| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1394478 | European Journal of Medicinal Chemistry | 2012 | 6 Pages |
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.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Hesperetin blocks TGFβ ligand–receptor interactions. ► Hesperetin inhibits downstream TGFβ-signaling. ► Hesperetin decreases TGFβ-induced cancer cell migration and invasion.
