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NF-kappa B TF proteins

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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NF-κB transcription factors (TFs) are homo- or heterodimeric complexes containing NFKB1/p105, NFKB1/p50, NFKB2/p52, REL, RELA/p65, and/or RELB proteins. They bind to κ-B sites in the DNA of their target genes to regulate the expression of genes that influence biological process including immune and inflammatory responses (cytokine production), development, growth, survival, and apoptosis. The different dimers are selective for κ-B sites, and act as transcriptional repressors or activators. The most abundant NF-κB transcriptional activator is the heterodimer containing NFKB1 and RELA. The RELA-REL complex is also an activator.
NF-κB activity is tightly regulated. An inactive state is maintained by interactions between transcriptionally active complexes and inhibitory proteins of the NF-κB inhibitor (I-κB) family. In turn the I-κBs are regulated by phosphorylation (catalysed by kinases IKKα and IKKβ) which promotes ubiquitin dependent degradation. Removal of the I-κBs disinhibits NF-κB TFs which then translocate into the nucleus to drive transcription of target genes. Dysregulated NF-κB pathway activity is associated with human diseases.

Targets

3280
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nuclear factor kappa B subunit 1 Show summary »

nuclear factor kappa B subunit 2 Show summary »

REL proto-oncogene, NF-kB subunit Show summary »

RELA proto-oncogene, NF-kB subunit Show summary »


Target Id 3280
Nomenclature RELA proto-oncogene, NF-kB subunit
Previous and unofficial names NF-κB p65 | NFKB3 | v-rel avian reticuloendotheliosis viral oncogene homolog A | RELA proto-oncogene
Genes RELA (Hs), Rela (Mm), Rela (Rn)
Ensembl ID ENSG00000173039 (Hs), ENSMUSG00000024927 (Mm), ENSRNOG00000030888 (Rn)
UniProtKB AC Q04206 (Hs), Q04207 (Mm)
Inhibitors
RelA inhibitor A55 (Binding) pKd 5.5 [8]
compound 11 [PMID: 30694059] pIC50 5.1 [3] - Mouse
Comment This protein is a component of the most abundant NF-κB transcription complex formed as a heterodimer with NFKB1 (p50). Following viral RNA detection by the RIG-I-like receptor MDA5, the RELA homodimeric NF-κB transcription factor is key to regulating the interferon response to SARS-CoV-2 infection [9].

RELB proto-oncogene, NF-kB subunit Show summary »

References

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How to cite this family page

Database page citation:

NF-kappa B TF proteins. Accessed on 15/02/2025. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=1099.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Buneman OP, Faccenda E, Harding SD, Spedding M, Cidlowski JA, Fabbro D, Davenport AP, Striessnig J, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Introduction and Other Protein Targets. Br J Pharmacol. 180 Suppl 2:S1-22.