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Inhibitors of AP-1 and NF-κB Mediated Transcriptional Activation: Therapeutic Potential in Autoimmune Diseases and Structural Diversity

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Cytokines and chemokines play a very important role in a number of inflammatory diseases. In activated T cells, transcription factors such as the activator protein-1 (AP-1) regulate IL-2 production and production of matrix metalloproteinases, the nuclear factor kappa B (NF-κB) is essential for the transcriptional regulation of the proinflammatory cytokines IL-1, IL-6, IL-8 and TNFα, and nuclear factor of activated T-cells (NFAT) is required for the transcriptional regulation of IL-2, IL-3, IL-4, IL-5, IL-8, IL-13, TNFα, and GM-CSF. During the last few years, several groups have developed inhibitors of AP-1, NF-κB or both, and NFAT. This review article presents the recent progress in the development of inhibitors for AP-1, NF-κB, and NFAT mediated transcriptional activation.

Keywords: AP-1; AP-1 PATHWAY; Autoimmune Diseases; Cytokines; Erythromycin; Inhibitors; NF-B; NF-kB PATHWAY; Transcriptional Activation; chemokines

Document Type: Review Article


Publication date: 2002-01-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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