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

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
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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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