Research progress of the biological characteristics of IkappaB kinase and its inhibitors].

Jian-Yue Xue, Bin Zhou, Da-Yong Zhang, Xiao-Ming Wu

Department of Chemistry and Materials, Chaohu College, Chaohu 238000, China.

Yao xue xue bao = Acta pharmaceutica Sinica 2011 Mar

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The NF-kappaB 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. IkappaB 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-kappaB 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.

Citation

Jian-Yue Xue, Bin Zhou, Da-Yong Zhang, Xiao-Ming Wu. Research progress of the biological characteristics of IkappaB kinase and its inhibitors]. Yao xue xue bao = Acta pharmaceutica Sinica. 2011 Mar;46(3):253-60