Disitertide(P144)TFA是转化生长因子TGFβ1的多肽抑制剂，特异性的阻断其与受体间的相互作用。Disitertide(P144)TFA也是PI3K的抑制剂和凋亡(apoptosis)诱导剂。
Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) TFA is also a PI3K inhibitor and an apoptosis inducer[1][2][3][4][5].
Disitertide (100 μg/mL) suppresses the protein expression levels of PI3K and p-Akt, and induce the protein expression of Bax in MC3T3-E1 cells[2]. Disitertide (TGF-β1 inhibitor) abrogates the MACC1- AS1 expression in GC cells, suggesting that targeting TGFβ signaling pathway may be a potential strategy to inhibit MSC-induced stemness and chemoresistance[3].Disitertide (P144, 10 μg/mL to 200 μg/mL) affects proliferation, induces apoptosis as well as anoikis in A172 and U-87 MG GBM cell lines[5]. Western Blot Analysis[2] Cell Line: Mouse embryo osteoblast precursor MC3T3-E1 cells.
Disitertide (Topical application, 300 μg/mL) may promote scar maturation and clinical improvement of hypertrophic scar morphology features in an "in vivo" model in nude mice after two weeks of treatment[4]. Animal Model: Human hypertrophic scars were implanted in 60 nude mice[4].
[1]. Cindy Neuzillet, et al. Targeting the TGFβ pathway for cancer therapy. Pharmacol Ther. 2015 Mar;147:22-31. [2]. Jun Yang, et al. Upregulation of microRNA?590 in rheumatoid arthritis promotes apoptosis of bone cells through transforming growth factor?β1/phosphoinositide 3?kinase/Akt signaling. Int J Mol Med. 2019 May;43(5):2212-2220. [3]. Wanming He, et al. MSC-regulated lncRNA MACC1-AS1 promotes stemness and chemoresistance through fatty acid oxidation in gastric cancer. Oncogene. 2019 Jun;38(23):4637-4654. [4]. Shan Shan Qiu, et al. Effect of P144? (Anti-TGF-β) in an "In Vivo" Human Hypertrophic Scar Model in Nude Mice. PLoS One. 2015 Dec 31;10(12):e0144489. [5]. Gabriel Gallo-Oller, et al. P144, a Transforming Growth Factor beta inhibitor peptide, generates antitumoral effects and modifies SMAD7 and SKI levels in human glioblastoma cell lines. Cancer Lett. 2016 Oct 10;381(1):67-75.
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