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Selective inhibitors of nuclear factor-kappaB activation and uses thereof
Selective inhibitors of nuclear factor-kappaB activation and uses thereof
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机译:核因子-κB活化的选择性抑制剂及其用途
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摘要
The present invention provides cell permeable NF-κB inhibitors consist of a polypeptide derived from the p65 subunit of NF-κB and a protein transduction domain derived from antennapedia third helix sequence. The inhibitor suppressed NF-κB activation induced by TNF, LPS, IL-1, okadaic acid, PMA, H2O2 and cigarette smoke condensate. NF-κB-regulated reporter gene expression induced by TNF, TNFR1, TRADD, TRAF2, NIK, IKK and p65 was suppressed by the inhibitor. The inhibitor enhanced TNF- and chemotherapeutic agent-induced apoptosis. Overall these results demonstrate a NF-κB inhibitor that can selectively inhibit NF-κB activation induced by various inflammatory stimuli, downregulate NF-κB mediated gene expression and upregulate apoptosis.
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机译:本发明提供细胞可渗透的NF-κB抑制剂,其由衍生自NF-κB的p65亚基的多肽和衍生自触足第三螺旋序列的蛋白质转导域组成。该抑制剂抑制了TNF,LPS,IL-1,冈田酸,PMA,H 2 Sub> O 2 Sub>和香烟烟雾冷凝物诱导的NF-κB活化。抑制剂抑制了TNF,TNFR1,TRADD,TRAF2,NIK,IKK和p65诱导的NF-κB调控的报告基因表达。该抑制剂可增强TNF和化疗药物诱导的细胞凋亡。总的来说,这些结果表明NF-κB抑制剂可以选择性地抑制由各种炎性刺激诱导的NF-κB活化,下调NF-κB介导的基因表达并上调凋亡。
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