Anthraquinone-fused enediynes: discovery, biosynthesis and development

Abstract

Covering: up to the end of July, 2021

Anthraquinone-fused enediynes (AFEs) are a subfamily of enediyne natural products. Dynemicin A (DYN A), the first member of the AFE family, was discovered more than thirty years ago. Subsequently, extensive studies have been reported on the mode of action and the interactions of AFEs with DNA using DYN A as a model. However, progress in the discovery, biosynthesis and clinical development of AFEs has been limited for a long time. In the past five years, four new AFEs have been discovered and significant progress has been made in the biosynthesis of AFEs, especially on the biogenesis of the anthraquinone moiety and their tailoring steps. Moreover, the streamlined total synthesis of AFEs and their analogues boosts the preparation of AFE-based linker-drugs, thus enabling the development of AFE-based antibody–drug conjugates (ADCs). This review summarizes the discovery, mechanism of action, biosynthesis, total synthesis and preclinical studies of AFEs.

Graphical abstract: Anthraquinone-fused enediynes: discovery, biosynthesis and development

Article information

Article type
Review Article
Submitted
19 Aug 2021
First published
21 Oct 2021

Nat. Prod. Rep., 2021, Advance Article

Anthraquinone-fused enediynes: discovery, biosynthesis and development

X. Yan, Nat. Prod. Rep., 2021, Advance Article , DOI: 10.1039/D1NP00054C

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