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一种免疫系统中重要转录因子NF-κB的抑制剂
由D. Baltimore等人于1986年识别到的NF-κB (核因子κB) 是一种控制基因转录的细胞内蛋白质复合物。1) NF-κB通常和IκB (抑制剂 κB)形成无活性复合物，游离在细胞质中。受到细胞外信号——磷酸化IκBα刺激后，IKK (IκB激酶)被激活，随后蛋白酶体使IκBα发生降解。之后，NF-κB转移到细胞核中，诱发与炎症免疫反应、细胞凋亡抑制分子、细胞抑制分子等相关的基因编码分子的转录。2) 小分子BAY 11-7082 能够抑制IKK对IκBα的磷酸化反应。3) 已有报道使用BAY 11-7082作为NF-κB抑制剂应用于癌症、炎症、病毒感染等研究中。4-7)
文献
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