SF 1670是一種PTEN抑制劑(IC 50 = 2 μ M)。PTEN(Phosphatase and Tensin Homolog deleted on Chromosome 10)是一種3-磷酸肌醇磷酸酶,可將PI(3 4 5)P3轉化為PI(4 5)P2,從而對抗PI 3-K對PKB/Akt的激活。用SF 1670預處理中性粒細胞導致增強的fMLP-1誘導的PI(3 4 5)P3信號傳導效應,例如Akt磷酸化、NADPH氧化酶介導的超氧化物形成、細胞極化、趨化性遷移和吞噬作用。SF1670也抑制CD45(IC50 = 200 nM)。Publications Powered by Bioz See more details on Bioz 1)Cojohari O. 等(2016)?!叭祟惥藜毎《菊T導Akt的非典型激活,以刺激短壽命單核細胞的存活?!癑 Virol 90(14):6443-6452.2)Yousefi B. 等(2017)。Balaglitazone通過在白血病細胞中以PPAR 3依賴的方式上調PTEN來逆轉P-糖蛋白介導的多藥耐藥?!癟umor Biology 39(10):1010428317716501.3)Alsina-Sanchés E. 等(2018)。“ALK 1(激活素受體樣激酶1)缺失通過PI 3 K(磷脂酰肌醇3-激酶)激活導致小鼠和人類血管增生。“動脈血栓形成和血管生物學38(5):1216-1229.4)Mitchell J.等人(2018)?!敖Y腸抑制磷酸酶和張力蛋白同源物增加結腸炎細菌導致結腸炎的發展在Il 10-/-小鼠。炎癥性腸病24(8):1718-1732。
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SF1670 is an inhibitor of PTEN (IC50 = 2 ??M). PTEN (Phosphatase and Tensin Homolog deleted on Chromosome 10) is a 3a€? phosphoinositide phosphatase that converts PI(3 4 5)P3 to PI(4 5)P2 thus opposing PKB/Akt activation by PI 3-K. Pretreatment of neutrophils with SF1670 leads to enhanced fMLP-1 induced PI(3 4 5)P3 signaling effects such as Akt phosphorylation NADPH oxidase-mediated superoxide formation cell polarization chemotactic migration and phagocytosis. SF1670 also inhibits CD45 (IC50 = 200 nM).Publications Powered by Bioz See more details on Bioz1) Cojohari O. et al. (2016). "Human cytomegalovirus induces an atypical activation of Akt to stimulate the survival of short-lived monocytes." J Virol 90(14): 6443-6452.2) Yousefi B. et al. (2017). "Balaglitazone reverses P-glycoprotein-mediated multidrug resistance via upregulation of PTEN in a PPAR?3-dependent manner in leukemia cells." Tumor Biology 39(10): 1010428317716501.3) Alsina-Sanch?-s E. et al. (2018). "ALK1 (Activin-Receptor Like Kinase 1) Loss Results in Vascular Hyperplasia in Mice and Humans Through PI3K (Phosphatidylinositol 3-Kinase) Activation." Arteriosclerosis thrombosis and vascular biology 38(5): 1216-1229.4) Mitchell J. et al. (2018). "Colonic Inhibition of Phosphatase and Tensin Homolog Increases Colitogenic Bacteria Causing Development of Colitis in Il10-/- Mice." Inflammatory Bowel Diseases 24(8): 1718-1732.