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J Cell Biochem. 2019 Jan;120(1):977-987. doi: 10.1002/jcb.27460. Epub 2018 Sep 14.

Novel TGF-β1 inhibitor antagonizes TGF-β1-induced epithelial-mesenchymal transition in human A549 lung cancer cells.

Jeong JH1,2, Jang HJ3, Kwak S1,2, Sung GJ1,2, Park SH1,2, Song JH1,2, Kim H1,2, Na Y4, Choi KC1,2.

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Department of Biomedical Sciences, Asan Medical Center, AMIST, University of Ulsan College of Medicine, Seoul, South Korea.
Department of Pharmacology, University of Ulsan College of Medicine, Seoul, South Korea.
College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul, South Korea.
College of Pharmacy, CHA University, Pocheon, South Korea.


Transforming growth factor β1 (TGF-β1), a multifunctional cytokine, is known to promote tumor invasion and metastasis and induce epithelial-mesenchymal transition (EMT) in various cancer cells. Inhibition of TGF-β1 signaling is a new strategy for cancer therapy. Most cancer cells display altered or nonfunctional TGF-β1 signaling; hence, TGF-β1 inhibitors exert limited effects on these cells. Recent studies have suggested that developing a TGF-β1 inhibitor from natural compounds is a key step to create novel therapeutic agents. This study aimed to develop a new anti-TGF-β1 therapy for cancer. We found an improved analog of chalcones, compound 67, and investigated its effects in vitro. We demonstrated the inhibitory role of compound 67 through migration and invasion assays on TGF-β1-induced EMT of human A549 lung cancer cells. Compound 67 inhibited TGF-β1-induced smad2 phosphorylation, suppressed TGF-β1-induced EMT markers, matrix metalloproteinase-2 (MMP-2) and MMP-9, and inhibited migration and invasion of A549 cells. The study results showed that compound 67 is useful to prevent tumor growth and metastasis.


chalcone; epithelial-mesenchymal transition (EMT); invasion; lung cancer; migration; transforming growth factor-β1 (TGF-β1)


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