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Thiopeptides: antibiotics with unique chemical structures and diverse biological activities

Abstract

Thiopeptides are a class of natural product antibiotics with diverse structures and functions. Their complex structures and biosynthesis have intrigued researchers since their discovery in 1948, but not a single thiopeptide has been approved for human use. This is mainly due to their poor solubility, challenging synthesis, and low bioavailability. This review summarizes the current research on the biosynthesis and biological activity of thiopeptide antibiotics since 2015. The focus of research since 2015 has been on uncovering biosynthetic routes, developing methods for total synthesis, and understanding the biological activity of thiopeptides. Overall, there is still much to learn about this family of molecules.

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Acknowledgements

We thank Christy Groves for assistance with the figures. Work on thiopeptides in the Burrows lab is funded by grants from the Natural Sciences and Engineering Research Council of Canada (NSERC) (RGPIN-2016-06521) and the Ontario Research Fund (RE07-048). DCKC was funded by an NSERC Canadian Graduate Scholarship—Master’s award and holds an Ontario Graduate Scholarship.

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Chan, D.C.K., Burrows, L.L. Thiopeptides: antibiotics with unique chemical structures and diverse biological activities. J Antibiot 74, 161–175 (2021). https://doi.org/10.1038/s41429-020-00387-x

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