化学性质

资料参考

VGX-1027是高效的免疫调节剂[1].

免疫治疗是指通过抑制\诱导或增强免疫反应从而治疗疾病.

VGX-1027是异恶唑啉化合物,具有高效免疫调节特性[1].微阵列分析中,脂多糖(LPS)刺激后,VGX-1027调节参与免疫活化\抗原加工和呈递的基因表达[2].在CD4+CD25 T细胞中,VGX-1027抑制肠道菌抗原诱导的细胞增殖[3].

在自发或加速糖尿病的NOD小鼠中,VGX-1027显著降低胰岛炎和糖尿病的发病率.在CBA/H小鼠中,VGX-1027显著抑制多次低剂量链脲佐菌素诱导的高血糖和破坏性胰岛炎的发展.同时,VGX-1027也抑制胰岛中诱导型一氧化氮合成酶介导的一氧化氮\巨噬细胞迁移抑制因子\炎症介质肿瘤坏死因子α和IL-1β的产生[1].在系统性红斑狼疮(SLE)的NZB/NZW F1小鼠中,VGX-1027改善疾病,提高存活[2].在急性炎症性肠炎小鼠中,VGX-1027抑制结肠炎的发展.VGX-1027也减少促炎细胞因子TNF-α\IL-12p70\白介素(IL)-1β\干扰素(IFN)-γ和核因子NF-κB (p65)的产生[3].

参考文献：
[1].  Stosic-Grujicic S, Cvetkovic I, Mangano K, et al. A potent immunomodulatory compound, (S,R)-3-Phenyl-4,5-dihydro-5-isoxazole acetic acid, prevents spontaneous and accelerated forms of autoimmune diabetes in NOD mice and inhibits the immunoinflammatory diabetes induced by multiple low doses of streptozotocin in CBA/H mice. J Pharmacol Exp Ther, 2007, 320(3): 1038-1049.
[2].  Fagone P, Muthumani K, Mangano K, et al. VGX-1027 modulates genes involved in lipopolysaccharide-induced Toll-like receptor 4 activation and in a murine model of systemic lupus erythematosus. Immunology, 2014, 142(4): 594-602.
[3].  Mangano K, Sardesai N, D'Alcamo M, et al. In vitro inhibition of enterobacteria-reactive CD4+CD25- T cells and suppression of immunoinflammatory colitis in mice by the novel immunomodulatory agent VGX-1027. Eur J Pharmacol, 2008, 586(1-3): 313-321.

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