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A Perspective on the Development of TGF-β Inhibitors for Cancer Treatment

1
Laboratory of Experimental Pathology, Graduate School of Comprehensive Human Sciences, University of Tsukuba, 1-1-1 Tennodai, Tsukuba, Ibaraki 305-8575, Japan
2
Cancer Signaling, Faculty of Medicine, University of Tsukuba, 1-1-1 Tennodai, Tsukuba, Ibaraki 305-8575, Japan
3
Peptide Core Facility, Transborder Medical Research Center, University of Tsukuba, 1-1-1 Tennodai, Tsukuba, Ibaraki 305-8575, Japan
4
Oncode Institute and Cell Chemical Biology, Leiden University Medical Center, 2300 RC Leiden, The Netherlands
*
Author to whom correspondence should be addressed.
Biomolecules 2019, 9(11), 743; https://doi.org/10.3390/biom9110743
Received: 14 September 2019 / Revised: 22 October 2019 / Accepted: 4 November 2019 / Published: 17 November 2019
(This article belongs to the Special Issue TGF-Beta Signaling in Physiology and Pathology)
Transforming growth factor (TGF)-β is a secreted multifunctional cytokine that signals via plasma membrane TGF-β type I and type II receptors and intercellular SMAD transcriptional effectors. Aberrant inter- and intracellular TGF-β signaling can contribute to cancer progression. In normal cells and early stages of cancer, TGF-β can stimulate epithelial growth arrest and elicit a tumor suppressor function. However, in late stages of cancer, when the cytostatic effects of TGF-β in cancer cells are blocked, TGF-β signaling can act as tumor promoter by its ability to stimulate epithelial-to-mesenchymal transition of cancer cells, by stimulating angiogenesis, and by promoting evasion of immune responses. In this review, we will discuss the rationale and challenges of targeting TGF-β signaling in cancer and summarize the clinical status of TGF-β signaling inhibitors that interfere with TGF−β bioavailability, TGF-β/receptor interaction, or TGF-β receptor kinase function. Moreover, we will discuss targeting of TGF-β signaling modulators and downstream effectors as well as alternative approaches by using promising technologies that may lead to entirely new classes of drugs. View Full-Text
Keywords: cancer therapy; epithelial-to-mesenchymal transition; immune evasion; signaling; SMAD; TGF-β; tumor microenvironment cancer therapy; epithelial-to-mesenchymal transition; immune evasion; signaling; SMAD; TGF-β; tumor microenvironment
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Huynh, L.K.; Hipolito, C.J.; ten Dijke, P. A Perspective on the Development of TGF-β Inhibitors for Cancer Treatment. Biomolecules 2019, 9, 743.

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