Target intelligence / Profile preview

Nuclear factor kappa-light-chain-enhancer of activated B cell (NF-κB)

Target
NF-κB
Molecular classification
Transcription factor, DNA-binding protein
01

Overview

Nuclear factor kappa-light-chain-enhancer of activated B cell (NF-κB) is a family of transcription factor protein complexes that control the transcription of DNA, especially genes related to immune and inflammatory responses, cell survival, proliferation, and apoptosis[1][3][5][7]. The family includes five main proteins in mammals: NF-κB1 (p105 and its processed form p50), NF-κB2 (p100 and p52), RelA (p65), RelB, and c-Rel. NF-κB proteins are typically found in the cytoplasm as inactive complexes bound to inhibitor proteins (IκBs); in response to a variety of stimuli—including stress, cytokines, free radicals, bacterial or viral antigens—these inhibitors are degraded, allowing NF-κB to translocate to the nucleus and activate target gene transcription. Dysregulation of NF-κB activity has been strongly implicated in the pathogenesis of cancer, chronic inflammation, autoimmune diseases, and improper immune development. NF-κB activity is considered a major therapeutic target in many disorders, but broad inhibition may lead to immunosuppression and other safety issues[1][3][5].

Other names
Nuclear factor-κBNF-kappaBNuclear factor kappa BNFKBNuclear factor NF-kappa-B p105 subunit (specific subunit, NFKB1)
02

Mechanism of action

Inhibition of IκB kinase (IKK); Inhibition of proteasome-mediated degradation of IκB; Inhibition of NF-κB DNA binding

03

Biological functions

Regulation of DNA transcriptionImmune responseCell survivalCytokine productionCell proliferationApoptosisSignal transduction
04

Disease associations

CancerInflammationAutoimmune diseaseInfectionNeurodegenerative diseaseImproper immune development
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Safety considerations

Broad suppression of immune functionIncreased risk of infectionsPotential effects on normal cell survival and proliferationPossible impact on wound healing and tissue repair
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Interacting drugs

Bortezomib

4 more in the full profile.

07

Biomarkers

NF-κB activation status (e.g., nuclear translocation or DNA binding activity)Expression levels of NF-κB target genes (e.g., proinflammatory cytokines)

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