Hesperetin: An inhibitor of the transforming growth factor-β (TGF-β) signaling pathway

Yong Yang, Joy Wolfram, Haifa Shen, Xiaohong Fang, Mauro Ferrari

Research output: Contribution to journalArticlepeer-review

41 Scopus citations


We have identified a previously unknown function of the natural compound, hesperetin. Here, we demonstrate that this small molecular agent is able to inhibit the transforming growth factor-β (TGF-β) signaling pathway. Single-molecule force measurements and single-molecule fluorescence imaging show that hesperetin interferes with ligand-receptor interactions. Furthermore, by Western blot analysis, it was confirmed that hesperetin also inhibits the phosphorylation of Smad3, a down-stream target of the TGF-β pathway. In addition we demonstrated that this compound hinders TGF-β1-induced cancer cell migration and invasion. These results suggest a potential future application for hesperetin as a TGF-β inhibitor in cancer therapy.

Original languageEnglish (US)
Pages (from-to)390-395
Number of pages6
JournalEuropean Journal of Medicinal Chemistry
StatePublished - Dec 2012


  • Atomic force microscopy
  • Hesperetin
  • Single-molecule fluorescence imaging
  • TGF-β inhibition

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology


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