Talaverrucin A, Heterodimeric Oxaphenalenone from Antarctica Sponge-Derived Fungus Talaromyces sp. HDN151403, Inhibits Wnt/β-Catenin Signaling Pathway

作者：Chunxiao Sun, Qianwen Liu, Mudassir Shah, Qian Che, Guojian Zhang, Tianjiao Zhu, Jianfeng Zhou, Xiaozhi Rong, Dehai Li · 发表于：Organic Letters · 年份：2022 · DOI：10.1021/acs.orglett.2c01394 · 被引用次数：23 · 研究领域：Wnt/β-catenin signaling in development and cancer、Cancer-related gene regulation、Developmental Biology and Gene Regulation

The Wnt/β-catenin signaling pathway is an evolutionarily conserved signaling cascade involved in a broad range of biological roles. Dysregulation of the Wnt/β-catenin pathway is implicated in congenital malformations and various kinds of cancers. We discovered a novel Wnt/β-catenin inhibitor, talaverrucin A ( 1 ), featuring an unprecedented 6/6/6/5/5/5/6 fused ring system, from an Antarctica sponge-derived fungus Talaromyces sp. HDN151403. Talaverrucin A exhibits inhibitory activity on the Wnt/β-catenin pathway in both zebrafish embryos in vivo and cultured mammalian cells in vitro, providing a naturally inspired small molecule therapeutic lead to target the Wnt/β-catenin pathway.