The transforming growth factor-beta (TGFbeta) is a potent regulator of tumorigenesis. In cancer, two distinctive behaviors of TGFbeta have been reported as a tumor suppressor at early stage of the disease, and as a tumor promoter at later stages. The past decades, the dualistic role of TGFbeta has garnered a lot of attention. As a result, cancer researchers' has been tasked to elucidate how TGFbeta signaling may lead to metastatic dissemination, how to tackle carcinogenesis and which therapeutic strategies should be adopted. Consequently, TGFbeta signaling pathways have been considered as appropriate targets for cancer therapy. The TGFbeta therapeutic strategies have emerged at three levels: ligand, ligand-receptor interaction and intracellular signaling level. Promising inhibitors of TGFbeta signaling have entered clinical trials and shown encouraging results. Here we review the three strategies of TGFbeta signaling inhibition and theirs applications in treatment of cancer.

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