Degradation of intracellular TGF-β1 by PROTACs efficiently reverses M2 macrophage induced malignant pathological events

  • Chem Commun (Camb). 2020 Mar 5;56(19):2881-2884. doi: 10.1039/c9cc08391j.
Yanqiao Feng  1 Hui Su  1 Yunzhi Li  1 Chunxiang Luo  1 Huiying Xu  1 Youqiao Wang  1 Haixia Sun  1 Guohui Wan  1 Binhua Zhou  2 Xianzhang Bu  1
Affiliations
Abstract

The first proteolysis targeting chimeras for the intracellular elimination of transforming growth factor-β1 (TGF-β1), which contributes to various diseases, are described. The appropriately designed DT-6 could efficiently degrade intracellular TGF-β1, and inhibit M2 macrophage induced epithelial to mesenchymal transition and invasive migration of Cancer cells.

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