Disitertide (P144) (P144) 是一种肽类转化生长因子-β 1 (TGF-β1) 抑制剂，专门设计用于阻断与其受体的相互作用。 Disitertide (P144) (P144) 也是一种 PI3K 抑制剂和凋亡诱导剂。
Disitertide is an inhibitor of TGF-β1.
Disitertide (P144) prevents TGF-β1-dependent inhibition of MV1Lu proliferation in vitro and markedly reduces binding of TGF-β1 to its receptors. Disitertide blocks TGF-β1-dependent stimulation of a reporter gene under the control of human α2(I) collagen promoter[1].
Treatment with Disitertide at low doses causes a significant inhibition of HSC activation and a marked reduction in liver fibrosis in a rat model of chronic exposure to CCl4. A dose as low as 70 μg of the 15-mer peptide Disitertide, given to rats (300 g body weight) on alternate days, decreases fibrogenesis significantly during chronic exposure to CCl4[1].
[1]. Ezquerro IJ et al. A synthetic peptide from transforming growth factor beta type III receptor inhibits liver fibrogenesis in rats with carbon tetrachloride liver injury. Cytokine. 2003 Apr;22(1-2):12-20.
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