iкb激酶生物学特征及抑制剂的研究进展.pdfVIP

药学学报 Acta Pharmaceutica Sinica 20 11, 46 (3) : 253260 ·253 · I B 酶生物学特征及其抑制剂研究进展 1 2 2* 2 薛建跃 , 周 彬 , 张大永 , 吴晓明 ( 1. 巢湖学院化学与材料科学系, 安徽 巢湖 238000; 2. 中国药科大学 学院, 江苏 南京 210009) 摘要: NF- B 信号通路调控超过 150 个靶基因的表达, 其中包括细胞因子、炎症趋化因子、白细胞黏附因子、 诱导效应酶等, 对机体免疫反应、炎症反应、应激反应、凋亡等发挥重要的作用。I B 激酶 (IKK) 是该信号通 路的关键激酶, 其结构较为独特, 由催化亚基和调节亚基组成。IKK 的激活需要两种亚基的相互作用和上 激酶 对其的磷酸化。鉴于 IKK 的关键作用, 研究者们以其为靶点已研发出大量的抑制剂, 为新型抗炎、抗肿瘤 物 的研发提供了极为有利的切入点。 关键词: NF- B; I B 激酶; 抗炎; 抗肿瘤 中图分类号: R916 文献标识码:A 文章编号: 05 13-4870 (20 11) 03-0253-08 Research progress of the biological characteristics of I B kinase and its inhibitors 1 2 2* 2 XUE Jian-yue , ZHOU Bin , ZHANG Da-yong , WU Xiao-ming (1. Dep artment of Chemistry and Materials, Chaohu College, Chaohu 238000, China; 2. School of Pharmacy, China Pharmaceutical University, Nanj ing 210009, China) Abstract: The NF- B pathway regulates the expression of over 150 target genes, e.g., cytokines, chemokines, leukocyte adhesion molecules and inducible effector enzymes. Consequently, it plays a crucial role in innate and adaptive immune responses, inflammatory response, stress responses, apoptosis and so on. I B kinase (IKK) is the key of this pathway, and it owns a special structure which consists of catalytic subunit and regulatory subunit. Naturally, the activation of IKK needs the interaction of the two subunits and phosphorylat