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

[ Vol. 9 , Issue. 2 ]

Author(s):

Moorthy s.s. Palanki   Pages 219 - 227 ( 9 )

Abstract:


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:

Inhibitors, AP-1, NF-B, Transcriptional Activation, Autoimmune Diseases, Cytokines, chemokines, AP-1 PATHWAY, NF-kB PATHWAY, Erythromycin

Affiliation:

Department of Medicinal Chemistry, Celgene Signal Research Division, 5555 Oberlin Drive, San Diego, CA 92121, USA



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