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
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PROTAC 降解细胞内 TGF-β 1 可有效逆转 M2 巨噬细胞诱导的恶性病理事件
DOI：
10.1039/c9cc08391j
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发表时间：
2020-03-07
影响因子：
4.9
通讯作者：
Bu, Xianzhang
中科院分区：
文献类型：
--
作者：
Feng, Yanqiao;Su, Hui;Bu, Xianzhang
首次以嵌合体为靶点的蛋白水解法用于转化生长因子-β1(转化生长因子-β1)的细胞内消除，转化生长因子-β1可导致多种疾病。设计合理的DT-6能有效降解细胞内的转化生长因子-β1，抑制M2巨噬细胞诱导的上皮向间充质转化和癌细胞的侵袭性迁移。
The first proteolysis targeting chimeras for the intracellular elimination of transforming growth factor-beta 1 (TGF-beta 1), which contributes to various diseases, are described. The appropriately designed DT-6 could efficiently degrade intracellular TGF-beta 1, and inhibit M2 macrophage induced epithelial to mesenchymal transition and invasive migration of cancer cells.