Characterization of SIS3, a novel specific inhibitor of Smad3, and its effect on transforming growth factor-β1-induced extracellular matrix expression

M Jinnin, H Ihn, K Tamaki - Molecular pharmacology, 2006 - Elsevier
This is the first report that characterizes specific inhibitor of Smad3 (SIS3) as a potent and
selective inhibitor of Smad3 function. In the reporter assay, the increased luciferase activity
of p3TP-lux by the overexpression of constitutively active form of ALK-5 was abrogated by
the treatment with SIS3 in a dose-dependent manner. Immunoprecipitation revealed that
SIS3 attenuated the transforming growth factor (TGF)-β1-induced phosphorylation of Smad3
and interaction of Smad3 with Smad4. On the other hand, this reagent did not affect the …