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.
Affiliations
- 1. School of Pharmaceutical Sciences, Sun Yat-sen University, GuangZhou 510006, China. [email protected] [email protected].
- 2. School of Pharmaceutical Sciences, Sun Yat-sen University, GuangZhou 510006, China. [email protected] [email protected] 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.
Products
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Cat. No.Product NameDescriptionTargetResearch Area
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target: TGF-beta/SmadResearch Areas: Cancer