展，包括筛查活动概述、经验教训和未来方向。
There is an urgent need for new and better drugs to treat tuberculosis due to lengthy and complex treatment regimens and a rising problem of drug resistance. Drug discovery efforts have increased over the past few years, with a larger focus on modern high-throughput screening technologies. A combination of target-based approaches, with the traditional empirical means of drug identification, has been complemented by the use of target-based phenotypic screens only recently made possibly with newer genetic tools. Using these approaches, a number of promising compound series have been discovered. However, significant problems remain in developing these into drugs. This review highlights recent advances in TB drug discovery, including an overview of screening campaigns, lessons learned and future directions.