TARGETING IKKβ FOR THE TREATMENT OF RHEUMATOID ARTHRITIS

被引：22

作者：

Bamborough, Paul ^{[1
]}

Morse, Mary A. ^{[1
]}

Ray, Keith P. ^{[2
]}

机构：

[1] GlaxoSmithKline R&D, Med Res Ctr, Stevenage SG1 2NY, Herts, England

[2] Ray Biosci Consulting Ltd, Prestwood, Bucks, England

来源：

DRUG NEWS & PERSPECTIVES | 2010年 / 23卷 / 08期

关键词：

NF-KAPPA-B; COLLAGEN-INDUCED ARTHRITIS; HIGHLY SELECTIVE INHIBITOR; PROTEIN-KINASE INHIBITORS; NEMO-BINDING DOMAIN; HIT-TO-LEAD; SIGNALING PATHWAY; MICE LACKING; IN-VIVO; DEPENDENT TRANSCRIPTION;

D O I：

10.1358/dnp.2010.23.8.1447844

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Activation of the nuclear factor-kappa B (NF-kappa B) family of transcription factors results in the expression of numerous genes involved in the regulation of the innate and adaptive immune responses, and has been implicated as a key mechanism in chronic inflammatory diseases including rheumatoid arthritis (RA). The I kappa B kinases (IKKs) are key components in the signaling pathway by which proinflammatory stimuli, such as lipopolysaccharide and tumor necrosis factor-alpha lead to the activation of NE-kappa B. The most widely studied of the IKKs is IKK beta. Inhibitors of the kinase activity of IKK beta offer opportunities for intervention in RA, as well as other inflammatory disorders. Some examples for which the most extensive data are available will here be reviewed.

引用

页码：483 / 490

页数：8

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