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Disitertide is a peptide inhibitor of TGF-β1-mediated activity that corresponds to amino acids 730-743 of the membrane proximal ligand-binding domain of human TGF-β receptor type 3 (TGFBR3), also known as beta-glycan.1,2 It inhibits the binding of TGF-β1 to TGF-β1 receptors in Mv 1 Lu mink lung epithelial cells by 95% at 200 µg/ml and rescues TGF-β1-inhibited growth in the same cells.1 Disitertide reduces TGF-β1-mediated reporter expression in primary human fetal skin fibroblasts at 50 and 100 µg/ml and decreases hepatic stellate cell (HSC) activation and liver fibrosis in a rat model of chronic liver injury. Topical application of disitertide reduces connective tissue growth factor (CTGF) levels and the number of myofibroblasts expressing α-smooth muscle actin (α-SMA) in the skin secretions of mice in a model of scleroderma and decreases dermal fibrosis in the same model.2
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1. A synthetic peptide from transforming growth factor β type III receptor inhibits liver fibrogenesis in rats with carbon tetrachloride liver injury. Cytokine 22(1-2), 12-20 (2003).
2. Topical application of a peptide inhibitor of transforming growth factor-