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Hesperetin: an inhibitor of the transforming growth factor-? (TGF-?) signaling pathway.

ABSTRACT: 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-? (TGF-?) 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-? pathway. In addition we demonstrated that this compound hinders TGF-?1-induced cancer cell migration and invasion. These results suggest a potential future application for hesperetin as a TGF-? inhibitor in cancer therapy.

SUBMITTER: Yang Y

PROVIDER: S-EPMC3513570 | biostudies-literature | 2012 Dec

REPOSITORIES: biostudies-literature

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

Yang Yong Y Wolfram Joy J Shen Haifa H Fang Xiaohong X Ferrari Mauro M

European journal of medicinal chemistry 20121025

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 ...[more]

PMID: 23153811

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