Target-Oriented Design and Biosynthesis of Thiostrepton-Derived Thiopeptide Antibiotics with Improved Pharmaceutical Properties
Target-Oriented Design and Biosynthesis of Thiostrepton-Derived Thiopeptide Antibiotics with Improved Pharmaceutical Properties
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具有改进药物特性的硫链丝菌素衍生硫肽抗生素的靶向设计和生物合成
DOI：
10.1039/c4qo00288a
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发表时间：
2015
影响因子：
5.4
通讯作者：
Wen Liu
中科院分区：
文献类型：
--
作者：
Shoufeng Wang;Qingfei Zheng;Jianfeng Wang;Zhixiong Zhao;Qingye Li;Yunsong Yu;Renxiao Wang;Wen Liu
Thiostrepton is a potent archetypal thiopeptide antibiotic. According to its mechanism known to target bacterial ribosome, we show here a rational design upon modeling of this molecule into the ribosome complex and an effective biosynthesis of new thiopeptide antibiotics through regioselective modifications. The resulting derivatives exhibit a series of anticipated and unanticipated pharmaceutical advantages, including improvement in activity against a number of drug-resistant pathogens and in water solubility that has largely affected the clinical use of thiostrepton.
