Modulation of the EMT/MET process by pyrrole-imidazole polyamide targeting human transforming growth factor-β1

Kosuke Saito, Noboru Fukuda, Ken Ichi Shinohara, Yoshikazu Masuhiro, Shigemasa Hanazawa, Hiroyuki Matsuda, Kyoko Fujiwara, Takahiro Ueno, Masayoshi Soma

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)


Transforming growth factor-β1 (TGF-β1) is a potent induction factor for epithelial-mesenchymal transition (EMT). Mesenchymal-epithelial transition (MET), as the inverse process of EMT, has recently been reported to promote the induction of induced pluripotent stem cells (iPSCs). We have developed pyrrole-imidazole (PI) polyamide, a novel gene regulator that targets human TGF-β1, and investigated its effects on the EMT/MET process. PI polyamide targeted to TGF-β1 significantly inhibited the mRNA expression of TGF-β1 and SNAI1 as an EMT marker and increased mRNA and protein expression of E-cadherin in human epithelial cells. To enhance the induction of iPSCs by the MET process, PI polyamide targeted to TGF-β1 was applied to human fibroblasts transfected with exogenous reprogramming factors by Sendai virus vector and grown in human iPSCs. The PI polyamide significantly increased the number of alkaline phosphatase-positive colonies. The expression of undifferentiated markers was also observed in these colonies. These results suggest that PI polyamide targeted to human TGF-β is a novel compound that can control the EMT/MET process of human epithelial cells and enhance the induction of human fibroblasts to iPSCs.

Original languageEnglish
Pages (from-to)112-120
Number of pages9
JournalInternational Journal of Biochemistry and Cell Biology
Publication statusPublished - 19 Aug 2015


  • Epithelial-mesenchymal transition
  • Mesenchymal-epithelial transition
  • Pyrrole-imidazole polyamide
  • Transforming growth factor-β1


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