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A New TGF-β1 Inhibitor, CTI-82, Antagonizes Epithelial–Mesenchymal Transition through Inhibition of Phospho-SMAD2/3 and Phospho-ERK

1
Department of Biomedical Sciences, Asan Medical Center, AMIST, University of Ulsan College of Medicine, Seoul 05505, Korea
2
College of Pharmacy, CHA University, Pocheon 487-010, Korea
*
Authors to whom correspondence should be addressed.
Biology 2020, 9(7), 143; https://doi.org/10.3390/biology9070143
Received: 22 May 2020 / Revised: 14 June 2020 / Accepted: 18 June 2020 / Published: 28 June 2020
(This article belongs to the Section Cell Biology)
Transforming growth factor-β1 (TGF-β1) is highly expressed in the tumor microenvironment and known to play a multifunctional role in cancer progression. In addition, TGF-β1 promotes metastasis by inducing epithelial–mesenchymal transition (EMT) in a variety of tumors. Thus, inhibition of TGF-β1 is considered an important strategy in the treatment of cancer. In most tumors, TGF-β1 signal transduction exhibits modified or non-functional characteristics, and TGF-β1 inhibitors have various inhibitory effects on cancer cells. Currently, many studies are being conducted to develop TGF-β1 inhibitors from non-toxic natural compounds. We aimed to develop a new TGF-β1 inhibitor to suppress EMT in cancer cells. As a result, improved chalcone-like chain CTI-82 was identified, and its effect was confirmed in vitro. We showed that CTI-82 blocked TGF-β1-induced EMT by inhibiting the cell migration and metastasis of A549 lung cancer cells. In addition, CTI-82 reduced the TGF-β1-induced phosphorylation of SMAD2/3 and inhibited the expression of various EMT markers. Our results suggest that CTI-82 inhibits tumor growth, migration, and metastasis. View Full-Text
Keywords: TGF-β1; TGF-β1 inhibitor; EMT; migration; invasion; chalcone TGF-β1; TGF-β1 inhibitor; EMT; migration; invasion; chalcone
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Jeong, J.-H.; Kim, H.; Park, S.-H.; Park, H.; Jeong, M.; Kwak, S.; Sung, G.-J.; Song, J.-H.; Na, Y.; Choi, K.-C. A New TGF-β1 Inhibitor, CTI-82, Antagonizes Epithelial–Mesenchymal Transition through Inhibition of Phospho-SMAD2/3 and Phospho-ERK. Biology 2020, 9, 143.

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