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噻唑肽类抗生素:具有独特化学结构和多样化生物活性的抗生素。

Thiopeptides: antibiotics with unique chemical structures and diverse biological activities.

机构信息

Department of Biochemistry and Biomedical Sciences, McMaster University, Hamilton, ON, Canada.

Michael G. DeGroote Institute for Infectious Diseases Research, McMaster University, Hamilton, ON, Canada.

出版信息

J Antibiot (Tokyo). 2021 Mar;74(3):161-175. doi: 10.1038/s41429-020-00387-x. Epub 2020 Dec 21.

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.

摘要

噻唑肽类抗生素是一类具有多种结构和功能的天然产物抗生素。自 1948 年发现以来,其复杂的结构和生物合成一直吸引着研究人员的兴趣,但没有一种噻唑肽类抗生素被批准用于人体。这主要是由于它们的溶解度差、合成具有挑战性和生物利用度低。本综述总结了 2015 年以来噻唑肽类抗生素生物合成和生物活性的研究进展。2015 年以来的研究重点是揭示生物合成途径、开发全合成方法以及了解噻唑肽类抗生素的生物活性。总的来说,对于这类分子还有很多需要了解的地方。

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