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- W1968070070 abstract "Transforming growth factor (TGFβ) is a 25-kDa dimeric polypeptide that plays a key role in a variety of physiological processes and disease states. Blocking TGFβ signaling represents a potentially powerful and conceptually novel approach to the treatment of disorders in which the signaling pathway is constitutively activated, such as cancer, chronic inflammation with fibrosis and select immune disorders. In this paper, we describe the biological properties of a novel series of quinazoline-derived inhibitors of the type I transforming growth factor receptor kinase (TβKIs) that bind to the ATP-binding site and keep the kinase in its inactive conformation. These compounds effectively inhibited TGFβ-induced Smad2 phosphorylation in cultured cells in vitro with an IC50 between 20 and 300 nM. Moreover, TβKIs were able to broadly block TGFβ-induced reporter gene activation. Finally, TβKIs inhibited TGFβ-mediated growth inhibition of normal murine mammary epithelial cells (NMuMG) and mink lung epithelial cells (Mv1Lu), and TGFβ-induced epithelial-mesenchymal transdifferentiation (EMT) of NMuMG cells. Thus, these chemical TβKIs have the potential to be further developed as anti-cancer and -fibrosis agents. In addition, they represent valuable new tools for dissecting the biochemical mechanisms of TGFβ signal transduction and understanding the role of TGFβ signaling pathways in different physiological and disease processes." @default.
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- W1968070070 date "2004-07-01" @default.
- W1968070070 modified "2023-10-15" @default.
- W1968070070 title "Selective inhibitors of type I receptor kinase block cellular transforming growth factor-β signaling" @default.
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- W1968070070 doi "https://doi.org/10.1016/j.bcp.2004.03.011" @default.
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