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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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Article information


Submitted
03 Nov 2014
Accepted
05 Dec 2014
First published
05 Dec 2014

Org. Chem. Front., 2015,2, 106-109
Article type
Research Article
Author version available

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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