IкB激酶生物学特征及其抑制剂研究进展  

Research progress of the biological characteristics of IкB kinase and its inhibitors

作　　者：薛建跃[1] 周彬[2] 张大永[2] 吴晓明[2] 

机构地区：[1]巢湖学院化学与材料科学系,安徽巢湖238000 [2]中国药科大学药学院,江苏南京210009

出　　处：《药学学报》2011年第3期253-260,共8页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(30973607);江苏省"六大人才高峰"资助项目(Y092003)

摘　　要：NF-кB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。IкB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游激酶对其的磷酸化。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、抗肿瘤药物的研发提供了极为有利的切入点。The NF-кB 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.IкB 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 phosphorylation by its upstream kinases.Actually,there are two methods of activation of the NF-кB pathway,and both of the methods need the IKK complex.Given to the crucial role of IKK,researchers have isolated and synthesized amounts of IKK inhibitors,and these provide a great convenience to develop novel anti-inflammatory and anti-tumor drugs.

关 键 词：NF-кB IкB激酶 抗炎 抗肿瘤 

分 类 号：R916[医药卫生—药学]