2. Academic Validation
  3. 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
Affiliations

Affiliations

  • 1 School of Pharmaceutical Sciences, Sun Yat-sen University, GuangZhou 510006, China. zhoubh5@mail.sysu.edu.cn phsbxzh@mail.sysu.edu.cn.
  • 2 School of Pharmaceutical Sciences, Sun Yat-sen University, GuangZhou 510006, China. zhoubh5@mail.sysu.edu.cn phsbxzh@mail.sysu.edu.cn and School of Chinese Pharmacy, Guizhou Minzu University, Guiyang 550025, China.
PMID: 32037404 DOI: 10.1039/c9cc08391j
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-156512
    99.82%, TGF-β1抑制剂
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