Structural highlights
Function
[AHRR_HUMAN] Mediates dioxin toxicity and is involved in regulation of cell growth and differentiation. Represses the transcription activity of AHR by competing with this transcription factor for heterodimer formation with the ARNT and subsequently binding to the xenobiotic response element (XRE) sequence present in the promoter regulatory region of variety of genes. Represses CYP1A1 by binding the XRE sequence and recruiting ANKRA2, HDAC4 and/or HDAC5. Autoregulates its expression by associating with its own XRE site.[1] [2] [ARNT_BOVIN] Required for activity of the Ah (dioxin) receptor. This protein is required for the ligand-binding subunit to translocate from the cytosol to the nucleus after ligand binding. The complex then initiates transcription of genes involved in the activation of PAH procarcinogens (By similarity). The heterodimer with HIF1A or EPAS1/HIF2A functions as a transcriptional regulator of the adaptive response to hypoxia (By similarity).
References
- ↑ Haarmann-Stemmann T, Bothe H, Kohli A, Sydlik U, Abel J, Fritsche E. Analysis of the transcriptional regulation and molecular function of the aryl hydrocarbon receptor repressor in human cell lines. Drug Metab Dispos. 2007 Dec;35(12):2262-9. Epub 2007 Sep 21. PMID:17890447 doi:http://dx.doi.org/10.1124/dmd.107.016253
- ↑ Zudaire E, Cuesta N, Murty V, Woodson K, Adams L, Gonzalez N, Martinez A, Narayan G, Kirsch I, Franklin W, Hirsch F, Birrer M, Cuttitta F. The aryl hydrocarbon receptor repressor is a putative tumor suppressor gene in multiple human cancers. J Clin Invest. 2008 Feb;118(2):640-50. doi: 10.1172/JCI30024. PMID:18172554 doi:http://dx.doi.org/10.1172/JCI30024