nuclear factor, erythroid 2 like 2 | Basic leucine zipper domain TFs | IUPHAR/BPS Guide to PHARMACOLOGY

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nuclear factor, erythroid 2 like 2

target has curated data in GtoImmuPdb

Target id: 3057

Nomenclature: nuclear factor, erythroid 2 like 2

Abbreviated Name: NRF2

Family: Basic leucine zipper domain TFs

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 605 2q31.2 NFE2L2 nuclear factor, erythroid 2 like 2 2
Mouse - 597 2 C3; 2 44.75 cM Nfe2l2 nuclear factor, erythroid derived 2, like 2
Rat - 597 3q23 Nfe2l2 nuclear factor, erythroid 2-like 2
Gene and Protein Information Comments
Multiple transcript variants encoding different isoforms have been characterized for the human gene.
Previous and Unofficial Names
nuclear factor, erythroid derived 2, like 2 | nuclear factor | NF-E2-related factor 2 | nuclear factor, erythroid 2-like 2
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
ML385 Hs Binding - - 3
[3]
Immunopharmacology Comments
NRF2 is included in GToImmuPdb as mutations in this gene have been reported in patients with IMDDHH, an inherited disease in which some of the symptoms arise from defective immune system function [1].
Immuno Process Associations
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0016567 protein ubiquitination IDA
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0071356 cellular response to tumor necrosis factor IMP
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes, IEA only
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GO:1902037 negative regulation of hematopoietic stem cell differentiation IEA
Immuno Process:  Immune system development
GO Annotations:  Associated to 1 GO processes, IEA only
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GO:1902037 negative regulation of hematopoietic stem cell differentiation IEA
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes, IEA only
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GO:0006954 inflammatory response IEA
Immuno Disease Associations
Disease Name:  Immunodeficiency, developmental delay, and hypohomocysteinemia (IMDDHH)
Disease Synonyms:  no synonynms
Comment:  IMDDHH is associated with heterozygous missense mutations in the NFE2L2 gene. The mutations detected affect the N-terminal Neh2 domain of NRF2 that facilitates binding to inhibitory KEAP1 proteins (so KEAP1 inhibition of NRF2 is reduced), and this subsequently leads to chronic activation of NRF2-responsive stress response genes.
Disease X-refs:  OMIM: 617744
References:  1
General Comments
NRF2 is a transcription factor that activates expression of genes containing the antioxidant response element (ARE). ARE-containing genes are involved in the physiological response to cellular insults such as oxidative stress.

References

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1. Huppke P, Weissbach S, Church JA, Schnur R, Krusen M, Dreha-Kulaczewski S, Kühn-Velten WN, Wolf A, Huppke B, Millan F et al.. (2017) Activating de novo mutations in NFE2L2 encoding NRF2 cause a multisystem disorder. Nat Commun, 8 (1): 818. [PMID:29018201]

2. Moi P, Chan K, Asunis I, Cao A, Kan YW. (1994) Isolation of NF-E2-related factor 2 (Nrf2), a NF-E2-like basic leucine zipper transcriptional activator that binds to the tandem NF-E2/AP1 repeat of the beta-globin locus control region. Proc. Natl. Acad. Sci. U.S.A., 91 (21): 9926-30. [PMID:7937919]

3. Singh A, Venkannagari S, Oh KH, Zhang YQ, Rohde JM, Liu L, Nimmagadda S, Sudini K, Brimacombe KR, Gajghate S et al.. (2016) Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors. ACS Chem. Biol., 11 (11): 3214-3225. [PMID:27552339]

How to cite this page

Basic leucine zipper domain TFs: nuclear factor, erythroid 2 like 2. Last modified on 05/12/2018. Accessed on 23/10/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3057.