Target intelligence / Profile preview

Activator protein 1 and Nuclear factor kappa B signaling pathways (AP-1/NF-κB)

Target
AP-1/NF-κB
Molecular classification
Transcription factor, Intracellular signaling pathway
01

Overview

Activator protein 1 (AP-1) and Nuclear factor kappa B (NF-κB) are pivotal transcription factor complexes that integrate signals from various stimuli, including cytokines, growth factors, and environmental stress, to regulate gene expression (PMID: 10889797). AP-1 is primarily composed of Jun and Fos family proteins, while NF-κB is a dimeric complex of Rel-family proteins such as p65 and p50 (PMID: 12496471). These pathways play central roles in the immune response, inflammation, and cell survival, and their constitutive activation is a hallmark of many cancers and autoimmune disorders (PMID: 11244040). Pharmacological modulation often involves glucocorticoids, which antagonize both factors, or proteasome inhibitors like bortezomib that prevent NF-κB activation (PMID: 14707102). Because these pathways control a vast array of physiological processes, therapeutic targeting requires careful balance to avoid severe immunosuppression or systemic toxicity (PMID: 15123778).

Other names
AP-1 signalingNF-kappaB signalingPro-inflammatory transcription factor pathwaysJun/Fos and Rel signaling
02

Mechanism of action

Inhibition of nuclear translocation, prevention of DNA binding, or inhibition of upstream activating kinases such as the IKK complex or MAPKs.

03

Biological functions

Signal transductionImmune responseInflammationCell proliferationApoptosisStress response
04

Disease associations

CancerInflammationAutoimmune diseaseInfection
05

Safety considerations

Broad immunosuppressionImpaired wound healingSystemic toxicity due to pleiotropic effectsPotential for metabolic disturbances
06

Interacting drugs

Dexamethasone

5 more in the full profile.

07

Biomarkers

Phospho-c-Jun levelsNuclear p65 localizationInterleukin-6 (IL-6)Tumor necrosis factor-alpha (TNF-alpha)

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