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Issue 2, 2015
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Target-oriented design and biosynthesis of thiostrepton-derived thiopeptide antibiotics with improved pharmaceutical properties

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Abstract

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.

Graphical abstract: Target-oriented design and biosynthesis of thiostrepton-derived thiopeptide antibiotics with improved pharmaceutical properties

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Publication details

The article was received on 03 Nov 2014, accepted on 05 Dec 2014 and first published on 05 Dec 2014


Article type: Research Article
DOI: 10.1039/C4QO00288A
Citation: Org. Chem. Front., 2015,2, 106-109
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    Target-oriented design and biosynthesis of thiostrepton-derived thiopeptide antibiotics with improved pharmaceutical properties

    S. Wang, Q. Zheng, J. Wang, Z. Zhao, Q. Li, Y. Yu, R. Wang and W. Liu, Org. Chem. Front., 2015, 2, 106
    DOI: 10.1039/C4QO00288A

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