Degradation of intracellular TGF-β1 by PROTACs efficiently reverses M2 macrophage induced malignant pathological events.
Yanqiao FengHui SuYunzhi LiChunxiang LuoHuiying XuYouqiao WangHaixia SunGuohui WanBinhua ZhouXianzhang BuPublished in: Chemical communications (Cambridge, England) (2020)
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.