| ID | 1144 | |
| PMID | 16117784 | |
| Year | 2005 | |
| Sequence | TSLDASIIWAMMQN | |
| Name | P144 | |
| Length | 14 | |
| N-Terminal Modification | Free | |
| C-Terminal Modification | Free | |
| Linear/ Cyclic | Linear | |
| Chirality | L | |
| Chemical Modification | None | |
| Origin of Peptide | Derived from the membrane-proximal ligand-binding domain of human TGF-β1 type III receptor (β-glycan) | |
| Nature of Peptide/Cargo | Interferes with TGF-β1 binding to its cellular receptors on Mv1Lu cells. Potent in vivo anti-fibrotic activity in the liver of rats receiving CCl4 | |
| Mechanism | P144 prevented TGF-β1-dependent inhibition of Mv1Lu cell proliferation and, in cultured fibroblasts, it induced a concentration-dependent decrease on TGF-β1-dependent stimulation of a reporter gene under the control of human α2(I) collagen promoter | |
| Cargo Sequence/Structure | None | |
| Name of cargo | Not applicable | |
| Assay | Sircol Collagen Assay kit, histological and immunohistochemical studies | |
| Enhancer | Skin sclerosis induced by bleomycin | |
| Properties of enhancer | Not mentioned | |
| Concentration | 10 g dimethicone, 40 g liquid paraffin, 0.1 g chlorocresol, 0.5 g cetrimide, and 5 g ketostearic alcohol. This mixture was warmed to 70ͦC and emulsified with 44.28 of water plus 0.010 g of P144 previously dissolved in 100 µL of dimethyl sulfoxide | |
| Incubation time | Daily application of 100µl of the P144 peptide lipogel preparation onto the shaved skin of the P144 peptide lipogel preparation for 4 weeks | |
| Tissue permeability (value with units) | Dermal thickness: Bleomycin treated-180%, Bleomycin plus P144 lipogel emulsion-120%, Bleomycin plus vehicle-200%. Soluble collagen: Bleomycin treated-215%, Bleomycin plus P144 lipogel emulsion-150%, Bleomycin plus vehicle-220%. Data represent mean±SD of 10 mice per group, and the values of PBS-treated mice are set to 100%. | |
| Tissue Sample | Shaved skin area of female C3H mice | |
| Ex vivo/In vivo/In vitro | in vitro | |
| STRUCTURE |
| |
| SMILES | N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC (=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O) N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C (=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(=O)N)C=O | |