ARNT
ARNT (Aryl hydrocarbon receptor nuclear translocator) is a gene whose normal job is to hold cell growth in check. The public catalogues list it as a drug target and a tumour suppressor, and an approved or late-stage drug is recorded against it. Tied to Skin cancer, Breast cancer, Small-cell lung cancer and 1 more.
Overview
Transcription factor that functions as an obligate heterodimerisation partner for several basic helix-loop-helix PER-ARNT-SIM (bHLH-PAS) proteins. Forms heterodimers with the aryl hydrocarbon receptor (AHR) to mediate the transcriptional response to xenobiotics by binding xenobiotic response elements (XREs) or dioxin response elements (DREs) in target gene promoters. Also heterodimerises with hypoxia-inducible factor alpha subunits (HIF1A, EPAS1, NPAS1 or NPAS3) to form hypoxia-inducible transcription factors that bind hypoxia response elements (HREs) and activate genes involved in cellular and systemic responses to hypoxia, including angiogenesis, erythropoiesis, and metabolic adaptation.
Open Targets scores its association with cancer at 0.65 (direct and indirect evidence; datatypes literature 0.91, genetic association 0.23, somatic mutation 0.81). IntOGen calls it a driver in 1 cohort (0 activating, 1 loss-of-function), covering Small Cell Lung Cancer. In OnCo, 1 product record names it (Belzutifan).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · ARNT (Aryl hydrocarbon receptor nuclear translocator) is a gene whose normal job is to hold cell growth in check. The public catalogues list it as a drug target and a tumour suppressor, and an approved or late-stage drug is recorded against it. Tied to Skin cancer, Breast cancer, Small-cell lung cancer and 1 more.
- 1 · What it is
ARNT (Aryl hydrocarbon receptor nuclear translocator) is a gene whose normal job is to hold cell growth in check. The public catalogues list it as a drug target and a tumour suppressor, and an approved or late-stage drug is recorded against it. Tied to Skin cancer, Breast cancer, Small-cell lung cancer and 1 more.
- 2 · What goes wrong in cancer
Transcription factor that functions as an obligate heterodimerisation partner for several basic helix-loop-helix PER-ARNT-SIM (bHLH-PAS) proteins.
- 3 · How drugs use it
No product in this corpus aims at ARNT yet. Because the protein is lost rather than overactive, drugs either restore its function or exploit the weakness its loss leaves (synthetic lethality).
External identifiers
Sources: HGNC HGNC:700 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P27540 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000143437 (association with cancer (MONDO_0004992) 0.65; per-cancer scores at or above 0.5: melanoma 0.56, skin cancer 0.56, breast cancer 0.51 (GraphQL API, CC0)); IntOGen ARNT (driver in 1 cohort (Act 0, LoF 1); Compendium_Cancer_Genes.tsv release 20240920, CC0 1.0)
Biology
Transcription factor that functions as an obligate heterodimerisation partner for several basic helix-loop-helix PER-ARNT-SIM (bHLH-PAS) proteins. Forms heterodimers with the aryl hydrocarbon receptor (AHR) to mediate the transcriptional response to xenobiotics by binding xenobiotic response elements (XREs) or dioxin response elements (DREs) in target gene promoters. Also heterodimerises with hypoxia-inducible factor alpha subunits (HIF1A, EPAS1, NPAS1 or NPAS3) to form hypoxia-inducible transcription factors that bind hypoxia response elements (HREs) and activate genes involved in cellular and systemic responses to hypoxia, including angiogenesis, erythropoiesis, and metabolic adaptation. Plays a central role in environmental sensing and developmental and physiological regulation of gene expression. Location: Nucleus (UniProt). Locus 1q21.3 (HGNC).
- Skin cancer: Open Targets association 0.56 with skin cancer (MONDO_0002898)
- Breast cancer: Open Targets association 0.51 with breast cancer (MONDO_0007254)
- Small-cell lung cancer: IntOGen driver in 1 cohort (SCLC)
- Melanoma: Open Targets association 0.56 with melanoma (MONDO_0005105)
Notes
top- Written by scripts/fetch-cancer-genes.ts from CIViC, Open Targets, IntOGen, HGNC and UniProt; the function text is UniProt's, condensed and in UK spelling. Roles: 1 OnCo product record names it; IntOGen calls it a loss-of-function (LoF) driver in 1 cohort. Evidence tier "approved-drug" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
Latest papers
topQuery for this target: (TITLE:"ARNT" OR ABSTRACT:"ARNT" OR TITLE:"aryl hydrocarbon receptor nuclear translocator" OR ABSTRACT:"aryl hydrocarbon receptor nuclear translocator" OR TITLE:"Aryl hydrocarbon receptor nuclear translocator" OR ABSTRACT:"Aryl hydrocarbon receptor nuclear translocator" OR TITLE:"HIF1B" OR ABSTRACT:"HIF1B" OR TITLE:"HIF-1beta" OR ABSTRACT:"HIF-1beta" OR TITLE:"bHLHe2" OR ABSTRACT:"bHLHe2") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about ARNT, not a curated reading list.
Similar pages
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