Recent Advances in the Development of TGF-β Signaling Inhibitors for Anticancer Therapy

TGF-beta is a multifunctional cytokine that plays an important role in both physiologic and pathologic processes, including cancer. Importantly, TGF-beta has a dual role in tumorigenesis, acting as a tumor suppressor or a tumor promoter, depending on the stage of tumor development The aberrantly upregulated production of TGF-beta has been strongly implicated in tumor progression, angiogenesis, and metastasis, as well as immune evasion. Therefore, hyperactivated TGF-beta signaling is considered a potential therapeutic target for cancer therapy. Numerous inhibitors of overactivated TGF-beta signaling have been developed, and some of them are currently in clinical trials. This review focuses on the TGF-beta signaling that contributes to tumor progression and immune evasion in the tumor microenvironment and presents recent achievements on TGF-beta signaling inhibition as a single or combined therapeutic approach in cancer therapy.